Disease Information

Drug Dictionary

(61)Cu-ATSM

A lipophilic copper(II)bis(thiosemicarbazone) labeled with the positron-emitting isotope (61)Cu with hypoxia-selective and radioisotopic activities. With a high membrane permeability and redox potential, (61)Cu-ATSM easily enters and selectively resides in hypoxic cells. The extent of (61)Cu-ATSM retention in tissue is inversely related to the state of tissue oxygenation allowing the quantitation of tissue hypoxia with positron emission tomography (PET).

1-methyl-d-tryptophan

A methylated tryptophan with anti-immunosuppressive activity. 1-methyl-d-tryptophan inhibits the enzyme indoleamine 2,3-dioxygenase (IDO), which degrades the essential amino acid tryptophan, and may increase or maintain tryptophan levels important to T cell function. Tryptophan depletion is associated with immunosuppression involving T cell arrest and anergy.

11C topotecan

A semisynthetic derivative of camptothecin, a cytotoxic, quinoline-based alkaloid extracted from the Asian tree Camptotheca acuminata radiolabeled with carbon 11 (11C) with antineoplastic and radiotracer properties. During the S phase of the cell cycle, topotecan inhibits topoisomerase I activity by stabilizing the cleavable complex between topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptotic cell death. Quantitation of 11C topotecan accumulated in tumor tissues by positron emission tomography (PET) may help predict responses to topotecan therapy.

123-I-MIP-1095

An iodine 123-radiolabled small molecule that exhibits high affinity for prostate-specific membrane antigen (PSMA) with potential use in molecular imaging. 123-I-MIP-1095, a radiolabeled glutamate-urea-lysine analogue, selectively binds PSMA, which allows imaging of PSMA-expressing prostate cancer cells with gamma scintigraph. PSMA is a transmembrane glycoprotein highly expressed by malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.

131I-TM-601

An iodine 131 (I 131) radioconjugate of the synthetic chlorotoxin (CTX) TM-601 with potential antiangiogenic and antineoplastic activities. CTX is a 36 amino acid neurotoxin found in the venom of the giant yellow scorpion Leiurus quinquestriatus that preferentially binds malignant cells of neuroectodermal origin. The recombinant version of this peptide, TM-601, is expressed in and purified from E. coli and then covalently linked to I 131 to produce 131I-TM-601. 131I-TM-601 binds to tumor cells of neuroectodermal origin and is internalized; administered once, it may be used as a radioimaging agent; repeated administration may result in a tumor-specific, cumulative radiocytotoxic dose of I 131. In addition, TM-601 alone, similar to native CTX, may inhibit angiogenesis due to its ability to bind to and inhibit matrix metalloproteinase 2 (MMP-2), an endopeptidase involved in tissue remodeling processes such as angiogenesis.

14C BMS-275183

The orally bioavailable C-4 methyl carbonate analogue of paclitaxel, labeled with radioactive carbon 14, with radioisotope and potential antineoplastic activities. 14C BMS-275183 binds to tubulin and inhibits microtubule disassembly, which may result in cell cycle arrest at the G2/M phase and inhibition of cell division, and subsequently cell death. This agent may be useful for treating multi-drug resistant (MDR) tumors because it does not appear to be a substrate for P-glycoprotein.

16, 16-dimethyl prostaglandin E2

A stable derivative of prostaglandin E2 (PGE2) with potential hematopoietic activity. Administration of 16,16 dimethyl-prostaglandin E2 (dmPGE2) appears to lead to increased formation of hematopoietic stem and progenitor cells. Even though the exact mechanism of action has yet to be fully elucidated, this agent may stimulate hematopoiesis by activating the Wnt signaling pathway, which increases cellular levels of beta-catenin, a subunit of the cadherin protein complex.

18-F-fluoroacetate

A radioconjugate and an acetate analog labeled with fluorine F 18 ((18)F-FAC), a positron-emitting isotope, with potential prostate tumor tracer property using positron emission tomography (PET). Although the mechanism of action is unclear, fluorine F 18 acetate preferentially accumulates in tumor tissue, serving as a tracer for imaging tumors with PET. Fluorine 18 has a longer radioactive half-life (110 min) vs. the half-life of carbon-11 acetate (20.4 min). Furthermore, (18)F-FAC showed a rapid clearance from liver and extensive excretion to bile and urine in comparison with carbon-11 acetate, therefore this tracer may be a useful alternative to C-11 acetate for the detection of prostate tumors by PET.

18F-FHBG

A fluorine-18-labeled acycloguanosine derivative substrate for herpes simplex virus type-1 thymidine kinase (HSV1-tk). 18F-FHBG is used as a reporter probe to image the expression of the herpes simplex virus type-1 thymidine kinase (HSV1-tk) gene in gene transfer therapy. HSV1-tk and and HSV1-tk-metabolized 18F-FHBG co-localize, allowing positron emission tomography (PET) localization of HSV1-tk gene-transfected tissue and the assessment of gene transfer efficiency.

18F-fluoroazomycin arabinoside

A radiofluorinated 2-nitroimidazole derivative with hypoxia-specific tracer activity. 18F-fluoroazomycin arabinoside is reduced under hypoxic conditions and is often seen in various malignant tumors, forming highly reactive intermediates. In its reduced form, 18F-fluoroazomycin arabinoside covalently binds to macromolecules, thereby accumulating in hypoxic cells and allowing radioisotopic imaging of these particular cells. Compared to 18F-misonidazole, 18F-fluoroazomycin arabinoside has a lower octanol:water partition coefficient; it therefore has less tendency to accumulate in lipophilic tissues and exhibits a faster renal clearance, leading to an improved imaging ability of hypoxic tissue.

18F-fluoromethylcholine

A radiotracer consisting of methylcholine labeled with the positron-emitting radioisotope fluorine F 18 (18F-FMCH) with potential imaging use. Upon administration, 18F-fluoromethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, an enzyme frequently upregulated in human tumors, yielding phosphoryl 18F-fluoromethylcholine. In turn, phosphoryl 18F-fluoromethylcholine is integrated into phospholipids in the cell membrane as part of phosphatidylcholine. As the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of 18F-FMCH uptake and incorporation, allowing tumor imaging with positron emission tomography (PET).

18F-fluoromisonidazole

A radiofluorinated 2-nitroimidazole derivate with hypoxia-specific tracer activity. Misonidazole is reduced under hypoxic conditions and in reduced form covalently binds to macromolecules in hypoxic cells. 18F (fluorine-18) radiofluorination of misonidazole to form 18F-fluoromisonidazole allows radioisotopic imaging of reduced misonidazole bound to macromolecules in hypoxic cells.

18F-labeled mini-PEG spacered RGD dimer

A radiotracer containing a pegylated dimeric Arg-Gly-Asp (RGD) peptide (NH2-mini-PEG-E[c(RGDyK)]2 or PRGD2) radiolabeled with fluorine 18F-fluorobenzoate (18F-FB), with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). Upon administration, the RGD moiety of 18F-labeled mini-PEG spacered RGD dimer (18F-FPRGD2) binds to alphaVbeta3 integrin. Upon PET, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. This agent exhibits increased integrin receptor binding affinity, tumor cell uptake and increased radiolabeling yield as compared to the non-pegylated form (18F-FRGD2). Integrins, transmembrane glycoproteins, may be upregulated on proliferating tumor vessel endothelial cells and various cancer cells; their overexpression has been associated with neovascularization, differentiation, proliferation of tumor cells, metastasis and an overall poor prognosis.

2'-F-ara-deoxyuridine

A deoxyuridine prodrug with potential antineoplastic activity. Upon cellular uptake, 2-F-ara-deoxyuridine (FAU) is phosphorylated by thymidine kinase to FAU monophosphate and subsequently methylated in the 5'-position by thymidylate synthase (TS) to its activated form, 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) 5-methyluracil monophosphate (FMAUMP). FMAUMP is incorporated into DNA leading to an inhibition of DNA synthesis and so cell growth. The catalytic activity of TS is critical to activation of FAU and subsequent incorporation into DNA. FAU may be beneficial in the case of tumors with high TS activity that are resistant to TS inhibitors.

2-0, 3-0 desulfated heparin

A non-anticoagulant heparin derivative in which the 2-O and 3-O sulfate groups of heparin are removed, with potential anti-inflammatory and antineoplastic activity. Upon administration, 2-O, 3-O desulfated heparin (ODSH) prevents the interaction of the receptor for advanced glycation end-products (RAGE) to its ligands, such as advanced glycation end-products (AGEs), Mac-1(CD11b/CD18), the nuclear protein high mobility group box protein-1 (HMGB-1), carboxymethyl lysine-bovine serum albumin (CML-BSA) and members of the S100 calgranulin family. In addition, this agent inhibits the enzymes heparanase, cathepsin G, and human leukocyte elastase, which are involved in inflammation and metastasis. ODSH also inhibits selectins, thereby preventing the adhesion of tumor cells to endothelium and platelets. Altogether, this may inhibit tumor cell invasiveness and metastasis. Unlike heparin, this agent does not induce heparin-induced thrombocytopenia (HIT). RAGE, a receptor belonging to the immunoglobulin superfamily, plays a key role in inflammation and is overexpressed in a variety of cancers.

2-fluoropropionyl-labeled pegylated dimeric RGD peptide

A radiopharmaceutical agent comprised of a pegylated dimeric arginine-glycine-aspartic acid (RGD)-based peptide labeled with 2-fluoropropionyl, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). The RGD moiety of 2-fluoropropionyl-labeled pegylated dimeric RGD peptide targets and binds to alphaVbeta3 integrin. Upon PET imaging, alphaVbeta3 integrin-expressing tumor cells can be visualized and expression levels can be quantified. Compared to other fluorine F 18 labeled RGD-containing peptides, this agent shows increased affinity to alphaVbeta3 integrin, enhanced tumor uptake as well as improved pharmacokinetics. alphaVbeta3 integrin, overexpressed on certain tumor cells and tumor endothelial cells, plays a key role in angiogenesis, tumor proliferation and survival.

2-hydroxyflutamide depot

A depot formulation containing a bioresorbable, controlled-release, calcium sulphate-based paste of the nonsteroidal antiandrogen 2-hydroxyflutamide (2-HOF) with potential antineoplastic activity. Upon injection into the tumor site in the prostate, 2-hydroxyflutamide depot slowly releases 2-HOF, which competitively binds to androgen receptors (ARs), blocking the binding of dihydrotestosterone (DHT). This may inhibit androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest and decreased cellular proliferation. In addition, 2-HOF inhibits nuclear uptake of androgen in androgen-responsive tissues.

2-hydroxyoleic acid

An orally bioavailable, synthetic analog of the fatty acid oleic acid, with potential antitumor activity. Upon administration, 2-hydroxyoleic acid (2OHOA) activates sphingomyelin synthase (SMS), thereby increasing the concentration of sphingomyelin (SM) and diacylglycerol (DAG) in the tumor cell membrane and decreasing membrane levels of phosphatidylethanolamine (PE) and phosphatidylcholine (PC). This restores the normal, healthy levels and ratios of membrane lipids. By restoring normal membrane lipid structure and composition, this agent inhibits membrane-protein associated signaling and the aberrant activity of signaling pathways in certain tumor cells, including the Ras/MAPK and PI3K/AKt pathways. This inhibits tumor cell proliferation, induces tumor cell differentiation, and eventually can cause cell death.

2-methoxyestradiol

An orally bioavailable estradiol metabolite with potential antineoplastic activity. 2-Methoxyestradiol inhibits angiogenesis by reducing endothelial cell proliferation and inducing endothelial cell apoptosis. This agent also inhibits tumor cell growth by binding to tubulin, resulting in antimitotic activity, and by inducing caspase activation, resulting in cell cycle arrest in the G2 phase, DNA fragmentation, and apoptosis.

2G-1 TCR retroviral vector-transduced lymphocytes

A preparation of autologous human T-lymphocytes isolated from renal cell cancer (RCC) patient and transduced with 2G-1 TCR, a retroviral vector encoding the alpha and beta chains of a T-cell receptor that recognizes TNF-related apoptosis inducing ligand (TRAIL) bound to death receptor 4 (DR4), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and introduction into the RCC patient, 2G-1 TCR retroviral vector-transduced lymphocytes may stimulate a cytotoxic T lymphocyte (CTL) response against RCC cells with TRAIL bound to DR4 on their surfaces. TRAIL, a member of the TNF superfamily, is a homotrimeric type II membrane protein that rapidly induces oligomerization of receptor intracellular death domains and apoptosis in a variety of tumor cells when bound to its receptors; DR4 (TRAIL receptor 1), a member of the TNF receptor family, is overexpressed by a variety of malignant cell types.

3'-aminomethyl nicotine-P. aeruginosa r-exoprotein A conjugate vaccine

A hapten-carrier immunoconjugate composed of the hapten trans-3-aminomethyl nicotine conjugated to a recombinant P. aeruginosa exoprotein A, rendered nontoxic through amino acid depletion, with potential immunostimulating activity. Upon vaccination with 3'-aminomethyl nicotine-P. aeruginosa r-exoprotein A conjugate vaccine, the immune system may produce anti-nicotine antibodies. Antibody-bound nicotine cannot pass the blood brain barrier (BBB) to activate brain nicotine receptors. Nicotine, a small organic molecule that is notimmunogenic, must be haptenized and conjugated to a carrierprotein, such as nontoxic recombinant P. aeruginosa exoprotein A, to induce an antibody response. Aluminiumhydroxide may be used as an adjuvant for this vaccine.

3'-C-ethynylcytidine

A synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule.

3,4-methylenedioxymethamphetamine

A ring-substituted amphetamine derivative, structurally related to the hallucinogen mescaline, with entactogenic, neurotoxic, and motor-stimulatory activities. 3,4-methylenedioxymethamphetamine (MDMA) produces an acute, rapid enhancement in both the release of serotonin from and the inhibition of serotonin reuptake by serotonergic nerve endings in the brain. Once within the cell, MDMA depletes stores of tryptophan hydroxylase (TPH) via acute oxidative inactivation; in turn, depleted stores of TPH leave cell terminals open to damage from oxidative stress, possibly a source of MDMA neurotoxicity. This agent also induces norepinephrine, dopamine, and acetylcholine release and can act directly on a number of receptors, including alpha 2-adrenergic and 5-hydroxytryptamine (5-HT) 2A receptors. MDMA may suppress the dyskinesia associated with long-term use of L-dopamine (L-DOPA) without affecting the efficacy of L-DOPA treatment.

3-deazauridine

A synthetic analogue of nucleoside uridine lacking a ring nitrogen in the 3-position. 3-deazauridine inhibits cytidine synthase, thereby reducing intracellular levels of cytidine and deoxycytidine and disrupting DNA and RNA synthesis. This agent may trigger apoptosis and enhance differentiation of neoplastic cells..

4'-iodo-4'-deoxydoxorubicin

An iodinated doxorubicin analogue with antiamyloid activity. 4'-Iodo-4'-deoxydoxorubicin (IDOX) binds with high affinity to five types of natural amyloid fibrils including immunoglobulin light chains, amyloid A, transthyretin (methionine-30 variant), -protein (Alzheimer), and 2-microglobulin. This agent may inhibit fibril growth, increasing the solubility of amyloid tissue deposits and facilitating their clearance. IDOX has also been shown to insulin amyloid fibrillogenesis in vitro.

4-nitroestrone 3-methyl ether

A synthetic derivative of estradiol. 4-nitroestrone 3-methyl ether inhibits estrogen sulfotransferase (EST), a progesterone-induced secretory endometrial enzyme which affects estrogen receptor levels. This agent has been shown to be an effective growth inhibitor of some chemically induced animal mammary tumors.

4-peptide melanoma vaccine

An emulsion of 4 melanoma peptides with potential immunomodulating and antineoplastic activities. Upon vaccination, 4-peptide melanoma vaccine may stimulate an immune response against 4 different melanoma associated antigens. This may lead to a reduction in tumor cell proliferation of cancer cells expressing these antigens.

5-FITC-labeled GI-heptapeptide

A radioconjugate consisting of the 7 amino acid peptide sequence ASYNYDA (GI heptapeptide) and labeled with the fluorescent dye fluorescein isothiocyanate (5-FITC), with potential imaging activity. Upon topical application to the esophageal mucosa using a spray, the heptapeptide moiety of 5-FITC-labeled GI-heptapeptide binds to abnormal cells in the esophagus; the FITC moiety allows for imaging with white light and the area of interest for biopsies can then be visualized.

5-fluoro-2-deoxycytidine

A fluorinated pyrimidine analogue antimetabolite with potential antineoplastic activity. As a prodrug, 5-fluoro-2-deoxycytidine is converted by intracellular deaminases to the cytotoxic agent 5-fluorouracil (5-FU). 5-FU is subsequently metabolized to active metabolites including 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP). FdUMP binds to and inhibits thymidylate synthase, thereby reducing the production of thymidine monophosphate, which leads to depletion of thymidine triphosphate and the inhibition of DNA synthesis and cell division. FUTP competes with uridine triphosphate (UTP) for incorporation into the RNA strand, which results in the inhibition of RNA and protein synthesis and cell proliferation. Other fluorouracil metabolites also get incorporated into both DNA and RNA, with further inhibition of cellular growth.

5-fluorouracil/salicylic acid topical solution

A topical formulation containing 0.5 % of antimetabolite 5-fluorouracil (5-FU) and 10% of salicylic acid, with potential antimitotic and keratolytic activity. Upon cutaneous application, 5-FU in the 5-fluorouracil/salicylic acid topical solution impedes pyrimidine metabolism thereby inhibiting cell growth, while the salicylic acid induces anti-inflammatory response and results in keratolytic effect. This may result in the breakdown of keratinocytes and prevent proliferation of keratinocytes locally.

5-[18F]fluorouracil

The fluorine-18 (18F)-radiolabeled pyrimidine analog 5-fluorouracil (5-FU) with positron-emitting activity. Upon administration, 5-[18F]fluorouracil distribution in tumor tissue may be measured with positron emission tomography (PET). The degree of 5-[18F]fluorouracil uptake in tumor tissue may help to predict the response to 5-fluorouracil-based chemotherapy or to determine the response to other therapeutic agents used to treat 5-FU-sensitive tumors.

50% oxygen/50% nitrous oxide premix

An equimolar gas mixture of oxygen (O2) and nitrous oxide (N2O) with potential analgesic activity. Upon inhalation, 50% oxygen/50% nitrous oxide premix produces rapidly reversible analgesia. The exact mechanism through which nitrous oxide exerts its analgesic effect has yet to be fully elucidated, but it appears to be associated with the neuronal release of endogenous opioid peptides.

6,8-bis(benzylthio)octanoic acid

A racemic mixture of the enantiomers of a synthetic alpha-lipoic lipoic acid analogue with potential chemopreventive and antineoplastic activities. Although the exact mechanism of action is unknown, 6,8-bis(benzylthio)octanoic acid has been shown to inhibit metabolic and regulatory processes required for cell growth in solid tumors. Both enantiomers in the racemic mixture exhibit antineoplastic activity.

6-azauridine

A synthetic triazine analogue of uridine with antimetabolite activity. 6-azauridine inhibits de novo pyrimidine synthesis and DNA synthesis and is converted intracellularly into mono, di-, and triphosphate derivatives, which incorporate into RNA and inhibit protein synthesis.

7-cyanoquinocarcinol

A semisynthetic analogue of the Streptomyces melanovinaceus-derived tetracyclic antitumor antibiotic quinocarmycin with potential antineoplastic activity. Quinocarmycin belongs to the naphthyridinomycin/saframycin class of antitumor antibiotics. These antibiotics appear to act through DNA alkylation.

7-hydroxystaurosporine

A synthetic derivative of staurosporine with antineoplastic activity. 7-hydroxystaurosporine inhibits many phosphokinases, including the serine/threonine kinase AKT, calcium-dependent protein kinase C, and cyclin-dependent kinases. This agent arrests tumor cells in the G1/S of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase chk1, resulting in apoptosis.

8-hydroxyquinoline sulfate ointment

An ointment formulation containing the sulfate salt of 8-hydroxyquinoline in a petrolatum and lanolin base with skin-protecting activity. Upon topical application, 8-hydroxyquinoline sulfate exhibits antiseptic activity while lanolin moisturizes and softens skin.

851B gel

A topical gel containing a peptide derived from the human papillomavirus (HPV). Application of 851B gel may stimulate the host immune system to trigger a cytotoxic T-lymphocyte response to cells that express HPV.

852A

A synthetic imidazoquinoline Toll-like receptor 7 (TLR7) agonist with immunostimulating and potential antitumor activities. TLR7 agonist 852A binds to and activates TLR7, thereby stimulating plasmacytoid dendritic cells (pDC) through the TLR7-MyD88-dependent signaling pathway. Activation of pDC results in secretion of interferon alpha, the production of proimflammatory cytokines, the upregulation of co-stimulatory molecules, and enhanced T and B-cell stimulatory responses.

99mTc-DTPA-mannosyl-dextran

A radiolabeled macromolecule consisting of the chelating agent diethylenetriamine pentaacetic acid (DTPA) and mannose each attached to a dextran backbone and labeled with metastable technetiumTc-99 (Tc-99m), with mannose binding and radioisotopic activities. Upon injection, the mannose moiety of 99mTc-DTPA-mannosyl-dextran binds to mannose-binding protein (MBP). As MBPs reside on the surface of dendritic cells and macrophages, this gamma-emitting macromolecule tends to accumulate in lymphatic tissue where it may be imaged using gamma scintigraphy. This agent exhibits rapid clearance from the injection site, rapid uptake and high retention within the first draining lymph node, and low uptake by the remaining lymph nodes. MBP is a C-type lectin that binds mannose or fucose carbohydrate residues, such as those found on the surfaces of many pathiogens, and once bound activates the complement system.

A-Hydrocort

(Other name for: hydrocortisone sodium succinate)

abagovomab

A murine IgG1 monoclonal anti-idiotype antibody, containing a variable antigen-binding region that functionally mimics the three-dimensional structure of a specific epitope on the ovarian cancer tumor-associated antigen CA-125, with potential antineoplastic activity. With a variable antigen-binding region that acts as a surrogate antigen for CA-125, abagovomab may stimulate the host immune system to elicit humoral and cellular immune responses against CA-125-positive tumor cells, resulting in inhibition of tumor cell proliferation.

abarelix

A synthetic decapeptide and antagonist of naturally occurring gonadotropin-releasing hormone (GnRH). Abarelix directly and competitively binds to and blocks the gonadotropin releasing hormone receptor in the anterior pituitary gland, thereby inhibiting the secretion and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH). In males, the inhibition of LH secretion prevents the release of testosterone. As a result, this may relieve symptoms associated with prostate hypertrophy or prostate cancer, since testosterone is required to sustain prostate growth.

abatacept

A soluble fusion protein consisting of the extracellulardomain of human cytotoxic T lymphocyte-associated antigen 4 (CTLA-4) linked toa modified Fc (hinge, CH2, and CH3 domains) portion of human immunoglobulin G1(IgG1) with immunosuppressive activity. Abatacept binds CD80 and CD86 on antigen presenting cells (APCs), blocking interaction with CD28 on T lymphocytes, which initiates a co-stimulatory signal required for full activation of T lymphocytes.

Abegrin

(Other name for: etaracizumab)

Abelcet

(Other name for: liposomal amphotericin B)

Aberel

(Other name for: tretinoin)

abexinostat

A novel, broad-spectrum hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. Abexinostat inhibits several isoforms of HDAC, resulting in an accumulation of highly acetylated histones, followed by the induction of chromatin remodeling; the selective transcription of tumor suppressor genes; and the tumor suppressor protein-mediated inhibition of tumor cell division and induction of tumor cell apoptosis. HDAC, upregulated in many tumor types, is an an enzyme that is responsible for the deacetylation of chromatin histone proteins.

abiraterone acetate

An orally active acetate salt of the steroidal compound abiraterone with antiandrogen activity. Abiraterone inhibits the enzymatic activity of steroid 17alpha-monooxygenase (17alpha-hydrolase/C17,20 lyase complex), a member of the cytochrome p450 family that catalyzes the 17alpha-hydroxylation of steroid intermediates involved in testosterone synthesis. Administration of this agent may suppress testosterone production by both the testes and the adrenals to castrate-range levels.

Abitrexate

(Other name for: methotrexate)

Ablavar

(Other name for: gadofosveset trisodium)

Abraxane

(Other name for: paclitaxel albumin-stabilized nanoparticle formulation)

absorbable adhesion barrier gel

An isotonic, sterile, absorbable adhesion barrier gel composed of polyethylene oxide and sodium carboxymethylcellulose, with protective activity. Upon application of a single layer into the uterine cavity at the end of any hysteroscopic surgery, the absorbable adhesion barrier gel may provide a protective barrier which protects the traumatized tissue and allows for healing. This gel may therefore prevent the formation of post-surgical intrauterine adhesions.

absorbable gelatin sponge

A sterile hemostatic agent composed of purified porcine-derived gelatin. In regional chemotherapy, absorbable gelatin sponge may be used to embolize arteries in the region of a tumor in order to block or retard blood flow; this blockage results in a locally increased concentration of chemotherapeutic agents delivered to the tumor when chemotherapeutic agents are infused into the embolized arterial circulation upstream of the blockage.

ABT-510

A synthetic peptide that mimics the anti-angiogenic activity of the endogenous protein thrombospondin-1 (TSP-1). ABT-510 inhibits the actions of several pro-angiogenic growth factors important to tumor neovascularization; these pro-angiogenic growth factors include vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF)), hepatocyte growth factor (HGF), and interleukin 8 (IL-8).

ABT-751

An orally bioavailable antimitotic sulfonamide. ABT-751 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of microtubules, thereby preventing tumor cell replication. This agent also disrupts tumor neovascularization, reducing tumor blood flow and so inducing a cytotoxic effect.

ABVD regimen

A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin), bleomycin, vinblastine and dacarbazine, used alone or in combination with radiation therapy, for the primary treatment of Hodgkin lymphoma. (NCI Thesaurus)

ABVE regimen

A regimen containing doxorubicin hydrochloride, bleomycin sulfate, vincristine sulfate and etoposide used in combination with radiation therapy for the treatment of low-risk, childhood Hodgkin lymphoma. (NCI Thesaurus)

ABVE-PC regimen

A regimen consisting of doxorubicin, bleomycin, vincristine, etoposide, prednisone and cyclophosphamide, given in combination with radiation therapy and used for the treatment of high-risk, childhood Hodgkin's lymphoma. (NCI Thesaurus)

AC regimen

A chemotherapy regimen consisting of doxorubicin hydrochloride (Adriamycin) and cyclophosphamide used in the adjuvant setting for the primary treatment of breast cancer. This regimen is also used for the treatment of recurrent and metastatic breast cancer. (NCI Thesaurus)

AC-T regimen

A chemotherapy regimen consisting of doxorubucin hydrochloride (Adriamycin) and cyclophosphamide, followed by paclitaxel (Taxol), administered on either a dose-dense or sequential schedule and used as an adjuvant treatment for breast cancer. (NCI Thesaurus)

acadesine

A 5-aminoimidazole-4-carboxamide (AICA) riboside, a purine nucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. Following cellular uptake, acadesine is phosphorylated to AICA ribotide (ZMP), which mimics 5'-adenosine monophosphate (AMP). Both AMP-activated protein kinase (AMPK) and AMPK kinase (AMPKK) are activated by ZMP, which appears to be necessary for the induction of apoptosis. Acadesine-induced apoptosis also appears to require cytochrome c release from mitochondria and caspase activation and is p53-independent. However, the exact mechanism of acadesine-induced apoptosis is unknown. T cells are significantly less susceptible than B cells to acadesine-induced apoptosis. AMPK regulates several cellular systems including the cellular uptake of glucose, the beta-oxidation of fatty acids, protein synthesis, and the biogenesis of glucose transporter 4 (GLUT4) and mitochondria.

acai berry juice

A juice product obtained from the fruit of the acai palm tree (Euterpe oleracea) with anti-inflammatory, antioxidant and potential chemopreventive activities. Besides high amounts of vitamins, minerals and fatty acids, acai berry is rich in phytonutrients such as anthocyanins and flavones which are potent scavengers of reactive oxygen species. The fruit also contains high amounts of the flavone velutin which exhibits potent anti-inflammatory properties. Velutin is able to inhibit the degradation of the inhibitor of nuclear factor kappa-B (NF-kB), thereby blocking the activation of NF-kB, as well as inhibiting phosphorylation of mitogen-activated protein kinase p38 and JNK. Inhibition of these processes results in suppression of the production of proinflammatory cytokines, such as tumor necrosis factor alpha and interleukin 6.

acarbose

A complex oligosaccharide used as a hypoglycemic agent in diabetes management. Acarbose inhibits enzymes required in catabolism of carbohydrates, specifically pancreatic alpha-amylase, which hydrolyzes complex starches to oligosaccharides in the lumen of the small intestine, and the membrane-bound intestinal alpha-glucosidases, which hydrolyze oligosaccharides, trisaccharides, and disaccharides to glucose and other monosaccharides in the small intestine. When acarbose is orally administered, less digestion of complex carbohydrates occur and less glucose is absorbed in the small intestine, thereby producing a smaller rise in postprandial blood glucose levels after a carbohydrate load.

Accutane

(Other name for: isotretinoin)

acelullar cadaveric dermal matrix

A human dermis-derived allograft material. Acellular cadaveric dermal matrix (ACDM) is derived from human cadaveric dermis from which the epidermis, all viable cells and major histocompatibility class (MHC) II antigens have been removed to minimize alloimmunogenicity, while the dermal collagen matrix is preserved. ACDM may placed over wounds to aid as a substitute for skin when necessary such as for surgical reconstruction or for protection against wound exposure and breakdown and wound infection.

acenocoumarol

A 4-hydroxycoumarin derivative with anticoagulant activity. As a vitamin K antagonist, acenocoumarol inhibits vitamin K epoxide reductase, thereby inhibiting the reduction of vitamin K and the availability of vitamin KH2. This prevents gamma carboxylation of glutamic acid residues near the N-terminals of the vitamin K-dependent clotting factors, including factor II, VII, IX, and X and anticoagulant proteins C and S. This prevents their activity and thus thrombin formation. Compared to other coumarin derivatives, acenocoumarol has a short half-life.

Aceon

(Other name for: perindopril erbumine)

acetaminophen

A p-aminophenol derivative with analgesic and antipyretic activities. Although the exact mechanism through which acetaminophen exert its effects has yet to be fully determined, acetaminophen may inhibit the nitric oxide (NO) pathway mediated by a variety of neurotransmitter receptors including N-methyl-D-aspartate (NMDA) and substance P, resulting in elevation of the pain threshold. The antipyretic activity may result from inhibition of prostaglandin synthesis and release in the central nervous system (CNS) and prostaglandin-mediated effects on the heat-regulating center in the anterior hypothalamus.

acetic acid

A synthetic carboxylic acid with antibacterial and antifungal properties. Although its mechanism of action is not fully known, undissociated acetic acid may enhance lipid solubility allowing increased fatty acid accumulation on the cell membrane or in other cell wall structures. Acetic acid, as a weak acid, can inhibit carbohydrate metabolism resulting in subsequent death of the organism.

acetylcysteine

A synthetic N-acetyl derivative of the endogenous amino acid L-cysteine, a precursor of the antioxidant enzyme glutathione. Acetylcysteine regenerates liver stores of glutathione. This agent also reduces disulfide bonds in mucoproteins, resulting in liquification of mucus. Some evidence suggests that acetylcysteine may exert an anti-apoptotic effect due to its antioxidant activity, possibly preventing cancer cell development or growth. In addition, acetylcysteine has inhibited viral stimulation by reactive oxygen intermediates, thereby producing antiviral activity in HIV patients.

acetylsalicylic acid

An orally administered non-steroidal antiinflammatory agent. Acetylsalicylic acid binds to and acetylates serine residues in cyclooxygenases, resulting in decreased synthesis of prostaglandin, platelet aggregation, and inflammation. This agent exhibits analgesic, antipyretic, and anticoagulant properties.

acetylsalicylic acid/simvastatin/atenolol/ramipril/thiazide capsule

An orally bioavailable combination pill containing aspirin, simvastatin, atenolol, ramipril and thiazide with preventive activity against cardiovascular disease (CVD). Aspirin is a cyclooxygenase inhibitor with antiplatelet, analgesic, antipyretic and anti-inflammatory activities; simvastatin is a statin with a cholesterol lowering effect; and the beta-blocker atenolol as well as the ACE inhibitor ramipril and the thiazide diuretic all have blood pressure lowering activity. Upon oral administration of aspirin/simvastatin/atenolol/ramipril/thiazide capsule, the combined effects of the active ingredients in this formulation lower the risk of CVD.

Achromycin

(Other name for: tetracycline hydrochloride)

Aciphex

(Other name for: rabeprazole sodium)

acitretin

An orally-active metabolite of the synthetic aromatic retinoic acid agent etretinate with potential antineoplastic, chemopreventive, anti-psoratic, and embryotoxic properties. Acitretin activates nuclear retinoic acid receptors (RAR), resulting in induction of cell differentiation, inhibition of cell proliferation, and inhibition of tissue infiltration by inflammatory cells. This agent may also inhibit tumor angiogenesis.

acivicin

A modified amino acid and structural analog of glutamine. Acivicin inhibits glutamine amidotransferases in the purine and pyrimidine biosynthetic pathways, thereby inhibiting tumor growth in cell lines dependent on glutamine metabolism.

aclarubicin

An oligosaccharide anthracycline antineoplastic antibiotic isolated from the bacterium Streptomyces galilaeus. Aclarubicin intercalates into DNA and interacts with topoisomerases I and II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. Aclarubicin is antagonistic to other agents that inhibit topoisomerase II, such as etoposide, teniposide and amsacrine. This agent is less cardiotoxic than doxorubicin and daunorubicin.

Acnestrol

(Other name for: diethylstilbestrol)

ACNU 50

(Other name for: nimustine)

acodazole

A synthetic imidazoquinoline with antineoplastic activity. Acodazole intercalates into DNA, resulting in disruption of DNA replication. Use of this agent has been associated with significant cardiotoxicity.

acridine carboxamide

A tricyclic acridine-based (or carboxamide-based) drug with dual topoisomerase inhibitor and potential antineoplastic activities. Acridine carboxamide inhibits both topoisomerases I and II and intercalates into DNA, resulting in DNA damage, the disruption of DNA repair and replication, the inhibition of RNA and protein synthesis, and cell death.

Actemra

(Other name for: tocilizumab)

ActHIB

(Other name for: Haemophilus influenzae b vaccine)

Actigall

(Other name for: ursodiol)

Actimmune

(Other name for: recombinant interferon gamma)

Actinex

(Other name for: masoprocol)

actinium Ac 225 lintuzumab

A radioimmunoconjugate consisting of the humanized monoclonal antibody lintuzumab conjugated to the alpha-emitting radioisotope actinium Ac 225 with potential antineoplastic activity. The monoclonal antibody moiety of actinium Ac 225 lintuzumab specifically binds to the cell surface antigen CD33 antigen, delivering a cytotoxic dose of alpha radiation to cells expressing CD33. CD33 is a cell surface antigen expressed on normal non-pluripotent hematopoietic stem cells and overexpressed on myeloid leukemia cells.

Actiq

(Other name for: fentanyl citrate)

Activase

(Other name for: alteplase)

Activella

(Other name for: estradiol/norethindrone acetate tablet)

ActiVin

(Other name for: IH636 grape seed proanthocyanidin extract)

Actonel

(Other name for: risedronate sodium)

Actos

(Other name for: pioglitazone hydrochloride)

acyclovir

A synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV.

acyclovir sodium

The sodium salt form of acyclovir, a synthetic analog of the purine nucleoside, guanosine, with potent antiviral activity against herpes simplex viruses type 1 and 2, varicella-zoster virus and other viruses. After conversion in vivo to the active metabolite acyclovir triphosphate, acyclovir competitively inhibits viral DNA polymerase, incorporates into and terminates the growing viral DNA chain, and inactivates viral DNA polymerase. The greater antiviral activity of acyclovir against HSV compared to VZV is due to its more efficient phosphorylation by the thymidine kinase of HSV.

Aczone Gel

(Other name for: dapsone gel, 5%)

Ad-hCMV-Flt3L

A human serotype 5, replication-defective, first generation adenoviral vector, with the viral E1a and E3 protein encoding regions deleted, which is engineered to express the soluble, immune-mediated stimulatory gene human fms-like tyrosine kinase 3 ligand (Flt3L), under the transcriptional control of the CMV promoter, with potential immunostimulating activity. Upon administration, Ad-hCMV-Flt3L is transduced into tumor cells and Flt3L is expressed. Flt3L stimulates both the proliferation of dendritic cells (DCs) and their migration to the tumor site. Upon exposure to the tumor-associated antigens (TAA) released from dying glioma cells, which were killed by thymidine kinase-mediated valacyclovir-induced tumor cell death, the DCs initiate a specific immune response against any remaining TAA-expressing tumor cells. Flt3L is a hematopoietic growth factor and ligand for the Flt3 tyrosine kinase receptor.

Ad-hCMV-TK

A human serotype 5, replication-defective, first generation adenoviral vector, with the viral E1a and E3 protein encoding regions deleted, which is engineered to express the herpes simplex virus thymidine kinase (HSV-tk) gene under the transcriptional control of the CMV promoter. This agent, when administered in conjunction with a synthetic acyclic guanosine analogue, possesses potential antineoplastic activity. Upon administration into the peritumoral region after tumor resection, adenoviral vector encoding HSV thymidine kinase is transduced into tumor cells, and HSV-tk is expressed. Tumor cells expressing HSV-tk are sensitive to synthetic acyclic guanosine analogues. Subsequent administration of a synthetic acyclic guanosine analogue, such as valacyclovir (VCV) or ganciclovir (GCV), kills the tumor cells expressing HSV-tk. The release of tumor-associated antigens (TAA) by dying tumor cells may then stimulate an antitumor cytotoxic T lymphocyte (CTL) response, directed aganst any remaining tumor cells.

Ad-REIC/DKK3 vaccine

A replication incompetent adenoviral vector encoding the full-length tumor suppressor gene Reduced Expression in Immortalized Cells (REIC or DKK3) (ad-REIC/DKK3), with potential antineoplastic activity. Upon intratumoral injection, tumor cells express REIC/DKK3 protein. This may result in the activation of c-Jun-NH2-kinase (JNK) and ultimately apoptosis via Bcl2 suppression and caspase-3 activation. Expression of REIC/DKK3 is normal in healthy cells but reduced or absent in many cancer cells; Forced overexpression of REIC/DKK3 in cancer cells may lead to an induction of tumor cell apoptosis and reduction of tumor cell growth while sparing normal, healthy cells naturally expressing endogenous REIC/DKK3.

Ad-sig-hMUC-1/ecdCD40L vaccine

A cancer vaccine consisting of a recombinant adenoviral vector encoding the tumor-associated antigen (TAA) human MUC-1 (hMUC-1) linked to the extracellular domain (ecd) of the co-stimulatory molecule CD40 ligand (CD40L) and an adenovirus signal sequence that encodes a secretory signal peptide (Ad-sig) with potential immunostimulating and antineoplastic activities. Due to the presence of the secretory signal peptide expressed by Ad-sig in the vaccine construct, transfected cells may secrete a fusion protein composed of hMUC-1 and the CD40L ecd. The CD40L moiety part of the fusion protein binds to CD40 receptors on dendritic cells (DCs). Subsequently, DCs may be activated and migrate, T-cells may expand, and a cytotoxic T lymphocyte (CTL) response against tumor cells that overexpress hMUC-1 may follow. MUC-1 is a hypoglycosylated TAA overexpressed by epithelial cancer cells.

Ad5-CMV-NIS

A recombinant type 5 adenovirus (Ad5), encoding the gene for the human sodium-iodide symporter (NIS) linked to the cytomegalovirus (CMV) promoter, with potential gene transfection activity. Upon intratumoral injection, Ad5-CMV-NIS is taken up by tumor cells, resulting in the cellular expression of NIS. Subsequently, orally administered iodine 131 is taken up by NIS-expressing tumor cells, which may result in the selective accumulation of a cytotoxic dose of beta and gamma radiation in non-thyroidal tumor cells, sparing adjacent normal tissue. NIS, an intrinsic membrane glycoprotein, is an ion pump that actively transports iodide into cells which concentrate iodine; in addition to thyroid epithelial cells, it is found in non-thyroidal tissues including the salivary glands, the gastric mucosa, and lactating mammary glands.

Ad5-yCD/mutTK(SR39)rep-ADP

A second generation, replication-competent adenovirus type 5 containing a yeast cytosine deaminase(yCD)/mutant sr39 herpes simplex virus thymidine kinase fusion (yCD/mutTKsr39) gene and the 11.6 kDa adenovirus death protein (ADP) gene with potential oncolytic activity. Upon intratumoral administration and transduction of Ad5-yCD/mutTK(SR39)rep-ADP into tumor cells and subsequent expression of cytosine deaminase and viral thymidine kinase, administered prodrugs 5-fluorocytosine (5-FC) and ganciclovir are converted into their respective metabolites 5-fluorouracil (5-FU) and ganciclovir-5-monophosphate (ganciclovir-MP); 5-FU is subsequently metabolized to cytotoxic active metabolites 5-fluoroxyuridine monophosphate (F-UMP) and 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP); ganciclovir-TP subsequently is converted by mammalian thymidine kinase to cytotoxic ganciclovir-triphosphate (ganciclovir -TP). Tumor cells adjacent to tumor cells transduced with this agent may be killed through a "bystander effect". ADP may enhance spread and oncolytic activity of replication-competent adenoviruses. In addition to its oncolytic activity, Ad5-yCD/mutTK(SR39)rep-ADP may exhibit radiosensitizing activity.

Ad5.SSTR/TK.RGD

An RGD-4Cmodified, infectivity-enhanced, bicistronic type 5 adenovirus expressing herpes simplex virus thymidine kinase (HSV-tk) gene, a therapeutic suicide gene, and the somatostatin receptor type 2 (SSTR2) gene with potential antineoplastic activity. Modification with the double cyclic peptide RGD-4C allows the virus to bind to cellular integrins, frequently expressed on the surfaces of ovarian cancer cells, instead of the coxsackie and adenovirus (CAR) receptor, which is often nonfunctional in ovarian cancer cells. Upon intratumoral administration, Ad5.SSTR/TK.RGD transfects tumor cells and expresses the HSV-tk gene. After subsequent administration of a synthetic acyclic guanosine analogue prodrug like ganciclovir (GCV), expressed HSV-tk phosphorylates and activates the prodrug, which may result in inhibition of DNA synthesis and apoptosis in HSV-tk-expressing cancer cells. Additionally, as a bystander effect, adjacent non-transfected cells may be killed by the activated antiviral drug. SSTR2 expression allows imaging of gene transfer into tumor cells using a radiolabeled somatostatin analogue.

Ad5CMV-p53 gene

A replication-defective adenoviral-CMV vector that encodes a wild-type p53 gene. Ad5CMV-p53 induces tumor cells that have been transfected with the vector to produce wild-type p53, a tumor suppressor gene that is deleted or mutated in a significant number of cancers. In transfected tumor cells, the wild-type p-53 gene product exerts an antitumor effect by blocking cell cycle progression at the G1/S regulation point, activating DNA repair proteins in the presence of DNA damage, and initiating apoptosis when DNA damage is irreparable.

Ad5F35-LMP1/LMP2-transduced autologous dendritic cells

Autologous dendritic cells (DCs) transduced with the replication-deficient adenoviral vector Ad5F53 encoding the Epstein-Barr virus (EBV) transmembrane latent membrane proteins 1 and 2 (LMP1/LMP2) with potential immunostimulatory activity. Vaccination with Ad5F35-LMP1/LMP2-transduced autologous dendritic cells may stimulate a specific cytotoxic T-lymphocyte (CTL) response against LMP1- and LMP2-expressing tumor positive cells, resulting in tumor cell lysis and inhibition of tumor cell proliferation. LMP1 and LMP2 are expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin disease.

Adanon

(Other name for: methadone hydrochloride)

Adapin

(Other name for: doxepin hydrochloride)

Adcetris

(Other name for: brentuximab vedotin)

Adderall

(Other name for: dextroamphetamine-amphetamine)

Adderall XR

(Other name for: dextroamphetamine-amphetamine)

ADE regimen

An induction chemotherapy regimen consisting of cytarabine (Ara-C), daunorubicin and etoposide used for the treatment of childhood acute myeloid leukemia. (NCI Thesaurus)

adecatumumab

A recombinant human IgG1 monoclonal antibody (MoAb) directed against the tumor associated antigen (TAA) epithelial cell adhesion molecule (EpCAM) with potential antitumor activity. Adecatumumab binds to EpCAM, which may result in antibody-dependent cellular cytotoxicity (ADCC) directed against EpCAM-expressing tumor cells. EpCAM (CD326), a cell surface protein upregulated on many tumor cell types, promotes the proliferation, migration and invasiveness of tumor cells; for some cancers, overexpression has been correlated with decreased survival.

adefovir dipivoxil

An acyclic nucleotide adenine analogue with potent antiviral activity. Adefovir is activated in vivo to a diphosphate metabolite which is incorporated into viral DNA, leading to viral RNA-dependent DNA polymerase inhibition, DNA chain termination and impairment of viral replication. This agent inhibits the reverse transcriptases of hepatitis B, herpes and HIV viruses, induces natural killer cell activity, and stimulates endogenous interferon production. Viral resistance to adefovir develops at a slower rate compared to other antivirals.

adenosine A3 receptor agonist CF102

An orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity. Adenosine A3 receptor agonist CF102 selectively binds to and activates the cell surface-expressed A3AR, deregulating Wnt and NF-kB signal transduction pathways downstream, which may result in apoptosis of A3AR-expressing tumor cells. A3AR, a G protein-coupled receptor, is highly expressed on the cell surfaces of various solid tumor cell types, including hepatocellular carcinoma (HCC) cells, and plays an important role in cellular proliferation.

adenovector encoding MDA7

A nonreplicating adenoviral vector (adenovector) encoding the melanoma differentiation-associated 7 gene (MDA7) with potential antineoplastic activity. After intratumoral injection and adenovector-mediated gene transfer of MDA7 into tumor cells, the expressed MDA7 transgene may inhibit tumor cell proliferation and induce tumor cell apoptosis.

adenovector-transduced AP1903-inducible MyD88/CD40-expressing autologous PSMA-specific prostate cancer vaccine BPX-201

A genetically-modified, dendritic cell (DC)-based vaccine in which the autologous cells are transduced with an adenoviral vector expressing the tumor antigen prostate-specific membrane antigen (PSMA) and a fusion protein composed of synthetic ligand inducible adjuvant iMC composed of a drug-inducible costimulatory CD40 receptor (iCD40) and the adaptor protein MyD88, with potential immunomodulating and antineoplastic activities. The iCD40 contains a membrane-localized cytoplasmic CD40 domain fused to the FK506 modified drug-binding protein 12 (FKBP12). Upon intradermal administration of BPX-201, these DCs accumulate in local draining lymph nodes. Twenty-four hours after vaccination, the dimerizing agent AP1903 is administered. AP1903 binds to the drug binding domain, leading to iMC oligomerization and activation of iCD40 and MyD88-mediated signaling in iMC-expressing DCs. This signaling pathway activates the DCs and stimulates a cytotoxic T-lymphocyte (CTL) response against host tumor cells that express PSMA. PSMA, a glycoprotein secreted by prostatic epithelial and ductal cells, is overexpressed in prostate cancer cells and is used as a tumor marker for both diagnosis and treatment evaluation. MyD88 is involved in interleukin 1 receptor (IL1R) and toll-like receptor (TLR) signaling.

adenovector-transduced AP1903-inducible MyD88/CD40-expressing autologous PSMA-specific prostate cancer vaccine BPX-201

A genetically-modified, dendritic cell (DC)-based vaccine in which the autologous cells are transduced with an adenoviral vector expressing the tumor antigen prostate-specific membrane antigen (PSMA) and a fusion protein composed of synthetic ligand inducible adjuvant iMC composed of a drug-inducible costimulatory CD40 receptor (iCD40) and the adaptor protein MyD88, with potential immunomodulating and antineoplastic activities. The iCD40 contains a membrane-localized cytoplasmic CD40 domain fused to the FK506 modified drug-binding protein 12 (FKBP12). Upon intradermal administration of BPX-201, these DCs accumulate in local draining lymph nodes. Twenty-four hours after vaccination, the dimerizing agent AP1903 is administered. AP1903 binds to the drug binding domain, leading to iMC oligomerization and activation of iCD40 and MyD88-mediated signaling in iMC-expressing DCs. This signaling pathway activates the DCs and stimulates a cytotoxic T-lymphocyte (CTL) response against host tumor cells that express PSMA. PSMA, a glycoprotein secreted by prostatic epithelial and ductal cells, is overexpressed in prostate cancer cells and is used as a tumor marker for both diagnosis and treatment evaluation. MyD88 is involved in interleukin 1 receptor (IL1R) and toll-like receptor (TLR) signaling.

adenovector-transduced AP1903-inducible MyD88/CD40-expressing autologous PSMA-specific prostate cancer vaccine BPX-201

A genetically-modified, dendritic cell (DC)-based vaccine in which the autologous cells are transduced with an adenoviral vector expressing the tumor antigen prostate-specific membrane antigen (PSMA) and a fusion protein composed of synthetic ligand inducible adjuvant iMC composed of a drug-inducible costimulatory CD40 receptor (iCD40) and the adaptor protein MyD88, with potential immunomodulating and antineoplastic activities. The iCD40 contains a membrane-localized cytoplasmic CD40 domain fused to the FK506 modified drug-binding protein 12 (FKBP12). Upon intradermal administration of BPX-201, these DCs accumulate in local draining lymph nodes. Twenty-four hours after vaccination, the dimerizing agent AP1903 is administered. AP1903 binds to the drug binding domain, leading to iMC oligomerization and activation of iCD40 and MyD88-mediated signaling in iMC-expressing DCs. This signaling pathway activates the DCs and stimulates a cytotoxic T-lymphocyte (CTL) response against host tumor cells that express PSMA. PSMA, a glycoprotein secreted by prostatic epithelial and ductal cells, is overexpressed in prostate cancer cells and is used as a tumor marker for both diagnosis and treatment evaluation. MyD88 is involved in interleukin 1 receptor (IL1R) and toll-like receptor (TLR) signaling.

adenoviral vector Ad5-CEA(6D) vaccine

A replication-defective, E1- and E2b-deleted oncolytic adenoviral serotype 5 (Ad5) encoding an epitope of human carcinoembryonic antigen (CEA) with potential antineoplastic activity. Adenoviral vector Ad5-CEA(6D) vaccine expresses a highly immunogenic analogue of CEA [CAP1-(6D)]. Upon administration, this vaccine may induce both humoral and cellular immune responses against tumor cells expressing the CEA antigen, thereby resulting in the immune-mediated inhibition of tumor cell proliferation and tumor cell death. CEA, a tumor-associated antigen, is overexpressed in various tumor cell types. Deletion of early genes E1 and E2b in Ad5 potentially circumvents pre-existing anti-adenovirus immunity and is capable of inducing strong immune responses.

adenoviral vector encoding HSV thymidine kinase

An adenoviral vector engineered to express the herpes simplex virus thymidine kinase (HSV-tk) gene, which, when administered in conjunction with a synthetic acyclic guanosine analogue, possesses potential antineoplastic activity. Adenoviral vector encoding HSV thymidine kinase is transduced into tumor cells, sensitizing tumor cells that overexpress HSV-tk to synthetic acyclic guanosine analogues. Subsequently, a low dose of a synthetic acyclic guanosine analogue such as valacyclovir (VCV) or ganciclovir (GCV) is given, which may preferentially kill tumor cells containing the adenoviral vector and overexpressing HSV-tk. Release of tumor-associated antigens (TAAs) by dying tumor cells may then stimulate an antitumor cytotoxic T lymphocyte (CTL) response.

adenoviral-transduced hIL-12-expressing autologous dendritic cells INXN-3001 plus activator ligand INXN-1001

Autologous dendritic cells tranduced with a replication incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-3001) in combination with the proprietary orally bioavailable, small molecule activator ligand INXN-1001, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer INXN-1001. Upon intratumoral injection of INXN-3001 and subsequent oral administration of activator ligand, INXN-1001 is able to induce expression of IL-12 in INXN-3001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells, inducing the secretion of interferon-gamma and inducing a cytotoxic T lymphocyte response against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. As INXN-1001 regulates both the timing and the levels of IL-12 expression, IL-12 toxicity can be reduced.

adenoviral-transduced hIL-12-expressing autologous dendritic cells INXN-3001 plus activator ligand INXN-1001

Autologous dendritic cells tranduced with a replication incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-3001) in combination with the proprietary orally bioavailable, small molecule activator ligand INXN-1001, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer INXN-1001. Upon intratumoral injection of INXN-3001 and subsequent oral administration of activator ligand, INXN-1001 is able to induce expression of IL-12 in INXN-3001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells, inducing the secretion of interferon-gamma and inducing a cytotoxic T lymphocyte response against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. As INXN-1001 regulates both the timing and the levels of IL-12 expression, IL-12 toxicity can be reduced.

adenoviral-transduced hIL-12-expressing autologous dendritic cells INXN-3001 plus activator ligand INXN-1001

Autologous dendritic cells tranduced with a replication incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-3001) in combination with the proprietary orally bioavailable, small molecule activator ligand INXN-1001, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer INXN-1001. Upon intratumoral injection of INXN-3001 and subsequent oral administration of activator ligand, INXN-1001 is able to induce expression of IL-12 in INXN-3001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells, inducing the secretion of interferon-gamma and inducing a cytotoxic T lymphocyte response against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation. As INXN-1001 regulates both the timing and the levels of IL-12 expression, IL-12 toxicity can be reduced.

adenovirus B7-1

A gene-viral vector complex comprised of an adenovirus vector and B7-1 gene targeting the CD80 antigen. Adenovirus B7-1 is used as a component in antineoplastic vaccines to elicit a cytotoxic T-cell response.

adenovirus encoding E.coli PNP

A replication-incompetent adenovirus encoding E. coli purine nucleoside phosphorylase (Ad/PNP) used as a prodrug activating agent. Administered intratumorally, Ad/PNP expresses the enzyme PNP, which may catalyze systematically administrated fludarabine phosphate prodrug into its active form 2-fluoroadenine (F-Ade). F-Ade inhibits DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth. Localized prodrug activation provides targeted chemotherapy, thereby potentially reducing systemic side effects.

adenovirus encoding human aquaporin-1

A replication-deficient, recombinant adenovirus encoding human aquaporin-1 with potential membrane water channel activity. Upon transfection of salivary glands, adenovirus encoding human aquaporin-1 (AdhAQP1) directs human aquaporin-1 (hAQP1) expression in the apical and basolateral plasma membranes of salivary secretory cells, which may result in increased saliva production. hAQP1, a water channel protein, is one of several highly conserved water channel proteins that mediate water permeability in cells of water-transporting tissues.

adenovirus encoding rat Her-2/neu

A replication-defective oncolytic adenovirus, encoding rat Her-2/neu (ErbB-2), with potential antineoplastic activity. Upon administration, adenovirus encoding rat HER-2/neu may induce an immune response against tumor cells expressing the HER-2/neu antigen, which may result in the immune-mediated inhibition of tumor cell proliferation and tumor cell death. Her-2/neu, a tumor-associated antigen and member of the epidermal growth factor receptor (EGFR) family of tyrosine kinases, is overexpressed in various tumor cell types.

adenovirus encoding recombinant human endostatin

A replication-defective, recombinant oncolytic adenovirus encoding human endostatin with potential antineoplastic activity. Endostatin, a 20 kDa C-terminal proteolytic fragment of collagen XVIII, is an important angiogenesis inhibitor. Upon intratumoral administration, the adenovirus infects and replicates in tumor cells. The expressed endostatin may inhibit endothelial cell proliferation and angiogenesis which may result in a reduction of tumor growth.

adenovirus encoding tyrosinase, MART-1/MAGE-A6-transduced autologous dendritic cell vaccine

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) transduced with a recombinant adenoviral vector encoding three full-length human melanoma associated antigens (MAAs), tyrosinase, melan-A (MART-1) and the melanoma antigen A6 (MAGEA6), with potential antineoplastic activity. Upon intradermal administration, adenovirus encoding tyrosinase/MART-1/MAGEA6-transduced autologous DC vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against tyrosinase/MART-1/MAGEA6-positive tumor cells, which may result in tumor cell death and decreased tumor growth. Tyrosinase, a melanoma-specific differentiation antigen, catalyzes the first step of melanin synthesis in melanocytes. Vaccination with multi-antigen modified DC may improve the efficacy of the DC immunotherapy.

adenovirus HER2-transduced autologous dendritic cell vaccine

A cell-based cancer vaccine composed of autologous dendritic cells (DCs) transduced with a replication-deficient adenovirus vector encoding HER-2 with potential antineoplastic activity. Upon administration, adenovirus HER2-transduced autologous dendritic cell vaccine may stimulate a cytotoxic T lymphocyte (CTL) response against HER-2-positive tumor cells, which may result in tumor cell death and decreased tumor growth.HER-2, a tyrosine kinase receptor for epidermal growth factor (EGF) (also known as neu and ErbB2), is overexpressed by some breast, ovarian, and gastric cancers.

adenovirus vector

One of a number of genetically-engineered adenoviruses designed to insert a gene of interest into a eukaryotic cell where the gene of interest is subsequently expressed. Unlike most other vectors, adenovirus vectors have the ability to infect post-mitotic cells. Thus, these agents are especially useful for gene transfer into neuronal cells.

adenovirus-interferon-gamma TG1042

A replication-defective adenoviral vector encoding human interferon-gamma (IFN-g) cDNA with potential antineoplastic and immunoregulatory activities. Upon intratumoral administration, the prolonged expression of IFN-g by adenovirus-interferon-gamma TG1042 promotes a T helper type 1 (Th1-type) immune response and inhibits the Th2-mediated cytokine production observed in many cutaneous lymphomas. IFN-g also mediates interleukin-12 (IL-12) production by antigen-presenting cells (APCs); activates macrophages, cytotoxic T-cells, and natural killer (NK) cells; upregulates major histocompatibility complex (MHC) molecules; and stimulates antibody-dependent cellular cytotoxicity (ADCC). Altogether, these IFN-g-mediated effects may result in an inhibition of tumor cell proliferation and tumor cell death.

adenovirus-mediated human interleukin-12

A replication-incompetent adenovirus encoding human pro-inflammatory cytokine interleukin-12 (IL-12) (Ad.hIL-12), with potential immunomodulating and antineoplastic activities. Upon intratumoral administration, the adenovirus selectively infects and replicates in tumor cells, which may result in tumor cell lysis. Synergistically, IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells (NKs), inducing secretion of interferon-gamma and inducing cytotoxic T cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation.

adenovirus-mediated human interleukin-12 INXN-2001 plus activator ligand INXN-1001

A replication incompetent adenovirus encoding the human pro-inflammatory cytokine interleukin-12 (IL-12) (INXN-2001) in combination with the proprietary activator ligand INXN-1001, with potential immunomodulating and antineoplastic activities. Production of IL-12 is controlled by an inducible DNA element that allows transcription initiation only in the presence of the ligand inducer. Upon intratumoral administration of INXN-2001 and oral administration of INXN-1001, INXN-1001 is able to induce expression of IL-12 from INXN-2001. IL-12 expressed by the adenovirus may activate the immune system by promoting the activation of natural killer cells (NKs), inducing secretion of interferon-gamma and inducing cytotoxic T cell responses against tumor cells, which may result in immune-mediated tumor cell death and inhibition of tumor cell proliferation.

adenovirus-p53 transduced dendritic cell vaccine

A cancer vaccine consisting of autologous dendritic cells (DCs) transduced with a recombinant adenovirus encoding p53 peptide, with potential immunomodulating activity. Intradermal vaccination with adenoviral-p53 transduced dendritic cell vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells expressing mutant p53, resulting in tumor cell lysis. p53, a tumor suppressor gene, is mutated in many tumor cells, resulting in the loss of apoptosis regulation and abnormal cell proliferation.

adenovirus-PSA prostate cancer vaccine

A cancer vaccine composed of a genetically engineered, replication-deficient type 5 adenovirus carrying the human prostate-specific antigen (PSA), with potential immunostimulating and antineoplastic activities. Upon subcutaneous vaccination with the adenovirus-PSA prostate cancer vaccine, the adenovirus infects cells and expresses PSA. In turn, PSA may activate the immune system and may induce a cytotoxic T-lymphocyte response against PSA-expressing tumor cells. PSA, a tumor associated antigen, is expressed by prostate epithelial cells and is overexpressed in prostate cancer.

adenovirus/cytomegalovirus/Epstein-Barr virus-specific allogeneic cytotoxic T lymphocytes

Allogeneic tri-viral specific, adenovirus, cytomegalovirus and Epstein-Barr virus (Adv, CMV and EBV or ACE), cytotoxic T-lymphocytes (CTLs) with potential antiviral activity. Donor-derived T-cells were exposed to dendritic cells nucelofected with DNA plasmids encoding Hexon and Penton (Adv), pp65 and IE1 (CMV), and LMP2, EBNA1 and BZLF1 (EBV), all are critical proteins for the proliferation of these viruses, and subsequently maintained in the presence of interleukins 4 and 7 with a novel culture device to expand and sustain the repertoire of CTLs. After an allogeneic hematopoietic stem cell transplant (HSCT), infusion of these CTLs primed towards Adv, CMV and EBV may prevent viral infection by these pathogens.

AdGMCAIX-transduced autologous dendritic cells

Autologous dendritic cells (DCs) transduced with a recombinant, replication-defective adenoviral vector expressing the fusion gene granulocyte-macrophage colony-stimulating factor (GM-CSF) and carbonic anhydrase IX (CA-IX or CA9) (GMCA-9), with potential immunomodulating activity. The autologous DCs are transduced ex vivo and express the GMCA-9 fusion protein on the cell surface. Upon intradermal administration of the AdGMCAIX-transduced autologous DCs back into the patient, the DCs activate the immune system to both mount a cytotoxic T lymphocyte-mediated response against tumor cells positive for the CA9 antigen, and generate memory T cells. This may result in decreased tumor growth. CA9, also known as G250, is a renal cell carcinoma (RCC)-associated antigen and a member of the carbonic anhydrase family that contains a human leukocyte antigen (HLA)-A2.1-restricted epitope; it is found in a majority of renal cell carcinomas while absent in most normal tissues. The cytokine GM-CSF enhances the immunogenicity of CA9-based DC vaccines.

ADH-1

A small, cyclic pentapeptide vascular-targeting agent with potential antineoplastic and antiangiogenic activities. ADH-1 selectively and competitively binds to and blocks N-cadherin, which may result in disruption of tumor vasculature, inhibition of tumor cell growth, and the induction of tumor cell and endothelial cell apoptosis. N-cadherin, a cell- surface transmembrane glycoprotein of the cadherin superfamily of proteins involved in calcium-mediated cell-cell adhesion and signaling mechanisms; may be upregulated in some aggressive tumors and the endothelial cells and pericytes of some tumor blood vessels.

adipose-derived regenerative cells

A population of cells derived from adipose tissue with stem cell and wound repair activities. Adipose-derived regenerative cells (ADRC) consists of several cell types, such as adult stem cells, vascular endothelial cells, and vascular smooth muscle cells, among others. These cells contribute to wound repair through a variety of mechanisms by promoting blood vessel growth and blocking apoptosis. In addition, ADRC can differentiate into several tissue types, such as bone, cartilage, fat, skeletal muscle, smooth muscle and cardiac muscle.

ado-trastuzumab emtansine

An antibody-drug conjugate (ADC) consisting of the recombinant anti-epidermal growth factor receptor 2 (HER2) monoclonal antibody trastuzumab conjugated to the maytansinoid DM1 via a nonreducible thioether linkage (MCC) with potential antineoplastic activity. The trastuzumab moiety of this ADC binds to HER2 on tumor cell surface surfaces; upon internalization, the DM1 moiety is released and binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that overexpress HER2. Linkage of antibody and drug through a nonreducible linker has been reported to contribute to the improved efficacy and reduced toxicity of this ADC compared to similar ADCs constructed with reducible linkers.

adozelesin

An alkylating agent that bind to the DNA minor groove in a sequence-specific manner and form covalent adducts with adenines, resulting in the inhibition of DNA replication and induction of apoptosis.

adrenocorticotropic hormone

A hormone secreted by the anterior portion of the pituitary gland and regulates hormone, primarily cortisol, secreted by the adrenal gland.

Adriamycin PFS

(Other name for: doxorubicin hydrochloride)

Adriamycin RDF

(Other name for: doxorubicin hydrochloride)

AdRTVP-1-transduced prostate cancer cell-based vaccine

A cell-based vaccine comprised of prostate cancer cells transduced with an adenoviral vector encoding human RTVP-1 (AdRTVP-1), with potential immunostimulating and antineoplastic activities. RTVP-1, also referred to as glioma pathogenesis-related protein 1 (GLIP1), is down-regulated in prostate tumors. Regulated by tumor suppressor p53, the expression of RTVP-1 functions as a tumor suppressor, and is abundant in normal human prostate epithelial cells as well as in differentiated macrophages. Administration of AdRTVP-1-transduced prostate cancer cell-based vaccine leads to an induction of apoptosis through the expression of RTVP-1, which may result in a reduction in prostate cancer cellular proliferation. In addition, this vaccine may induce a cytotoxic T lymphocyte (CTL) response against prostate specific tumor- associated antigens.

Adrucil

(Other name for: fluorouracil)

ADVEXIN

(Other name for: Ad5CMV-p53 gene)

AE37 peptide/GM-CSF vaccine

A vaccine containing HER2/Neu-derived epitope (amino acids 776-790) linked to li-Key peptide (li-Key/HER2/neu hybrid peptide or AE37), and combined with granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential antineoplastic and immunoadjuvant activities. Upon vaccination, AE37 may activate the immune system and stimulate T-helper cells against HER2/Neu expressing cancer cells. GM-CSF may potentiate the immune response against cancer cells expressing the HER2/Neu antigen. The Ii-Key moiety, a 4-amino acid (LRMK) epitope from the MHC class II-associated invariant chain (Ii protein), increases T-helper cell stimulation against HER2/neu antigen when compared to unmodified class II epitopes. HER2/neu, a tumor associated antigen (TAA), is overexpressed in a variety of tumor cell types and is highly immunogenic.

AEE788

An orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis.

AEG35156

A second-generation synthetic antisense oligonucleotide with potential antineoplastic activity. AEG35156 selectively blocks the cellular expression of X-linked inhibitor of apoptosis protein (XIAP), a pivotal inhibitor of apoptosis that is overexpressed in many tumors. This agent reduces total levels of XIAP in tumor cells, working synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. XIAP interferes with both the intrinsic and extrinsic program-death signaling pathways, which may render tumor cells resistant to apoptosis.

Aeroseb-Dex

(Other name for: dexamethasone)

Aeroseb-HC

(Other name for: therapeutic hydrocortisone)

aerosol sargramostim

An aerosol inhalation formulation containing a yeast-derived glycosylated recombinant form of human granulocyte macrophage colony stimulating factor (GM-CSF) with potential immunostimulating activity. Sargramostim binds to specific cell surface receptors, modulating the proliferation and differentiation of a variety of hematopoietic progenitor cells with some specificity towards stimulation of leukocyte production. This agent also activates neutrophils, monocytes, macrophages, and dendritic cells and promotes antigen presentation, upregulates antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated, lymphokine-activated killer cell function. Aerosol inhalation may help achieve high concentrations of sargramostim in the lung.

aerosolized aldesleukin

An aerosol formulation of aldesleukin, a recombinant form of interleukin-2 (IL-2), with potential immunostimulating activity. Upon IL-2 inhalation, this cytokine activates lymphokine-activated killer cells and natural killer cells, and induces expression of cytotoxic cytokines, such as interferon-gamma and transforming growth factor-beta. This may eventually halt tumor cell growth. Localized administration of IL-2 may decrease toxicity and increase efficacy.

aerosolized liposomal rubitecan

An aerosolized liposomal preparation of a water-insoluble derivative of camptothecin with potential antineoplastic activity. 9-nitro-20 (S)-camptothecin and its active metabolite 9-aminocamptothecin (9-AC) selectively stabilize topoisomerase I-DNA covalent complexes during S-phase, thereby inhibiting religation of topoisomerase I-mediated single-strand DNA breaks and producing potentially lethal double-strand DNA breaks when encountered by the DNA replication machinery. This agent is formulated with dilauroylphosphatidylcholine and nebulized in particle sizes of 1.2-1.6 micrometer mass median aerodynamic diameter.

afamelanotide

A synthetic peptide analogue of the naturally occurring alpha-melanocyte stimulating hormone (a-MSH) with potential photoprotective activity. Mimicking the action of a-MSH, afamelanotide stimulates melanocytes to increase the production and release of melanin. Increased melanocyte melanin may protect against ultraviolet radiation (UVR)-initiated cellular DNA damage, oxidation of membrane proteins, and alterations in intracellular signaling processes in epidermal cells. Endogenously, a-MSH is released by skin cells in response to UVR exposure, stimulating melanocytes to produce and release melanin.

afatinib dimaleate

The dimaleate salt form of afatinib, an orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types.

Affinitac

(Other name for: ISIS 3521)

Affinitak

(Other name for: ISIS 3521)

afimoxifene

A tamoxifen metabolite with both estrogenic and anti-estrogenic effects. Afimoxifene has a higher affinity for the estrogen receptor than tamoxifen, and functions as an antagonist in breast cancer cells.

Afinitor

(Other name for: everolimus)

Afinitor Disperz

(Other name for: everolimus tablets for oral suspension)

Aflodac

(Other name for: sulindac)

AFP gene hepatocellular carcinoma vaccine

A cancer vaccine composed of naked plasmid DNA of the gene for the tumor-associated antigen alpha-fetoprotein (AFP), a macromolecule that acts as a specific immunologic target for hepatocellular carcinoma. This agent exerts an antitumor effect by inducing cytotoxic T-lymphocytes to attack AFP-expressing tumor cells.

AFP464

A synthetic lysyl prodrug of the amino-substituted flavone derivate aminoflavone with antiproliferative and antineoplastic activities. AFP464 is rapidly converted to aminoflavone in plasma. Aminoflavone activates the aryl hydrocarbon receptor (AhR) signaling pathway leading to an increase in cytochrome P450 1A1 (CYP1A1) and cytochrome P450 1A2 (CYP1A2) expression and, to a lesser extent, an increase in cytochrome P450 1B1 (CYP1B1) expression. Subsequently, aminoflavone is metabolized to toxic metabolites by the cytochromome P450 enzymes that it induces; these toxic metabolites covalently bind to DNA, resulting in the phosphorylation of p53, the induction of the p53 downstream target p21Waf1/Cip1, and apoptosis. Pulmonary toxicity may be dose-limiting.

afuresertib

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Afuresertib binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

AG-024322

A cyclin-dependent kinase (CDK) inhibitor with antineoplastic activity. AG-024322 selectively inhibits cyclin-dependent kinases (particularly CDK1,2 and 4), enzymes that regulate cell cycle progression. Inhibition of CDK may result in cell cycle arrest, induction of apoptosis, and inhibition of DNA replication and tumor cell proliferation.

Agaricus blazei Murill extract

A dietary supplement containing an extract of the Basidiomycete fungus Agaricus blazei Murill with potential chemopreventive, antineoplastic and immunopotentiating activities. Agaricus blazei Murill extract contains high levels of phytochemicals, especially beta-D-glucans. Beta-D-glucans may promote dendritic cell (DC) maturation; increase interferon gamma (IFN-gamma), tumor necrosis factor alpha (TNF-alpha) and immunoglobulin levels; and may enhance natural killer (NK) cell activity, potentially boosting anti-tumor host immune responses.

agatolimod sodium

The tricosasodium salt of a synthetic 24-mer oligonucleotide containing 3 CpG motifs with potential antineoplastic and immunostimulatory activity. Agatolimod selectively targets Toll-like receptor 9 (TLR9), thereby activating dendritic and B cells and stimulating cytotoxic T cell and antibody responses against tumor cells bearing tumor antigens.

AIM2(-1)/HT001(-1)/TAF1B(-1) frameshift peptide vaccine

A cancer vaccine containing the three frame shift peptides (FSP) AIM2(-1), HT001(-1) and TAF1B(-1), with potential immunomodulating activity. Upon administration, the AIM2(-1)/HT001(-1)/TAF1B(-1) FSP vaccine may induce an immune response against microsatellite instability (MSI) colorectal cancer-associated antigens. Frame shift mutations of AIM2 (absent in melanoma 2, an interferon-inducible protein), HT001 (asteroid homolog 1 or ASTE1, with an unknown function) and TAF1B (TATA box-binding protein-associated RNA polymerase I B, a transcription factor) are seen in MSI-positive colorectal cancers and may be associated with malignant transformation, tumor progression and the presence of tumor-infiltrating lymphocytes. These FSPs all have one-base deletions.

AK 3012

A proprietary topical formulation. Upon subcutaneous administration, the active ingredient in AK 3012 may inhibit actinic keratosis.

Aknoten

(Other name for: tretinoin)

Akt antisense oligonucleotide RX-0201

A 20-mer antisense oligodeoxynucleotide (ODN) against the proto-oncogene Akt with potential antineoplastic activity. Akt-1 antisense oligonucleotide RX-0201 binds to Akt-1 mRNA, inhibiting translation of the transcript; suppression of Akt-1 expression may result in the inhibition of cellular proliferation and the induction of apoptosis in tumor cells that overexpress Akt-1. Akt-1 is a serine-threonine protein kinase that stimulates proliferation and inhibits apoptosis of tumor cells.

AKT inhibitor ARQ 092

An orally bioavailable inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. The AKT signaling pathway is often deregulated in cancer and is associated with tumor cell proliferation, survival and migration.

Akt inhibitor AZD5363

A novel pyrrolopyrimidine derivative, and an orally available inhibitor of the serine/threonine protein kinase AKT (protein kinase B) with potential antineoplastic activity. AKT inhibitor AZD5363 binds to and inhibits all AKT isoforms. Inhibition of AKT prevents the phosphorylation of AKT substrates that mediate cellular processes, such as cell division, apoptosis, and glucose and fatty acid metabolism. A wide range of solid and hematological malignancies show dysregulated PI3K/AKT/mTOR signaling due to mutations in multiple signaling components. By targeting AKT, the key node in the PIK3/AKT signaling network, this agent may be used as monotherapy or combination therapy for a variety of human cancers.

Akt inhibitor GDC-0068

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GDC-0068 binds to and inhibits the activity of Akt in a non-ATP-competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Akt inhibitor GSK2141795

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor GSK2141795 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Akt inhibitor LY2780301

An orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor LY2780301 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway, thereby leading to inhibition of cell proliferation and the induction of apoptosis in tumor cells. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Akt inhibitor MK2206

An orally bioavailable allosteric inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. Akt inhibitor MK2206 binds to and inhibits the activity of Akt in a non-ATP competitive manner, which may result in the inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Akt inhibitor SR13668

An orally bioavailable indole-3-carbinol (I3C) analogue inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic and antiangiogenic activities. Akt inhibitor SR13668 binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation, and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Alba-Dex

(Other name for: dexamethasone)

albuterol sulfate

The sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Albuterol stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP concentrations relax bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent albuterol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Aldactone

(Other name for: spironolactone)

Aldara

(Other name for: imiquimod)

aldesleukin

A recombinant analog of the endogenous cytokine interleukin-2 (IL-2) with immunoregulatory and antineoplastic activities. Aldesleukin binds to and activates the IL-2 receptor, followed by heterodimerization of the cytoplasmic domains of the IL-2R beta and gamma(c) chains; activation of the tyrosine kinase Jak3; and phosphorylation of tyrosine residues on the IL-2R beta chain, resulting in an activated receptor complex. Various cytoplasmic signaling molecules are recruited to the activated receptor complex and become substrates for regulatory enzymes that are associated with the receptor complex. This agent enhances lymphocyte mitogenesis; stimulates long-term growth of human IL-2 dependent cell lines; enhances lymphocyte cytotoxicity; induces lymphokine-activated killer (LAK) cell and natural killer (NK) cell activities; and induces expression of interferon-gamma. Aldesleukin may induce T cell-mediated tumor regression in some tumor types.

aldoxorubicin

A 6-maleimidocaproyl hydrazone derivative prodrug of the anthracycline antibiotic doxorubicin (DOXO-EMCH) with antineoplastic activity. Following intravenous administration, aldoxorubicin binds selectively to the cysteine-34 position of albumin via its maleimide moiety. Doxorubicin is released from the albumin carrier after cleavage of the acid-sensitive hydrazone linker within the acidic environment of tumors and, once located intracellularly, intercalates DNA, inhibits DNA synthesis, and induces apoptosis. Albumin tends to accumulate in solid tumors as a result of high metabolic turnover, rapid angiogenesis, hyervasculature, and impaired lymphatic drainage. Because of passive accumulation within tumors, this agent may improve the therapeutic effects of doxorubicin while minimizing systemic toxicity.

alefacept

A recombinant dimeric fusion protein consisting of the extracellular CD2-binding domain of the human leukocyte function-associated antigen 3 (LFA-3; CD58) linked to the Fc portion of human immunoglobulin G1 (IgG1) with potential immunosuppressive activity. Alefacept binds to the CD2 receptor expressed on the majority of T lymphocytes, blocking the binding of endogenous LFA-3, located on antigen-presenting cells (APCs), to the CD2 receptor; the activation and proliferation of T lymphocytes in response to LFA-3 binding is thus inhibited. In addition, binding of the IgG1 moiety of this agent to the Fc gamma receptor on the surface of natural killer (NK)cells may bridge NK cells and target T lymphocytes, initiating NK cell-mediated apoptosis of T lymphocytes.

alemtuzumab

A recombinant DNA-derived humanized monoclonal antibody directed against the cell surface glycoprotein CD52. Alemtuzumab is an IgG1 kappa with human variable framework and constant regions, and complementarity-determining regions derived from a rat monoclonal antibody. This agent selectively binds to CD52, thereby triggering a host immune response that results in lysis of CD52 + cells. CD52 is a glycoprotein expressed on the surface of essentially all normal and malignant B and T cells, a majority of monocytes, macrophages and natural killer (NK) cells, a subpopulation of granulocytes, and tissues of the male reproductive system.

alendronate sodium

The sodium salt of alendronate, a second generation bisphosphonate and synthetic analog of pyrophosphate with bone anti-resorption activity. Alendronate sodium binds to and inhibits the activity of geranyltranstransferase (farnesyl pyrophosphate synthetase), an enzyme involved in terpenoid biosynthesis. Inhibition of this enzyme prevents the biosynthesis of isoprenoid lipids (FPP and GGPP) that are donor substrates of farnesylation and geranylgeranylation during the post-translational modification of small GTPase signalling proteins, which is important in the process of osteoclast turnover. As a result, osteoclast activity is inhibited and bone resorption and turnover are reduced.

Alfenta

(Other name for: alfentanil hydrochloride)

alfentanil hydrochloride

The hydrochloride salt of alfentanil, a synthetic short-acting opioid with analgesic and local anesthesia enhancing activity. Alfentanil hydrochloride primarily binds to mu-opioid receptor, a G-protein-coupled receptor, thereby mimicking the actions of morphine, the prototypical mu receptor agonist. This agent induces anti-nociception responses mediated through inhibiting the release of various neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline; in addition, the release of vasopressin, somatostatin, insulin and glucagon are also inhibited.

Alferon

(Other name for: recombinant interferon alpha-2a)

Alferon N

(Other name for: recombinant interferon alfa)

alfuzosin hydrochloride

The hydrochloride salt of alfuzosin, a quinazoline compound with smooth muscle-relaxing activity. Alfuzosin selectively binds to and antagonizes post-synaptic alpha1-adrenoreceptors in smooth muscle of the prostate, bladder base, bladder neck, prostatic capsule, and prostatic urethra, initiating relaxation of smooth muscle and resulting in improvement of urine flow and the symptoms of benign prostatic hyperplasia (BPH). This agent also blocks alpha1-adrenoreceptors in peripheral vascular smooth muscle, resulting in vasodilatation and a decrease in peripheral vascular resistance.

algenpantucel-L

A cancer vaccine comprised of irradiated allogeneic pancreatic cancer cells transfected to express murine alpha-1,3-galactosyltransferase with potential antitumor activity. Vaccination is associated with the expression of murine alpha-1,3-galactosyl (alpha-gal) carbohydrate residues on cell membrane glycoproteins and glycolipids of the vaccine pancreatic cancer cell allograft; murine alpha-gal epitopes, not present on human cells, then induce a hyperacute rejection of the vaccine pancreatic cancer cell allograft. The hyperacute rejection involves the binding of pre-existing human anti-alpha-gal antibodies (which naturally occur against gut flora) to murine alpha-gal epitopes, resulting in the rapid activation of antibody-dependent cell-mediated cytotoxicity (ADCC) towards allograft cells. The host immune system then attacks endogenous pancreatic cancer cells, resulting in ADCC towards endogenous pancreatic cancer cells.

ALIMTA

(Other name for: pemetrexed disodium)

alisertib

A second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Alisertib binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis, and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers.

alitretinoin

An orally- and topically-active naturally-occurring retinoic acid with antineoplastic, chemopreventive, teratogenic, and embryotoxic activities. Alitretinoin binds to and activates nuclear retinoic acid receptors (RAR) and retinoid X receptors (RXR); these activated receptors act as transcription factors, regulating gene expression that results in the inhibition of cell proliferation, induction of cell differentiation, and apoptosis of both normal cells and tumor cells.

ALK inhibitor CH5424802

An orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. Upon administration, ALK inhibitor CH542480 binds to and inhibits ALK kinase, ALK fusion proteins as well as the gatekeeper mutation ALKL1196M known as one of the mechanisms of acquired resistance to small-molecule kinase inhibitors. The inhibition leads to disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK dysregulation and gene rearrangements are associated with a series of tumors.

ALK inhibitor RO5424802

An orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity. Upon administration, ALK inhibitor RO5424802 binds to and inhibits ALK kinase, which leads to a disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK dysregulation and gene rearrangements are associated with a series of tumors. Additionally, ALK mutations are associated with acquired resistance to small molecule tyrosine kinase inhibitors.

ALK inhibitor X-396

An orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK is not expressed in healthy adult human tissue but ALK dysregulation and gene rearrangements are associated with a series of tumors; ALK mutations are associated with acquired resistance to small molecule tyrosine kinase inhibitors.

Alka Seltzer Gold

(Other name for: sodium bicarbonate/potassium bicarbonate/anhydrous citric acid)

Alkagin

(Other name for: zinc oxide/aluminum starch octenylsuccinate/glycyrrhetinic phytosome/vitamin E/botanical extracts-based skin protectant paste)

Alkeran

(Other name for: melphalan)

AllerNaze

(Other name for: triamcinolone acetonide)

allodepleted haploidentical T cells expressing inducible Caspase 9

Allodepleted haploidentical T-lymphocytes transduced with the Gal-V pseudotyped retrovirus vector encoding SFG.iCasp9-2A-deltaCD19, with potential immune reconstitution property. SFG.iCasp9-2A-deltaCD19 contains the suicide gene inducible caspase 9 (iCasp9) linked with a 2A-like cleavable peptide to the selectable marker, truncated human CD19 (deltaCD19). iCasp9 consists of a human FK506 drug-binding domain with an F36V mutation (FKBP12-F36V) linked to human caspase 9 using a short linker (SGGGS). Donor T cell therapy may help control transplant-related viral infections following allogeneic hematopoietic stem cell transplantation. However, even the addition of allodepleted donor T cells can lead to graft-versus-host disease (GVHD). In the event that GVHD begins to develop, the chemical homodimerizer AP1903 can be administered, which binds to the FKBP12-F36V domain activating caspase 9. This results in the death of T cells causing GVHD while sparing the virus reactive T-cells.

AlloDerm

(Other name for: acelullar cadaveric dermal matrix)

allogeneic acute myeloid leukemia antigen-expressing dendritic cell vaccine

A cancer vaccine consisting of allogeneic, immortalized dendritic precursor cells derived from a patient with acute myelogenous leukemia (AML), with potential immunostimulatory and antineoplastic activities. Upon ex vivo stimulation and expansion of the precursor cells into mature, fully functional dendritic cells (DCs) and subsequent administration, the allogeneic AML antigen-expressing DC vaccine may elicit a potent cytotoxic T-cell (CTL) and antibody response against AML antigen-expressing cells, resulting in tumor cell death.

allogeneic adenovirus-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T-lymphocytes (CTLs) specifically reactive to human adenovirus (Ad) with potential immunomodulating and anti-adenoviral activities. Upon immunoprophylactic adoptive cell therapy, infusion of allogeneic Ad-specific CTLs may help reconstitute Ad-specific CTL responses in patients at risk of developing Ad infections after allogeneic stem cell transplant or in Ad-infected immunocompromised hosts. These allogeneic Ad-specific CTLs are prepared by multiple rounds of stimulation with donor peripheral blood mononuclear cells and lymphoblastoid cell lines that have been transduced with Ad5f35, a recombinant adenoviral vector carrying no transgene.

allogeneic B7.1/HLA-A1 transfected tumor cell vaccine

An allogeneic whole cell vaccine, derived from irradiated allogenic tumor cells manipulated to express human B7.1 (CD80 antigen) and human leukocyte antigen (HLA) A1, with potential antitumor activity. Vaccination with allogeneic B7.1/HLA-A1 transfected tumor cell vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor cell proliferation.

allogeneic CD19-specific CAR-modified CD8 positive central memory-derived virus-specific T cells

A preparation of allogeneic Epstein-Barr virus (EBV)- and human cytomegalovirus (CMV)-specific CD8+ central memory-derived T effector-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) anti-CD19/CD3 zeta chain fusion protein coupled to the intracellular signal domain of CD28 antigen, with potential immunostimulating, anti-viral and antineoplastic activities. Upon infusion, allogeneic CD19-specific CAR-modified CD8+ central memory-derived virus-specific T cells directs the T-lymphocytes to CD19-expressing tumor cells, stimulating a selective toxicity to tumor cells which may eventually result in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. The viral specific T-cells exert antiviral immunity.

allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28

A preparation consisting of allogeneic, differentiated Th1-like T cells bound to T cell-stimulating monoclonal antibodies with potential antitumor activity. More specifically, allogeneic CD4+ memory Th1-like T cells/microparticle-bound anti-CD3/anti-CD28 are composed of a proprietary preparation of mismatched, allogeneic differentiated CD4+ memory Th1-like T cells bound to paramagnetic, epoxy-covered 4.5 micron microparticles with covalently bound anti-CD3/anti-CD28 monoclonal antibodies at a 2:1 bead:cell ratio. The CD4+ memory Th1-like T cells are derived from precursors found in the circulation of a normal donor. Stimulated by the microparticle-bound monoclonal antibodies, the infused T cells produce pro-inflammatory, anti-tumor cytokines such as like IFN-gamma, TNF-beta, and IL-2, disabling tumor immune avoidance mechanisms and stimulating the host immune system to both reject the infused T cells and kill tumor cells.

allogeneic CMV/AdV-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T lymphocytes (CTLs) specifically reactive to cytomegalovirus (CMV) and adenovirus (AdV) with potential antiviral activity. Allogeneic CMV/AdV-specific cytotoxic T lymphocytes are prepared by exposing donor-derived CTLs to a lethally irradiated Epstein-Barr virus-positive lymphoblastoid B cell line (EBV-LCL) that has been transduced with a clinical-grade adenoviral vector (Ad5f35CMVpp65) as a source of CMV and AdV antigens. Infusion of these CTLs into stem cell transplant recipients may prevent CMV and AdV viral disease.

allogeneic cytomegalovirus-specific cytotoxic T lymphocytes

A population of allogeneic cytotoxic T lymphocytes (CTLs) specifically reactive to the herpes virus cytomegalovirus (CMV) with potential immunomodulating and antiviral activities. Upon immunoprophylactic adoptive cell therapy infusion with allogeneic cytomegalovirus-specific cytotoxic T lymphocytes, these CTLs may help reconstitute CMV-specific CTL responses in CMV-infected immunocompromised hosts after allogeneic hematopoietic stem cell transplant, thereby potentially preventing the occurrence of CMV viral disease or reducing the amount of antiviral drug therapy.

allogeneic dendritic cell vaccine COMBIG-DC

A cancer vaccine consisting of allogeneic, immortalized dendritic cells (DCs) loaded with tumor specific antigens and activated, with potential immunostimulatory and antineoplastic activities. Upon intratumoral administration of the allogeneic dendritic cell vaccine COMBIG-DC, these activated DCs attract natural killer (NK) cells, induce an anti-inflammatory response leading to the induction of NK-cell-mediated tumor cell death. Upon release of tumor associated antigens (TAAs) from the lysed tumor cells, these antigens are taken up by antigen presenting cells which activate the immune system to elicit a potent cytotoxic T-cell (CTL) response against the TAAs, resulting in the death of TAAs-expressing tumor cells.

allogeneic dendritic cell-myeloma idiotype vaccine

A cell-based vaccine composed of allogeneic dendritic cells pulsed ex-vivo with an autologous myeloma idiotype with potential antineoplastic activity. Upon administration, allogeneic dendritic cell-myeloma idiotype vaccine may stimulate the host immune system to mount a specific cytotoxic T-lymphocyte (CTL) response against myeloma cells, resulting in cell lysis.

allogeneic Epstein-Barr virus-specific cytotoxic T lymphocytes

A preparation of lymphocytes harvested from a patient with an Epstein-Barr virus (EBV)-positive tumor. Ex vivo, the lymphocytes are activated against EBV-specific antigens and then returned to the patient, where they mount a specific immune response against EBV-positive tumor cells.

allogeneic GM-CSF-secreting breast cancer vaccine

An allogenic vaccine consisting of irradiated breast cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene. Upon vaccination, the genetically modified cells secrete GM-CSF, thereby potentiating a tumor-specific T cell response against breast cancer cell-asociated antigens.

allogeneic GM-CSF-secreting lethally irradiated whole melanoma cell vaccine

An allogeneic cancer vaccine composed of lethally irradiated whole melanoma cancer cells that are genetically modified to secrete the immunostimulatory cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Upon intradermal injections, allogeneic GM-CSF-secreting lethally irradiated whole melanoma cell vaccine secretes GM-CSF. In turn, GM-CSF may stimulate the body's immune system against tumor cells by enhancing the activation of dendritic cells (DCs) and promoting antigen presentation to both B- and T-lymphocytes. In addition, GM-CSF promotes antibody-dependent cellular cytotoxicity (ADCC), and increases interleukin-2-mediated lymphokine-activated killer cell function.

allogeneic GM-CSF-secreting tumor vaccine PANC 10.05 pcDNA-1/GM-Neo

An allogeneic cancer vaccine composed of lethally irradiated, whole pancreatic cancer cells transfected with a plasmid carrying the gene for cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Allogeneic GM-CSFsecreting tumor vaccine PANC 10.05 pcDNA-1/GM-Neo secretes GM-CSF thereby activating dendritic cells, promoting antigen presentation to B- and T-cells, and promoting a cytotoxic T-lymphocyte (CTL) response. This may eventually kill tumor cells. The pancreatic tumor cells are derived from the PANC 10.05 tumor cell line.

allogeneic GM-CSF-secreting tumor vaccine PANC 6.03 pcDNA-1/GM-Neo

An allogeneic cancer vaccine composed of lethally irradiated, whole pancreatic cancer cells transfected with a plasmid carrying the gene for cytokine granulocyte-macrophage colony-stimulating factor (GM-CSF), with potential immunostimulating and antineoplastic activities. Allogeneic GM-CSFsecreting tumor vaccine PANC 6.03 pcDNA-1/GM-Neo secretes GM-CSF thereby activating dendritic cells, promoting antigen presentation to B- and T-cells, and promoting a cytotoxic T-lymphocyte (CTL) response. This may eventually kill tumor cells. The pancreatic tumor cells are derived from the PANC 6.03 tumor cell line.

allogeneic GM-CSF-transfected myeloma cell vaccine

An allogeneic tumor cell vaccine containing myeloma cancer cells transfected with the granulocyte macrophage-colony-stimulating factor (GM-CSF) gene with potential antineoplastic activity. Upon vaccination, allogeneic GM-CSF-based myeloma cellular vaccine secretes GM-CSF, which may potentiate a tumor-specific cytotoxic T-lymphocyte (CTL) response against myeloma cancer cell-associated antigens.

allogeneic HLA A2/4-1BB ligand-expressing melanoma vaccine

An allogeneic melanoma cell vaccine derived from a cell line with high expression of melanoma associated antigens and genetically modified to express both HLA-A2 and 4-1BB ligand, with potential immunostimulating and antineoplastic activities. Upon administration, the 4-1BB ligand of the allogeneic HLA-A2/4-1BB ligand-expressing melanoma vaccine binds to 4-1BB on activated T-lymphocytes, which induces a strong immune response against HLA-A2 positive melanoma cells.

allogeneic IL13-zetakine/HyTK-expressing-glucocorticoid resistant cytotoxic T lymphocytes GRm13Z40-2

A preparation of glucocorticoid receptor (GR) negative, allogeneic cytotoxic T-lymphocytes (CTLs) expressing a membrane-tethered interleukin 13 (IL13) cytokine chimeric T-cell antigen receptor (zetakine), with potential antineoplastic activity. Upon transfection of donor T-lymphocytes with a plasmid encoding a fusion protein of the IL13-zetakine and the selection-suicide expression enzyme HyTK, these modified CTLs are expanded and introduced into a patient with glioblastoma multiforme (GBM). This agent specifically targets IL13 receptor alpha2, a glioma-restricted cell-surface epitope; the CTLs exert their cytolytic effect thereby killing IL13Ra2-expressing glioma cells. In addition, IL13-zetakine redirected CTLs induce production of certain cytokines. Furthermore, due to the fact that these CTLs are GR negative, they can be used concomitantly with glucocorticoid therapy. The IL13-zetakine consists of an extracellular IL-13 E13Y mutein-human IgG4 hinge-Fc chimera fused to human cytoplasmic CD3-zeta via the transmembrane domain of human CD4.

allogeneic irradiated melanoma cell vaccine CSF470

An allogeneic cancer vaccine composed of a mixture of lethally irradiated whole melanoma cancer cells obtained from four different melanoma cell lines, with potential immunostimulating and antineoplastic activities. Upon intradermal injections, allogeneic irradiated melanoma cell vaccine may stimulate the body's immune system to exert a cytotoxic T-lymphocyte response and antibody-dependent cellular cytotoxicity (ADCC) against the melanoma cancer cells.

allogeneic large multivalent immunogen breast cancer vaccine

A cancer vaccine, containing human-specific large multivalent immunogens (LMIs) isolated from the membrane fraction of cells from a breast cancer cell line, with potential immunostimulatory and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen breast cancer vaccine may stimulate a cytotoxic T lymphocyte (CTL) immune response against tumor cells that express the breast cancer cell-specific LMIs.

allogeneic large multivalent immunogen melanoma vaccine LP2307

A cancer vaccine, containing human-specific large multivalent immunogen (LMI) isolated from plasma membrane fractions of the melanoma cell lines MSM-M1 and MSM-M2, with potential immunostimulating and antineoplastic activities. Upon administration, allogeneic large multivalent immunogen melanoma vaccine LP2307 may stimulate a CD8+ cytotoxic T lymphocyte (CTL) response against melanoma tumor cells that express melanoma-specific LMI.

allogeneic LMP1-/LMP2- specific cytotoxic T-lymphocytes

A preparation of cytotoxic T-lymphocytes (CTL), specifically reactive to the Epstein-Barr virus (EBV) latent membrane proteins (LMP) 1 and 2, with potential antineoplastic activity. Peripheral blood mononuclear cells (PBMC) are collected from a donor and are exposed ex vivo to dendritic cells (DCs) transfected with a replication-deficient adenovirus encoding EBV LMP1/2 to generate LMP1/2-specific CTL which are subsequently expanded. Administration of allogeneic LMP1-/LMP2- specific CTL to patients with LMP1/2-positive tumors may result in a specific CTL response against tumor cells expressing LMP1 and LMP2, resulting in cell lysis and inhibition of tumor cell proliferation. As tumor associated antigens (TAAs), LMP1 and LMP2 are expressed in various malignancies including nasopharyngeal cancer and EBV-positive Hodgkin lymphoma.

allogeneic melanoma vaccine AGI-101H

A cancer vaccine derived from two gentically modified human melanoma cell lines with potential antineoplastic activity. Allogeneic melanoma vaccine AGI-101H consists of a 1:1 mixture of cells from two genetically modified human melanoma cell lines, designated as Mich1H6 and Mich2H6, that have been gamma-irradiated to render the cells non-proliferative. Upon administration, this vaccine may stimulate a cytotoxic immune response against melanoma tumor cells.

allogeneic multipotent adult progenitor cells

A biologic product that consists of undifferentiated stem cells, obtained from adult bone marrow or other non-embryonic tissue sources, that are expanded in vitro and deposited in master cell banks for "off-the-shelf" use, with potential hematopoiesis-inducing and immunomodulating activities. Allogeneic multipotent adult progenitor cells (MAPCs) are non-immunogenic due to the lack of major histocompatibility (MHC) molecule expression, and so elicit no immune response upon administration. In vivo, bone marrow-derived adult stem cells are capable of maturing into a broad range of cell types and may help restore the immune system by producing multiple therapeutic molecules in response to inflammation and tissue damage.

allogeneic natural killer cell line MG4101

A population of allogeneic, cytotoxic natural killer (NK) cells with potential antitumor activity. Allogeneic natural killer cell line MG4101 is derived from cells of a normal, healthy donor upon leukapheresis and activation.

allogeneic renal cell carcinoma vaccine MGN1601

A whole cell vaccine comprised of irradiated allogeneic renal cell carcinoma (RCC) with potential immunostimulating and antineoplastic activities. Allogeneic renal cell carcinoma vaccine MGN1601 contains two active ingredients: 1) genetically modified allogeneic RCC cells that are transiently transfected with four different MIDGE (Minimalistic Immunogenically Defined Gene Expression) vectors encoding IL-7, GM-CSF, CD80 and CD154 and 2) the synthetic DNA-based immunomodulator dSLIM-30L1, a TLR9 agonist. Vaccination results in expression of IL-7, GM-CSF, CD80 and CD154, which all contribute to the activation or enhancement of immune responses. Furthermore, administration of this RCC vaccine may elicit a cytotoxic T lymphocyte (CTL) response against similar host tumor cells, resulting in decreased tumor growth. TLR9 is a member of the TLR family, which plays a fundamental role in pathogen recognition and activation of innate immunity.

allogeneic T lymphocytes BPX-501

Allogeneic T lymphocytes with potential immune reconstitution activity. Donor T lymphocytes are transduced with a retroviral vector (BPZ-1001) encoding the inducible suicide gene caspase 9 (iCasp9) and linked to a drug binding domain. Donor T-cell therapy may help control transplant-related infections following allogeneic hematopoietic stem cell transplantation. However, the addition of donor T cells can lead to graft-versus-host disease (GVHD). In the event that GVHD begins to develop, the chemical homodimerizer AP1903 can be administered, which binds to the drug binding domain and induces caspase 9 expression. This activates apoptosis in the T cells causing GVHD.

allogeneic tumor cell vaccine

A vaccine composed of tumor cells isolated from the tumor of one patient, killed and processed, and administered to another patient in order to stimulate cytotoxic immune responses to a similar tumor cell type. The cells found in this type of whole-cell vaccine express many cell-surface tumor-associated antigens. This vaccine is frequently administered with an adjuvant immunostimulant.

allopurinol

A structural isomer of hypoxanthine. Allopurinol inhibits xanthine oxidase, an enzyme that converts oxypurines to uric acid. By blocking the production of uric acid, this agent decreases serum and urine concentrations of uric acid, thereby providing protection against uric acid-mediated end organ damage in conditions associated with excessive production of uric acid, i.e. the massive cell lysis associated with the treatment of some malignancies.

almurtide

A synthetic muramyl dipeptide (MDP) H8analogue with potential immunostimulating and antineoplastic activity. As a derivative of the mycobacterial cell wall component MDP, almurtide activates both monocytes and macrophages. This results in the secretion of cytokines and induces the recruitment and activation of other immune cells, which may result in indirect tumoricidal or cytostatic effects.

Alocrest

(Other name for: injectable liposomal vinorelbine)

aloe vera gel

A preparation of leaf pulp from the parenchymal tissue of the plant Aloe vera (Liliaceae). Aloe vera gel contains carbohydrate polymers, such as glucomannans or pectic acid, and various vitamins and essential amino acids, as well as other organic and inorganic compounds. This agent has been used internally or externally for sunburn, skin problems, insect bites, ulcers, arthritis, constipation, and as an immune system enhancer.

alogliptin

A selective, orally bioavailable, pyrimidinedione-based inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. In addition to its effect on glucose levels, alogliptin may inhibit inflammatory responses by preventing the toll-like receptor 4 (TLR-4)-mediated formation of proinflammatory cytokines.

Aloxi

(Other name for: palonosetron hydrochloride)

alpha fetoprotein adenoviral vector vaccine

A vaccine consisting of a recombinant adenoviral vector encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis.

alpha fetoprotein plasmid DNA vaccine

A vaccine consisting of plasmid DNA encoding alpha fetoprotein. After vaccination, expressed alpha fetoprotein may stimulate a cytotoxic T lymphocyte (CTL) response against tumor cells that express alpha fetoprotein, resulting in tumor cell lysis.

alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine

An allogeneic lung cancer vaccine with potential immunostimulating and antineoplastic activities. Derived from allogeneic lung tumor cells, alpha-1,3-galactosyltransferase-expressing allogeneic lung tumor cell vaccine is engineered to express the murine alpha-1,3-galactosyltransferase (GalT), an enzyme humans lack. GalT catalyzes the expression of foreign alpha-1,3-galactosyl (alpha-gal) carbohydrate epitopes in glycoproteins and in glycolipids on the cell membranes of the allogeneic lung tumor cells present in the vaccine, essentially producing a "xenograft". The hyperacute rejection involves pre-existing human anti-alpha-gal antibodies that bind the foreign alpha-gal epitopes expressed by the vaccine tumor cell xenograft, resulting in complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) towards endogenous lung tumor cells with unmodified carbohydrate epitopes.

alpha-1-proteinase inhibitor human

Human serum-derived alpha-1 proteinase inhibitor (alpha-1-antitrypsin or AAT) with immunomodulating and anti-inflammatory activity. Upon administration, AAT reduces the production of proinflammatory cytokines, such as tumor necrosis factor-alpha, interleukin (IL)-1 beta, IL-32, IL-6, and proteinase 3, and induces the production of anti-inflammatory cytokines, such as IL-10 and the IL-1 receptor antagonist IL-1RN. This agent also downregulates heparan sulfate and reduces the expansion of cytotoxic effector T cells, interferes with the maturation of dendritic cells and increases T regulatory cells. Altogether, AAT may attenuate acute graft-versus-host disease (GvHD) and may facilitate graft acceptance and survival. In addition, AAT enhances levels of cAMP and activation of cAMP-dependent protein kinase A. AAT, a 52kD protein and serine protease inhibitor, belongs to the serpin superfamily.

alpha-fetoprotein peptide-pulsed autologous dendritic cell vaccine

A cell-based cancer vaccine comprising autologous dendritic cells pulsed with four alpha-fetoprotein (AFP) peptides, with potential immunostimulatory and antineoplastic activities. Upon administration, AFP peptide-pulsed autologous dendritic cell vaccine may stimulate anti-tumoral cytotoxic T lymphocyte (CTL) and antibody responses against AFP-expressing cancer cells, resulting in tumor cell lysis. AFP is overexpressed in a variety of cancer cells.

alpha-Gal glycosphingolipids

A preparation of glycosphingolipids (GSL), containing the disaccharide epitope galactose-alpha-1,3-galactose (alpha-Gal), with potential antineoplastic activity. Upon intratumoral injection, alpha-Gal glycosphingolipids may stimulate the immune system to mount complement-mediated cytotoxicity (CMC) and antibody-dependent cell-mediated cytotoxicity (ADCC) responses against alpha-Gal GSL, which may result in tumor cell death; these responses involve natural anti-alpha-Gal immunoglobulins (Igs). As antibodies that occur naturally due to sensitization to alpha-Gal present on symbiotic bacterial flora, anti-alpha-Gal Igs are present in unusually high amounts in human sera. GSL represent a glycolipid subtype containing the amino alcohol sphingosine; tumor-associated GSL antigens contain various oligosaccharide residues.

alpha-galactosylceramide-pulsed autologous dendritic cells

A cancer vaccine comprised of autologous dendritic cells (DCs) pulsed with the marine sponge glycolipid alpha-galactosylceramide (alpha-GalCer) with potential immunostimulatory and antimetastatic activities. Upon administration, alpha-galactosylceramide-pulsed autologous dendritic cells may result in the activation and proliferation of a subset of endogenous natural killer T ( NKT) cells, B cells, and CD4+ and CD8+ T cells, and the production of interferon-gamma and interleukin-12; these cascade events may result in a T helper-1 cell-biased proinflammatory antitumor immune response. The NKT cell ligand alpha-GalCer was originally isolated from the marine sponge Agelas mauritianusis.

alpha-lipoic acid

A naturally occurring micronutrient, synthesized in small amounts by plants and animals (including humans), with antioxidant and potential chemopreventive activities. Alpha-lipoic acid acts as a free radical scavenger and assists in repairing oxidative damage and regenerates endogenous antioxidants, including vitamins C and E and glutathione. This agent also promotes glutathione synthesis. In addition, alpha-lipoic acid exerts metal chelating capacities and functions as a cofactor in various mitochondrial enzyme complexes involved in the decarboxylation of alpha-keto acids.

alpha-lipoic acid/vitamin/mineral supplement PolyMVA

A proprietary water- and lipid-soluble polymer-based nutritional supplement composed of a complex mixture of alpha-lipoic acid bound to palladium (palladium lipoic acid complex (PdLA)) and other minerals, vitamins and amino acids, including vitamins B1, B2 and B12, formylmethionine, acetyl cysteine, and trace amounts of molybdinum, rhodium, and ruthenium, with potential anti-oxidant and cytoprotective activities. Upon oral administration, the alpha-lipoic acid-palladium/vitamin/mineral supplement acts as a free radical scavenger, crosses the cell membrane and is able to transfer electrons from fatty acids to DNA via the electron transport chain in mitochondria, which protects against DNA damage. This could protect non-cancerous cells from the oxidative damage caused by radiation and chemotherapy. In addition, in the hypoxic conditions found within tumors, the excess electrons can generate free radicals within mitochondria and could induce both cytochrome c release and apoptosis.

alpha-type-1 polarized dendritic cells

A population of mature polarized dendritic cells with potent immunostimulating activity. Treating bone marrowed-derived dendritic cells (DCs) with interferon-alpha (IFN-a), polyinosinic:polycytidylic acid (poly I:C) and bacterial CpG-DNA produces mature but not exhausted alpha type-1 polarized DCs (alphaDC1) that are capable of: 1) high responsiveness to other lymphoid chemokines, and 2) producing high levels of interleukin-12p70 (IL-12p70), characteristics found in human type-1 polarized dendritic cells. When pulsed with specific tumor associated antigens (TAAs), alphaDC1 may induce a potent cytotoxic T lymphocyte (CTL) response against TAA-expressing tumor cells.

alprazolam

A triazolobenzodiazepine agent with anxiolytic, sedative-hypnotic and anticonvulsant activities. Alprazolam binds to a specific site distinct from the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) binding site on the benzodiazepine-GABA-A-chloride ionophore receptor complex located in the limbic, thalamic and hypothalamic regions of the central nervous system (CNS). This binding causes an allosteric modification of the receptor and enhances the affinity of GABA to the receptor leading to an increase in the frequency of chloride-channel opening events. This leads to an increase in chloride ion conductance, neuronal hyperpolarization, inhibition of the action potential and leads to a decrease in neuronal excitability.

alprostadil

The naturally occuring prostaglandin E1 (PGE1) which displays a variety of pharmacologic actions. Alprostadil is a potent vasodilator agent that increases peripheral blood flow, inhibits platelet aggregation, and induces bronchodilation. Used in the treatment of erectile dysfunction, this agent produces corporal smooth muscle relaxation by binding to PGE receptors, resulting in the activation of adenylate cyclase and the subsequent accumulation of 3'5'-cAMP.

Altace

(Other name for: ramipril)

alteplase

A recombinant therapeutic agent which is chemically identical to or similar to endogenous tissue plasminogen activator (tPA). tPA is a serine protease which converts plasminogen to plasmin, a fibrinolytic enzyme. Upon administration, alteplase increases plasmin enzymatic activity, resulting in hyperfibrinolysis and potential dissolution of a thrombus or embolism.

Althose

(Other name for: methadone hydrochloride)

altretamine

A synthetic cytotoxic s-triazine derivative similar in structure to alkylating agent triethylenemelamin with antineoplastic activity. Although the precise mechanism by which altretamine exerts its cytotoxic effect is unknown, N-demethylation of altretamine may produce reactive intermediates which covalently bind to DNA, resulting in DNA damage.

alum adjuvant

An aluminum compound with immune adjuvant activity. This agent adsorbs and preciptates protein antigens in solution; the resulting precipitate improves vaccine immunogenicity by faclitating the slow release of antigen from the vaccine depot formed at the site of inoculation.

ALVAC(2) melanoma multi-antigen therapeutic vaccine

A therapeutic cancer vaccine, based on a replication-defective recombinant canarypox virus (ALVAC) encoding multiple melanoma antigens, with potential immunostimulatory and antineoplastic activities. Vaccination with ALVAC(2) melanoma multi-antigen therapeutic vaccine may stimulate the host immune system to mount an immune response against antigen-expressing melanoma cells, resulting in inhibition of tumor growth and/or metastasis.

ALVAC(2)-NY-ESO-1 (M)/TRICOM vaccine

A cancer vaccine consisting of a replication-defective recombinant canarypox virus [ALVAC(2)] encoding the cancer-testis antigen NY-ESO and the TRIad of COstimulatory Molecules (B7-1, ICAM-1 and LFA-3; also called TRICOM), with potential immunostimulatory and antineoplastic activities. Upon administration, ALVAC(2)/NY-ESO (M)/TRICOM vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against NY-ESO-expressing cancer cells, which may result in the inhibition of tumor cell proliferation. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cells, including bladder, breast, hepatocellular, melanoma, and prostate tumor cells. TRICOM may enhance antigen presentation and activate cytotoxic T-cells. In addition, ALVAC(2) encodes the vaccinia virus (vv) E3L ad K3L genes, which may potentiate the translation of the NY-ESO and TRICOM genes.

ALVAC-CEA vaccine

A cancer vaccine consisting of ALVAC, a highly attenuated poxvirus strain derived from the canarypox virus, encoding for the tumor associated antigen (TAA) carcinoembryonic antigen (CEA), with potential antineoplastic activity. Upon administration, ALVAC-CEA vaccine expresses CEA and may stimulate a host immune response against tumor cells expressing CEA. This may result in the inhibition of tumor growth and/or metastasis. CEA is overexpressed in a variety of tumor cell types.

ALVAC-ESO-1 vaccine

A cancer vaccine consisting of a replication-defective recombinant canarypox virus (ALVAC) encoding the cancer-testis antigen NY-ESO-1, with potential immunostimulatory and antineoplastic activities. Upon administration, ALVAC-ESO-1 vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against NY-ESO-1-expressing cancer cells, which may result in the inhibition of tumor cell proliferation. NY-ESO-1, a tumor associated antigen (TAA), is found in normal testis and on the surface of various tumor cells.

ALVAC-hB7.1

A vaccine comprise of a canarypox viral vector that carries the gene for human B7.1 (CD80 antigen) with potential use as an autologous therapeutic cancer vaccine. Tumor cells harvested from a patient are infected with ALVAC-hB7 1, thereby producing an autologous cell line that exhibits increased expression of HLA class I and class II, CD54 (ICAM), and CD80. Increased expression of these proteins by this autologous cell line may activate an antitumor T-cell response when the modified cells are administered to the patient.

ALVAC-MART-1 vaccine

A cancer vaccine containing a replication-defective recombinant canarypox virus (ALVAC), encoding an epitope of MART-1 (melanoma antigen recognized by T-cells), with potential immunostimulatory and antineoplastic activities. Upon administration, the MART-1 epitope is expressed by the ALVAC vector in ALVAC-MART-1 vaccine; a host cytotoxic T lymphocyte (CTL) response against MART-1-expressing tumor cells may follow, resulting in tumor cell lysis and decreased tumor cell proliferation.

alvespimycin hydrochloride

The hydrochloride salt of alvespimycin, an analogue of the antineoplastic benzoquinone antibiotic geldanamycin. Alvespimycin binds to HSP90, a chaperone protein that aids in the assembly, maturation and folding of proteins. Subsequently, the function of Hsp90 is inhibited, leading to the degradation and depletion of its client proteins such as kinases and transcription factors involved with cell cycle regulation and signal transduction.

alvimopan

A synthetic trans-3,4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons andthe immune cells of the lamina propria in the human gut. Upon administration, this agent binds to mu-opioid receptors in the gut, thereby reversing opiod-related disturbances in gut motility. Alvimopan is approximately three to nine times more potent than naloxone.

alvocidib

A synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.

amantadine hydrochloride

The hydrochloride salt of amantadine, a synthetic tricyclic amine with antiviral, antiparkinsonian, and antihyperalgesic activities. Amantadine appears to exert its antiviral effect against the influenza A virus by interfering with the function of the transmembrane domain of the viral M2 protein, thereby preventing the release of infectious viral nucleic acids into host cells; furthermore, this agent prevents virus assembly during virus replication. Amantadine exerts its antiparkinsonian effects by stimulating the release of dopamine from striatal dopaminergic nerve terminals and inhibiting its pre-synaptic reuptake. This agent may also exert some anticholinergic effect through inhibition of N-methyl-D-aspartic acid (NMDA) receptor-mediated stimulation of acetylcholine, resulting in antihyperalgesia.

amatuximab

A humanized IgG1 monoclonal antibody directed against human mesothelin with potential antineoplastic activity. Amatuximab binds to mesothelin, triggering an antibody dependent cellular cytotoxicity (ADCC)-mediated host immune response against mesothelin-expressing tumor cells, which may result in tumor cell lysis. Mesothelin, a 40kDa cell surface glycoprotein, is overexpressed in several human tumors, including mesothelioma and ovarian and pancreatic adenocarcinomas.

Ambien

(Other name for: zolpidem tartrate)

AmBisome

(Other name for: liposomal amphotericin B)

Ambochlorin

(Other name for: chlorambucil)

Amboclorin

(Other name for: chlorambucil)

Amdray

(Other name for: valspodar)

American ginseng

The aromatic root of the perennial herb Panax quinquefolius, native to eastern North America. American ginseng, used in Chinese traditional medicine and available as a nutritional supplement, is classified as an adaptogenic herb with multiple effects, many of which are regulatory in nature. It contains a complex mixture of saponin glycosides, also known as ginsenosides or panaxosides. Although the mechanism of action is unclear, this agent is reported to enhance the immune system and reduce fatigue.

Amevive

(Other name for: alefacept)

Amfebutamone

(Other name for: bupropion hydrochloride)

amifampridine

An organic compound derived from pyridine with potassium channel inhibition activity. Amifampridine inhibits potassium channel efflux, increasing the duration of the action potential, which results in an increase in the duration of calcium channel opening and enhanced acetylcholine (ACh) release. Increased ACh availability at the motor end plate allows muscles to contract.

amifostine trihydrate

The trihydrate form of a phosphorylated aminosulfhydryl compound. After dephosphorylation of amifostine by alkaline phosphatase to an active free sulfhydryl (thiol) metabolite, the thiol metabolite binds to and detoxifies cytotoxic platinum-containing metabolites of cisplatin and scavenges free radicals induced by cisplatin and ionizing radiation. The elevated activity of this agent in normal tissues results from both the relative abundance of alkaline phosphatase in normal tissues and the greater vascularity of normal tissues compared to tumor tissues.

aminobenzoate potassium

The potassium salt form of aminobenzoate, with anti-inflammatory and antifibrotic activities. Aminobenzoate potassium increases oxygen uptake at the tissue level and may enhance monoamine oxidase (MAO) activity, which requires oxygen as a substrate. Enhanced MAO activity maybe accountable for the prevention or regression of fibrosis, which may occur due to too much serotonin or too little MAO activity.

aminocamptothecin

A water-insoluble camptothecin derivative. Aminocamptothecin binds to the nuclear enzyme topoisomerase I, thereby inhibiting repair of single-strand DNA breakages. Because the terminal lactone ring of aminocamptothecin required for the agent's antitumor activity spontaneously opens under physiological conditions to an inactive carboxy form, the drug must be administered over an extended period of time to achieve effective cytotoxicity.

aminolevulinic acid hydrochloride

A topically administered metabolic precursor of protoporphyrin IX. After topical administration, aminolevulinic acid hydrochloride (ALA HCl) is converted to protoporphyrin IX (PpIX) which is a photosensitizer. When the proper wavelength of light activates protoporphyrin IX, singlet oxygen is produced, resulting in a local cytotoxic effect.

aminophylline

A methylxanthine and derivative of theophylline. Aminophylline relaxes smooth muscles, particularly bronchial muscles. This xanthine most likely exerts its effect by inhibiting cAMP or cGMP phosphodiesterases, thereby increasing levels of the second messenger cAMP or cGMP intracellularly. Other mode of actions include an adenosine antagonistic effect on the activity of CD4 lymphocytes and mediator release from mast cells thereby decreasing lung sensitivity to allergens and other substances that cause inflammation. Aminophylline also acts as a CNS stimulant and exerts a positive chronotropic and inotropic effect on the heart.

aminopterin

A synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analogue, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synthesis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis.

aminothiadiazole

A synthetic derivative of nicotinamide adenine dinucleotide (NAD). Aminothiadiazole competitively inhibits inosine 5-monophosphate dehydrogenase, thereby disrupting the regulation of cell proliferation and differentiation in a number of cells. This agent is also a selective human adenosine A3 receptor antagonist.

amiodarone hydrochloride

The hydrochloride salt of an iodine-rich benzofuran derivative with antiarrhythmic and vasodilatory activities. As a class III antiarrhythmic agent, amiodarone blocks the myocardial calcium, potassium and sodium channels in cardiac tissue, resulting in prolongation of the cardiac action potential and refractory period. In addition, this agent inhibits alpha- and beta-adrenergic receptors, resulting in a reduction in sympathetic stimulation of the heart, a negative chronotropic effect, and a decrease in myocardial oxygen demands. Amiodarone may cause vasodilation by stimulation of the release of nitric oxide and cyclooxygenase-dependent relaxing endothelial factors.

Amitiza

(Other name for: lubiprostone)

amitriptyline hydrochloride

The hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive activities. Amitriptyline inhibits the re-uptake of norepinephrine and serotonin by the presynaptic neuronal membrane in the central nervous system (CNS), thereby increasing the synaptic concentration of norepinephrine and serotonin. Due to constant stimulation to these receptors, amitriptyline may produce a downregulation of adrenergic and serotonin receptors, which may contribute to the antidepressant activity. In the CNS the antinociceptive activity of this agent may involve high affinity binding to and inhibition of N-methyl-D-aspartate (NMDA) receptors and/or the enhancement of the action of serotonin at the spinal terminals of an opioid-mediated intrinsic analgesia system.

AML mRNA plus lysate loaded autologous dendritic cell vaccine

A cancer vaccine consisting of autologous dendritic cells loaded with separate preparations of acute myelogenous leukemia (AML) cell lysate and AML-specific messenger RNA (mRNA) with potential immunostimulatory and antineoplastic activities. Upon administration, AML mRNA plus lysate loaded autologous dendritic cell vaccine may elicit a potent cytotoxic T-cell (CTL) response against AML cells, resulting in tumor cell death.Autologous dendritic cells doubly-loaded with AML cell lysate and AML-specific mRNA may elicit superior primary, recall, and effector lytic immune responses compared to autologous dendritic cells loaded with tumor lysate or tumor mRNA alone.

Ammoidin

(Other name for: methoxsalen)

ammonium trichlorotellurate

A synthetic non-toxic tellurium derivative, structurally similar to cisplatin, with immuno-modulating, antiviral, and hair growth-promoting activities. Ammonium trichlorotellurate may inhibit the inflammatory cytokine interleukin-10 (IL-10) and may induce hematopoietic cells to express interleukin-2 (IL-2), IL-2 receptors, granulocyte-macrophage colony-stimulating factor (GM-CSF), IL-3, tumor necrosis factor (TNF) and interferons (INFs). This agent is also a potent inducer of IL-1 and IL-6. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced myelosuppression. In addition, this agent exhibits hair growth-promoting activity by inducing anagen production and inhibiting catagen production, resulting in the promotion of follicular keratinocyte proliferation and interference with follicular keratinocyte terminal differentiation, respectively. Accordingly, ammonium trichlorotellurate may protect against chemotherapy-induced alopecia.

Amnesteem

(Other name for: isotretinoin)

amnion-derived cellular cytokine solution

A topical cellular cytokine solution containing a distinct combination of growth factors and cytokines secreted by and released from amnion-derived multipotent progenitor (AMP) cells, with potential immunomodulating and skin healing activities. The amnion-derived cellular cytokine solution (ACCS) contains near physiological levels of transforming growth factor beta, tissue inhibitor of metalloproteinase-1 (TIMP-1) and TIMP-2, as well as the angiogenesis factors platelet-derived growth factor (PDGF), vascular endothelial growth factor (VEGF) and angiogenin that are normally found in healing wounds. Upon spraying the solution onto affected areas, the cytokines and growth factors in ACCS appear to increase the migration, proliferation and differentiation of both keratinocytes and fibroblasts; enhance the migration and phagocytosis of macrophages in wounds; and increase epithelialization. Together these processes may accelerate skin healing and tissue repair. Also, ACCS may be beneficial in the treatment of radiation burns of the skin.

amonafide dihydrochloride

The dihydrochloride salt of amonafide, an imide derivative of naphthalic acid. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis.

amonafide L-malate

The malate salt of amonafide, an imide derivative of naphthalic acid, with potential antineoplastic activity. Amonafide intercalates into DNA and inhibits topoisomerase II, resulting in DNA double-strand breaks (DSB) and inhibition of DNA replication and RNA synthesis.

amoxicillin

A broad-spectrum, semisynthetic aminopenicillin antibiotic with bactericidal activity. Amoxicillin binds to and inactivates penicillin-binding protein (PBP) 1A located on the inner membrane of the bacterial cell wall. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This interrupts bacterial cell wall synthesis and results in the weakening of the bacterial cell wall and causes cell lysis.

amoxicillin-clavulanate potassium

A combination of the semisynthetic broad-spectrum antibiotic amoxicillin and the beta-lactamase enzyme inhibitor clavulanate potassium. Clavulanate potassium increases the serum half-life of amoxicillin by inhibiting beta-lactamase-mediated metabolism of amoxicillin. Amoxicillin inhibits bacterial cell wall synthesis by binding to penicillin binding proteins and inhibiting peptidoglycan synthesis, a critical component of bacterial cell walls.

Amoxil

(Other name for: amoxicillin)

amphotericin B deoxycholate

The deoxycholate salt of amphotericin B, a polyene antifungal antibiotic produced by Streptomyces nodosus, with antifungal activity. Amphotericin B binds to ergosterol, an essential component of the fungal cell membrane, resulting in depolarization of the membrane; alterations in cell membrane permeability and leakage of important intracellular components; and cell rupture. This agent may also induce oxidative damage in fungal cells and has been reported to stimulate host immune cells.

ampicillin sodium/sulbactam sodium

A combination formulation of the sodium salts of the antibiotic ampicillin and the beta-lactamase inhibitor sulbactam with antibacterial activity. Ampicillin, a broad-spectrum, semisynthetic penicillin, binds to and inactivates penicillin-binding proteins (PBP) located on the inner membrane of the bacterial cell wall, thereby interfering with the cross-linking of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. As a result, the cell wall is weakened and the cell lyses. The sulbactam component irreversibly binds to bacterial beta-lactamase at or near its active site, thereby interfering with substrate binding and inhibiting bacterial metabolism of penicillin and cephalosporin beta-lactam antibiotics, effectively extending their antibiotic spectrum to include many beta-lactam-resistant bacteria.

Ampligen

(Other name for: rintatolimod)

Amplimexon

(Other name for: imexon)

amrubicin hydrochloride

The hydrochloride salt of a third-generation synthetic 9-amino-anthracycline with antineoplastic activity. Amrubicin intercalates into DNA and inhibits the activity of topoisomerase II, resulting in inhibition of DNA replication, and RNA and protein synthesis, followed by cell growth inhibition and cell death. This agent has demonstrated a higher level of anti-tumor activity than conventional anthracycline drugs without exhibiting any indication of the cumulative cardiac toxicity common to this class of compounds.

Amsa P-D

(Other name for: amsacrine)

amsacrine

An aminoacridine derivative with potential antineoplastic activity. Although its mechanism of action is incompletely defined, amsacrine may intercalate into DNA and inhibit topoisomerase II, resulting in DNA double-strand breaks, arrest of the S/G2 phase of the cell cycle, and cell death. This agent's cytotoxicity is maximal during the S phase of the cell cycle when topoisomerase levels are greatest. In addition, amsacrine may induce transcription of tumor promoter p53 protein and block p53 ubiquitination and proteasomal degradation, resulting in p53-dependent tumor cell apoptosis.

amsilarotene

A retinobenzoic acid with potential antineoplastic activity. Amsilarotene inhibits retinoblastoma-gene product (RB) phosphorylation and increases the presence of 2 cyclin-dependent kinase (CDK) inhibitors, resulting in cell cycle arrest. This agent also causes a cytotoxic decline in cyclin A and thymidylate synthase expression.

amuvatinib

An orally bioavailable synthetic carbothioamide with potential antineoplastic activity. Amuvatinib binds to mutant forms of the stem cell factor receptor (c-Kit; SCFR), inhibiting clinically relevant mutants of this receptor tyrosine kinase that may be associated with resistance to therapy. In addition, amuvatinib inhibits activities of other receptor tyrosine kinases, such as c-Met, Ret oncoprotein, and mutant forms of Flt3 and PDGFR alpha, which are frequently dysregulated in variety of tumors. This agent also suppresses the induction of DNA repair protein Rad51, thereby potentiating the activities of DNA damage-inducing agents. Mutant forms of c-Kit are often associated with tumor chemoresistance.

anakinra

A recombinant human nonglycosylated interleukin-1 (IL-1) receptor antagonist with potential antineoplastic activity. Anakinra binds to the IL-1 receptor, thereby blocking the binding of the IL-1 to and activation of its receptor. Blockade of IL-1 activity may inhibit the cascade of downstream pro-angiogenic factors such as vascular endothelial cell growth factor, tumor necrosis factor-alpha, and IL-6, resulting in inhibition of tumor angiogenesis.

anamorelin hydrochloride

The orally bioavailable hydrochloride salt of a synthetic, small-molecule ghrelin mimetic with appetite-stimulating and anabolic activities. Anamorelin binds to and stimulates the growth hormone secretagogue receptor (GHSR) centrally, thereby mimicking the appetite-stimulating and growth hormone-releasing effects of grhelin. Stimulation of GHSR may also reduce the production of the pro-inflammatory cytokines TNF-alpha and interleukin-6, which may play a direct role in cancer-related loss of appetite.

anastrozole

A nonsteroidal inhibitor of estrogen synthesis that resembles paclitaxel in chemical structure. As a third-generation aromatase inhibitor, anastrozole selectively binds to and reversibly inhibits aromatase, a cytochrome P-450 enzyme complex found in many tissues including those of the premenopausal ovary, liver, and breast; aromatase catalyzes the aromatization of androstenedione and testosterone into estrone and estradiol, the final step in estrogen biosynthesis. In estrogen-dependent breast cancers, anastrozole may inhibit tumor growth.

anaxirone

A synthetic triepoxide alkylating agent with potential antineoplastic activity. Anaxirone alkylates DNA via actual or derived epoxide groups, resulting in inhibition of DNA synthesis. This agent has been shown to exhibit a broad spectrum of antineoplastic activity against experimental tumors, including those resistant to other alkylating agents.

Ancef

(Other name for: cefazolin sodium)

Ancestim

(Other name for: recombinant human stem cell factor)

ancitabine hydrochloride

The hydrochloride salt of a cytarabine congener prodrug with antineoplastic activity. Upon administration, ancitabine is slowly hydrolyzed into cytarabine. Subsequently, cytarabine is converted to the triphosphate form within the cell and then competes with cytidine for incorporation into DNA. Because the arabinose sugar sterically hinders the rotation of the molecule within DNA, DNA replication ceases, specifically during the S phase of the cell cycle. Cytarabine agent also inhibits DNA polymerase, resulting in a decrease in DNA replication and repair. Compared to cytarabine, a more prolonged, consistent cytarabine-mediated therapeutic effect may be achieved with ancitabine because of the slow hydrolytic conversion of ancitabine to cytarabine.

Ancobon

(Other name for: flucytosine)

AndroGel

(Other name for: testosterone gel)

androgen antagonist APC-100

An orally available, vitamin E derivative and androgen receptor (AR) antagonist with potential anti-oxidant, chemopreventative and antineoplastic activity. APC-100 binds to ARs in target tissues thereby inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. By inhibiting the formation of the complex between androgen activated AR- and the AP1 transcription factor JunD, the expression of androgen-responsive genes is blocked. One such gene is spermidine/spermine N1-acetyl transferase gene (SSAT) which is responsible for the breakdown of polyamines, which are produced in high levels by prostatic epithelial cells, into reactive oxygen species (ROS) that cause cellular damage. APC-100 may ultimately lead to an inhibition of growth in both AR-dependent and AR-independent prostate tumor cells.

androgen receptor antagonist ARN-509

A small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes. This ultimately inhibits the expression of genes that regulate prostate cancer cell proliferation and may lead to an inhibition of cell growth in AR-expressing tumor cells.

androgen receptor antisense oligonucleotide EZN-4176

A locked nucleic acid (LNA)-based antisense oligonucleotide targeting the androgen receptor (AR) mRNA, with potential antineoplastic activity. Upon administration, EZN-4176 is hybridized and releases the complementary sequences of AR mRNA, thereby blocking translation of the AR protein and inhibiting AR-induced tumor cell growth and promoting tumor cell apoptosis in AR-overexpressing tumor cells. AR is overexpressed in certain breast and prostate cancers and is involved in tumor cell proliferation and survival. LNAs contain a methylene bridge linking 2'-oxygen and 4'-carbon of ribose sugar rings, thereby increasing their thermal stability and decreasing degradation.

Android-F

(Other name for: fluoxymesterone)

androstane steroid HE3235

An orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agentinhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2.

Aneustat

(Other name for: multifunctional/multitargeted anticancer agent OMN54)

Ang2/VEGF-binding peptides-antibody fusion protein CVX-241

A fusion protein containing angiopoietin-2 (Ang2) and vascular endothelial growth factor (VEGF) derived peptides covalently attached, via a proprietary diketone linker, to a proprietary humanized catalytic aldolase monoclonal antibody, with potential antiangiogenic and antineoplastic activities. The Ang2/VEGF peptide moieties of Ang2/VEGF-binding peptides-antibody fusion protein CVX-241 bind to Ang2 and VEGF receptors, which may inhibit tumor angiogenesis and tumor cell proliferation. The proprietary humanized catalytic IgG1 monoclonal aldolase antibody contains reactive lysine residues in its binding sites, which react covalently with compounds having a diketone function; the Ang2 and VEGFR peptide moieties are then covalently attached to the diketone linkers via a proprietary spacer. Both VEGF and Ang2 are upregulated in a variety of cancer cell types and play a crucial role in angiogenesis. This agent possesses an enhanced half-life compared to the naked peptides.

Angelica sinensis root extract

An herbal extract derived from the root of the plant Angelica sinensis with possible antiinflammatory, antispasmodic, vasodilatory, estrogenic, and antitumor activities. Angelica sinensis contains volatile oils, including safrole, isosafrole, and n-butylphthalide; coumarin derivatives, including psoralens, bergapten, osthol, imperatorin, and oxypeucedanin; and ferulic acid. The coumarin derivatives in this agent may vasodilate and relax smooth muscle and may exhibit additive anticoagulant effects. Ferulic acid, a phenolic phytochemical present in plant cell walls, may neutralize free radicals such as reactive oxygen species.In addition, Angelica sinensis extract has been shown to inhibit the growth and induce apoptosis of glioblastoma mutltiforme brain tumor cells through p53-dependent and p53-independent pathways.

Angiocal

(Other name for: anti-VEGF anticalin PRS-050-PEG40)

Angiocept

(Other name for: pegdinetanib)

angiogenesis inhibitor GT-111

An adenovirus encoding an endothelial cell-specific, murine pre-proendothelin-1 (PPE-1) promoter and a Fas-based chimeric death receptor with potential anti-angiogenic activity. Endothelial cell-specific transcriptional control of the adenoviral vector is achieved by the use of a modified murine PPE-1 promoter that is specifically activated in PPE-1-expressing angiogenic endothelial cells residing in the tumor microvasculature. Subsequently, the Fas-c (Fas-chimeric) death receptor, containing Fas and tumor necrosis factor (TNF) receptor 1 (TNFR1) moieties, is expressed in angiogenic endothelial cells; endothelial cell-specific Fas-mediated apoptosis is initiated by the binding of TNF-alpha, abundant in the tumor microenvironment, to the TNFR1 moiety of the expressed Fas-c death receptor.

angiogenesis inhibitor JI-101

An orally active inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor beta (PDGFRb), and the ephrin B4 receptor B4 (EphB4) with potential antiangiogenic and antineoplastic activities. Angiogenesis inhibitor JI-101 binds to and inhibits VEGFR2, PDGFRb and EphB4, which may inhibit tumor angiogenesis and, so, cellular proliferation in tumor cells overexpressing VEGFR2, PDGFRb and EphB4. The receptor tyrosine kinases VEGFR2, PDGFRb and EphB4 may be overexpressed in a number of different cancer cell types and may play crucial roles in tumor angiogenesis.

angiogenesis/heparanase inhibitor PG545

A synthetic heparan sulfate mimetic with potential anti-angiogenic and antineoplastic activity. PG545 inhibits the cleavage of heparan sulfate from cell surface proteoglycan by heparanase and thus inhibits the neovascularization induced by interaction between heparan sulfate and other extracellular matrix proteins. In this manner, this agent may have the potential to slow the progression of growth of solid tumors.

angiostatin

Encoded by human PLG Gene (Plasminogen Family) and expressed in the kidney, angiostatin is an angiogenesis inhibitor present in plasma and other extracellular fluids that blocks neovascularization and mediates suppression of metastases. Containing at least three kringles, angiostatin is a 38-kD internal (serine protease) proteolytic fragment of plasminogen.

Angiozyme

(Other name for: anti-FLT-1 ribozyme)

anguidine

A trichothecene mycotoxin and potent teratogen. Anguidine inhibits initiation of protein synthesis, resulting in the death of rapidly proliferating cells. Anguidine also has been shown to both potentiate and protect against the cytotoxic effects of other drugs.

anidulafungin

A cyclic lipopeptide echinocandin derivative with antifungal activity. Anidulafungin inhibits 1,3 beta-D-glucan synthase, an enzyme involved in fungal cell wall synthesis, resulting in cell lysis and death. This agent is active against Candida species and Aspergillus.

aniline mustard

An alkylating mustard with antineoplastic activity. Aniline mustard forms covalent linkages with nucleophilic centers, resulting in depurination, base miscoding and strand scission, and crosslinking of DNA strands, all of which contribute to its cytotoxicity.

anlotinib hydrochloride

The hydrochloride salt form of anlotinib, a receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic and anti-angiogenic activities. Upon administration, anlotininib targets multiple RTKs, including vascular endothelial growth factor receptor type 2 (VEGFR2) and type 3 (VEGFR3). This agent may both inhibit angiogenesis and halt tumor cell growth.

Ansaid

(Other name for: flurbiprofen)

Antabuse

(Other name for: disulfiram)

anthracycline analogue GPX-150

A synthetic non-cardiotoxic analogue of the anthracycline antibiotic doxorubicin with potential antineoplastic activity. Anthracycline analogue GPX-150 intercalates DNA and impedes the activity of topoisomerase II, inducing single and double-stranded breaks in DNA; inhibiting DNA replication and/or repair, transcription, and protein synthesis; and activating tumor cell apoptosis.

anti-A33 monoclonal antibody KRN330

A recombinant fully human monoclonal antibody directed against the human A33 antigen, with potential immunomodulatory and antineoplastic activity. Anti-A33 monoclonal antibody KRN330 recognizes and binds to the human A33 antigen, which may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against A33-positive colorectal cancers. A33 antigen, a 43 kDa transmembrane glycoprotein of the immunoglobulin superfamily, is highly and homogenously expressed in 95% of colorectal cancer cancers with only restricted expression in normal colonic mucosa and small bowel epithelia.

anti-A5B1 integrin monoclonal antibody PF-04605412

A monoclonal antibody directed against the human alpha5beta1 integrin with potential antiangiogenic and antineoplastic activities. Anti-alpha5beta1 integrin monoclonal antibody PF-04605412 selectively binds to alpha5beta1 integrin, preventing the binding of integrin ligands. This may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alpha5beta1-expressing tumor cells. Alpha5beta1 integrin, a cell adhesion and signaling receptor, is often overexpressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration.

anti-AGS-16 monoclonal antibody AGS-16M18

A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-16 with potential antineoplastic activity. Anti-AGS-16 monoclonal antibody AGS-16M18 selectively binds to AGS-16, triggering complement-dependent cell lysis (CDCL) and antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells expressing AGS-16. While normally expressed at low levels in the proximal tubules of the kidney, AGS-16 has been found to be overexpressed in more than 95% of kidney and 40% of liver neoplasms.

anti-AGS-5 antibody-drug conjugate ASG-5ME

An antibody drug conjugate (ADC) containing the fully human IgG2k monoclonal antibody targeting an epitope of SLC44A4 (AGS-5) linked, via a valine-citrulline (vc) maleimidocaproyl (mc) linker, to the antimicrotubulin drug monomethyl auristatin E (MMAE), with potential antineoplastic activity. The monoclonal antibody moiety of ASG-5ME selectively binds to AGS-5. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and tumor cell apoptosis. SLC44A4, potentially a sodium-dependent transmembrane transport protein, is overexpressed on more than 80 percent of samples derived from patients with pancreatic, prostate and gastric cancers.

anti-AGS-8 monoclonal antibody AGS-8M4

A humanized monoclonal antibody directed against the activator of g-proteins signaling (AGS) cell surface protein AGS-8 with potential antineoplastic activity. Anti-AGS-8 monoclonal antibody AGS-8M4 selectively binds to AGS-8, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing AGS-8. While normally expressed at low levels in the heart in response to ischemia, AGS-8 has been found to be expressed in more than 70% of ovarian neoplasms.

anti-ALK-1 monoclonal antibody PF-03446962

A fully human, IgG2 monoclonal antibody directed against activin-like receptor kinase 1 (ALK-1) with potential antineoplastic activity. Anti-ALK-1 monoclonal antibody PF-03446962 binds to and neutralizes ALK-1. This may disrupt tumor endothelial cell function and inhibit tumor angiogenesis, eventually leading to an inhibition of tumor cell proliferation. ALK-1, a member of the transforming growth factor beta (TGF-b) type I receptor family, is overexpressed on endothelial cells in a variety of tumor cell types and increases endothelial cell proliferation and migration.

anti-amyloid monoclonal antibody NEOD001

A monoclonal antibody against amyloid with potential use in the treatment of amyloid light chain (AL) and AA amyloidosis. Upon intravenous administration, anti-amyloid monoclonal antibody NEOD001 specifically binds to amyloid fibrils. This prevents the formation of amyloid deposits in certain organs and facilitates their clearance. It also reduces the level of amyloid deposits in organs and prevents organ dysfunction.

anti-ANG2 monoclonal antibody MEDI-3617

A fully human IgG1 monoclonal antibody against angiopoietin 2 (ANG2), with potential antiangiogenic activity. Anti-ANG2 monoclonal antibody MEDI-3617 binds to Ang2 and interferes with the interaction between Ang2 and its receptor TEK tyrosine kinase (Tie2), thereby resulting in the disruption of vascular remodeling. This may inhibit angiogenesis and may eventually lead to an inhibition of tumor cell proliferation.

anti-B4 blocked ricin immunotoxin

An immunotoxin comprised of an anti-B4 (anti-CD19) murine monoclonal antibody linked to the modified plant-derived toxin blocked ricin. The antibody moiety of anti-B4 blocked ricin immunotoxin binds to B lymphocytes that express B4; after internalization of the immunotoxin by the B4-expressing B cell, the ricin moiety cleaves the N-glycosidic bond between the ribose and adenine base at position 4324 in the B lymphocyte 28S ribosomal RNA, resulting in ribosome inactivation, inhibition of protein synthesis, and cell death. "Blocked" ricin is ricin which has been chemically modified such that the lectin binding sites of the B chain (galactose-binding sites) have been blocked by covalent attachment of affinity ligands, leaving the ribosome-inactivating activity of the ricin A chain intact.

anti-B7H1 monoclonal antibody MEDI4736

A monoclonal antibody directed against B7H1 (B7 homolog 1; programmed cell death ligand 1) with potential immunostimulating activity. Upon intravenous administration, MEDI4736 binds to the cell surface antigen B7H1, thereby blocking B7H1 signaling. This may activate the immune system to exert a cytotoxic T-lymphocyte (CTL) response against B7H1-expressing tumor cells. B7H1, a member of the B7 protein superfamily and a negative regulator of cytokine synthesis, is overexpressed on certain tumor cell types.

anti-c-fms monoclonal antibody AMG 820

A fully human IgG2 monoclonal antibody against the colony-stimulating factor-1 (CSF-1 or M-CSF) receptor c-fms (or CSFR1), with potential antineoplastic activity. Upon administration, anti-c-fms monoclonal antibody AMG 820 binds to and blocks c-fms, thereby blocking CSF-1 binding to its receptor and suppressing CSF-1-induced c-fms signaling. This results in the suppression of recruitment and activation of tumor associated macrophages (TAM) within the tumor microenvironment. This eventually leads to a decrease in tumor growth. c-fms, a transmembrane protein belonging to the tyrosine kinase family, is overexpressed in certain tumor cell types and plays an essential role in macrophage differentiation and regulation of cell proliferation. The presence of TAM is correlated with tumor proliferation, invasion and a poor prognosis.

anti-c-Met monoclonal antibody ABT-700

A monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-Met), with potential antineoplastic activity. Anti-c-Met monoclonal antibody ABT-700 binds to c-Met, thereby preventing c-Met binding to its ligand, HGF and the subsequent activation of the HGF/c-Met signaling pathway. This may cause cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.

anti-c-MET monoclonal antibody LY2875358

A humanized IgG4 monoclonal antibody directed against human hepatocyte growth factor receptor (HGFR or c-MET) with potential antineoplastic activity. Anti-c-MET monoclonal antibody LY2875358 binds to c-MET, thereby preventing the binding of HGF to its receptor c-Met and subsequent activation of the HGF/c-Met signaling pathway. This may result in cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in many tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.

anti-CA6-DM4 immunoconjugate SAR566658

An immunoconjugate consisting of a humanized monoclonal antibody against the tumor-associated sialoglycotope CA6 (huDS6) conjugated to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. The anti-CA6 monoclonal antibody moiety of SAR566658 targets and binds to the cell surface antigen CA6. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CA6-expressing tumor cells. The CA6 epitope is found on a variety of solid tumors, including breast, ovarian, cervical, lung and pancreatic tumors.

anti-CCR2 monoclonal antibody MLN1202

A humanized monoclonal antibody directed against the human chemokine receptor 2 (CCR2), with potential antiangiogenic, immunomodulating, antimetastatic, and antineoplastic activities. Anti-CCR2 human monoclonal antibody MLN1202 binds to CCR2 and prevents binding of the endothelium-derived CLL2 (monocyte chemoattractant protein-1 or MCP1) to its receptor CCR2, which may result in inhibition of CCR2 activation and so inhibition of angiogenesis, tumor cell migration, and tumor cell proliferation. In addition, this agent may reduce levels of C-reactive protein (CRP). The G-protein coupled receptor CCR2 is expressed on the surface of monocytes and macrophages, stimulates the migration and infiltration of these cell types, and plays an important role in inflammation, angiogenesis, and tumor cell migration and proliferation.

anti-CD19 antibody-drug conjugate SGN-CD19A

An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the auristatin derivative monomethyl auristatin F (MMAF), with potential antineoplastic activity. Upon administration of anti-CD19 antibody-drug conjugate SGN-CD19A, the antibody moiety targets the cell surface antigen CD19, found on a number of B-cell-derived cancers. Upon antibody/antigen binding and internalization, the immunoconjugate releases MMAF, which binds to tubulin and inhibits its polymerization. Inhibition of tubulin polymerization may result in G2/M phase arrest and tumor cell apoptosis. This causes inhibition of cell growth of CD19-expressing tumor cells. CD19, a B-cell antigen, is overexpressed by a variety of different cancer cell types.

anti-CD19 fully human monoclonal antibody MDX-1342

A fully human anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential antineoplastic activity. Anti-CD19 monoclonal antibody MDX-1342 binds to CD19, depleting and eliminating CD19-expressing B-cells. CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.

anti-CD19 monoclonal antibody DI-B4

A low-fucosylated, humanized, IgG1 isotype, monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody DI-B4 binds to CD19, which may result in a strong antibody-dependent cellular cytotoxicity (ADCC) directed at CD19-expressing B-cells but with minimal complement dependent cytotoxicity. DI-B4 contains low levels of fucose, which contributes to its enhanced ADCC activity. CD19 is a B-cell specific membrane antigen that is widely expressed during B-cell development and in all B-cell lineage malignancies.

anti-CD19 monoclonal antibody MEDI-551

A humanized immunoglobulin IgG1 kappa monoclonal antibody directed against the B-cell-specific membrane protein CD-19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody MEDI-551 binds to CD19, which may result in a cytotoxic T-lymphocyte (CTL) response and antibody-dependent cellular cytotoxicity (ADCC) to CD19-expressing B-cells. The Fc portion of MEDI-551 does not contain a fucose sugar moiety, which may contribute to its enhanced ADCC activity.CD19 is a membrane antigen that is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.

anti-CD19 monoclonal antibody XmAb5574

An Fc engineered, humanized anti-CD19 monoclonal antibody directed against the B-cell-specific membrane protein CD19 with potential immunostimulating and antineoplastic activities. Anti-CD19 monoclonal antibody XmAb5574 targets and binds to CD19, thereby depleting and eliminating CD19-expressing B-cells. The modified Fc region of XmAb5574 increases binding affinity to Fc-gamma receptors of effector cells and thereby enhances antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cell-mediated phagocytosis (ADCP). CD19 is widely expressed during B-cell development, from pro-B-cell to early plasma cell stages.

anti-CD19-CAR retroviral vector-transduced autologous T cells

A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD19 scFv (single chain variable fragment); an extracellular portion of human CD28 and the entire transmembrane and cytoplasmic portion of human CD28; and the cytoplasmic portion of the human TCR-[zeta] molecule with potential immunostimulating and antineoplastic activities. Upon administration, anti-CD19-CAR retroviral vector-transduced autologous T cells may stimulate host cytotoxic T lymphocyte (CTL) and antibody responses against CD19-expressing tumor cells, resulting in tumor cell lysis. CD19 antigen is a B-cell specific cell surface antigen expressed in all B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. CD28 is essential for CD4+ T-cell proliferation, interleukin-2 production, and T-helper type-2 (Th2) development.

anti-CD19-DM4 immunoconjugate SAR3419

An immunoconjugate consisting of an anti-CD19 monoclonal antibody conjugated to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-CD19-DM4 conjugate SAR3419 targets the cell surface antigen CD19, found on a number of B-cell-derived cancers. Upon antibody/antigen binding and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of CD19-expressing tumor cells.

anti-CD19/CD22 bispecific ligand-directed toxin DT2219ARL

An immunotoxin consisting of two scFv ligands recognizing human CD19 and CD22 linked to the first 389 amino acids of diphtheria toxin (DT), DT 390, with potential antineoplastic activity. The VH and VL regions of anti-CD22 (sFv) and anti-CD19 are reversed and linked by an aggregration stabilizing linker (ARL) consisting of a 20 amino acid segment of human muscle aldolase (hma) and an Xho1 -compatible restriction site; the CDR3 region of the VH of anti-CD22 sFv is mutated to enhance its affinity. The anti-CD19 and anti CD-22 portions of the immunotoxin specifically bind to CD19 and CD22 receptors on tumor B cells. Upon internalization, DT catalyzes ADP ribosylation of elongation factor 2 (EF-2) which may result in the irreversible inhibition of protein synthesis and cell death in CD19- and CD22-expressing tumor cells. CD19 and CD22 transmembrane proteins upregulated on malignant B cells.

anti-CD20 monoclonal antibody TL011

A monoclonal antibody directed against human CD20 with potential antineoplastic activity. Anti-CD20 monoclonal antibody TL011 specifically binds to the B cell-specific cell surface antigen CD20 antigen (MS4A1; membrane-spanning 4-domains, subfamily A, member 1), thereby potentially triggering an immune response against CD20-positive B cells, leading to B cell apoptosis. CD20 is a non-glycosylated cell surface phosphoprotein that is exclusively expressed on B cells during most stages of B cell development and is often overexpressed in B-cell malignancies.

anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T lymphocytes

A preparation of autologous blood T-lymphocytes that have been genetically modified to express a chimeric antigen receptor (CAR) consisting of an anti-CD20 scFv (single chain variable fragment); the cytoplasmic portion of the human TCR-[zeta] molecule; and the co-stimulatory molecule 4-1BB (CD137), with potential immunostimulating and antineoplastic activities. Upon transfusion, anti-CD20-CAR-CD3zeta-4-1BB-expressing autologous T-lymphocyte cells direct T-cells to CD20-expressing tumor cells. This results in cytotoxic T lymphocyte (CTL) and antibody responses against CD20-expressing tumor cells, causing tumor cell lysis. The CD20 antigen, a non-glycosylated cell surface phosphoprotein, is a B-cell specific cell surface antigen expressed in B-cell lineage malignancies. CD3 zeta is one of several membrane-bound polypeptides found in the T-cell receptor (TCR)/CD3 complex and regulates the assembly of complete TCR complexes and their expression on the cell surface. The 4-1BB co-stimulatory molecule signaling domain enhances activation and signaling after recognition of CD20; the inclusion of this signaling domain may increase the antitumor activity compared to the inclusion of the CD3-zeta chain alone.

anti-CD200 monoclonal antibody ALXN6000

A humanized monoclonal antibody directed against the human immunosuppressive molecule CD200 (OX-2) with potential immunomodulating and antineoplastic activities. Anti-CD200 monoclonal antibody ALXN6000 binds to CD200, blocking the binding of CD200 to its receptor, CD200R, present on cells of the macrophage lineage; inhibition of CD200 may augment the cytotoxic T-lymphocyte (CTL) mediated immune response against CD200-expressing tumor cells. CD200 is a type 1a transmembrane protein, related to the B7 family of co-stimulatory receptors, and is upregulated on the surface of multiple hematologic malignant cells; this transmembrane protein appears to be involved in the downregulation of a Th1 (helper T cell) immune response.

anti-CD22 monoclonal antibody-MMAE conjugate DCDT2980S

An antibody-drug conjugate (ADC) composed of MCDT2219A , a humanized IgG1 anti-CD22 monoclonal antibody covalently linked, via a protease-cleavable peptide linker, to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule disrupting agent, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DCDT2980S binds to B-cell-specific CD22 receptors and is rapidly internalized, thereby delivering MMAE intracellularly. Upon proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. CD22, a cell surface glycoprotein, is expressed on mature B-cells and on most malignant B-cells.

anti-CD27 monoclonal antibody CDX-1127

A human agonistic monoclonal antibody (MoAb) specific for CD27, with potential immunostimulating and antineoplastic activity. Upon administration of CDX-1127, this MoAb binds to CD27 and may potentiate the immune response by increasing the cytotoxic T-lymphocyte (CTL) response against CD27-expressing tumor cells. This may lead to growth inhibition of CD27-expressing tumor cells. In addition, this agent may increase the proliferation and activation of antigen-specific T lymphocytes upon co-administration of TAA-containing vaccines, such as dendritic cell vaccines. CD27, a co-stimulatory molecule and member of the tumor necrosis factor family overexpressed in certain tumor cell types, is constitutively expressed on mature T-lymphocytes, memory B cells and natural killer cells and plays an important role in NK cell mediated cytolytic activity and T and B lymphocyte proliferation and activation.

anti-CD27L antibody-drug conjugate AMG 172

An immunoconjugate consisting of a human IgG1 monoclonal antibody directed against CD27L conjugated, via a non-cleavable linker, to the cytotoxic agent maytansinoid DM1, with potential antineoplastic activity. The monoclonal antibody moiety of this immunoconjugate binds to CD27L on tumor cell surfaces. After internalization, the DM1 moiety binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting both cell division and proliferation of cancer cells that express CD27L. CD27L, a type II transmembrane protein and member of the tumor necrosis factor family, is a co-stimulatory molecule constitutively expressed on a subset of activated T-cells, B-cells, and dendritic cells, which is overexpressed in certain tumor cell types.

anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1)

A bivalent recombinant fusion protein immunotoxin derived from the anti-CD3 monoclonal antibody UCHT1 with potential antineoplastic activity. Anti-CD3 immunotoxin A-dmDT390-bisFv(UCHT1) consists of 1-390 amino acid residues of chain A diphtheria toxin (DT) joined via a spacer to the Fv fragment of UCHT1, which is connected to a second UCHT1 Fv fragment via a disulfide bond (hence the "bisFv" designation); the addition of the second Fv fragment overcomes the steric hindrance of immunotoxin binding due to the large N-terminal DT domain. Once inside target T cells, the DT moiety catalyzes the transfer of the ADP-ribose moiety of NAD to diphthamide, a posttranslationally modified histidine residue found in elongation factor 2 (EF-2); inactivation of EF-2, disruption of polypeptide chain elongation, and cell death ensue. CD3 is a complex of five cell-surface polypeptides associated with the T cell receptor (TCR) complex.

anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells

Autologous activated T cells that have been coated with bispecific antibodies (BiAb), with potential antineoplastic and immunomodulating activities. In vitro, T cells are activated through exposure to the anti-CD3 murine monoclonal antibody OKT3 and low-dose interleukin 2 (Il-2) for 6-14 days and then armed with anti-CD3 x anti-CD20 bispecific antibody (CD20Bi). Upon administration, anti-CD3 x anti-CD20 bispecific antibody-armed activated T cells (AATC) attach to CD3-expressing T cells and CD20-expressing tumor cells, selectively cross-linking T cells and tumor cells. This may result in the recruitment and activation of cytotoxic T lymphocyte (CTLs), CTL-mediated specific tumor cell lysis, and the secretion of antitumor cytokines and chemokines. CD20, a cell surface phosphoprotein, is found on normal B cells and most B-cell tumors.

anti-CD3/anti-CD20 trifunctional bispecific monoclonal antibody FBTA05

A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. FBTA05 contains two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human CD20, a tumor-associated antigen that is exclusively expressed on B cells during most stages of B-cell development and often overexpressed in B-cell malignancies. In addition, the modified Fc portion of this antibody binds Fc receptors on antigen presenting cells (APCs) such as macrophages and dendritic cells (DCs). FBTA05 brings T cells, CD20-expressing tumor B-cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against CD20-expressing tumor B-cells. Fc-mediated binding of APCs in the tricellular complex potentiates CD20 antigen presentation to T cells and the activation of anti-tumor cytotoxic T cells.

anti-CD30 monoclonal antibody MDX-1401

A fully human, second-generation, nonfucosylated monoclonal antibody directed against the cell surface receptor CD30 with potential immunomodulating and antineoplastic activities. Anti-CD30 monoclonal antibody MDX-1401 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas. Compared to conventional antibodies, deletion of fucose molecules on the antibody backbone, as is done in MDX-1401, may result in an increased affinity for Fc receptors and an enhanced antibody-dependent cellular cytotoxicity (ADCC).

anti-CD30 monoclonal antibody XmAb2513

A humanized monoclonal antibody directed against the cell surface receptor CD30 with potential immunotherapeutic activity. Anti-CD30 monoclonal antibody XmAb2513 specifically binds to the CD30 antigen, which may result in a cytotoxic T lymphocyte (CTL) response against CD30-expressing tumor cells. CD30, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on activated lymphocytes transiently and is constitutively expressed in hematologic malignancies including Hodgkin's disease and some T-cell non-Hodgkin's lymphomas.

anti-CD30/CD16A monoclonal antibody AFM13

A tetravalent bispecific antibody directed against human CD30 and the human low affinity IgG Fc region receptor (FCGR3A; CD16A), with potential immunomodulating and antineoplastic activities. Anti-CD30/CD16A monoclonal antibody AFM13 binds to the CD16A expressed on natural killer (NK) cells with two of its binding sites and to CD30 on CD30-expressing tumor cells with the other two binding sites, thereby selectively cross-linking tumor and NK cells. This may result in NK cell activation, antibody-dependent cellular cytotoxicity (ADCC) and eventually tumor cell lysis. CD30, a cell surface receptor and a member of the tumor necrosis factor (TNF) receptor superfamily, is overexpressed in hematologic malignancies; CD16A is specifically expressed on the surface of NK cells.

anti-CD33 monoclonal antibody-DM4 conjugate AVE9633

An immunoconjugate consisting of the humanized monoclonal antibody huMy9-6 conjugated to the cytotoxic maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody portion of anti-CD33 monoclonal antibody-DM4 conjugate AVE9633 specifically binds to the cell surface antigen CD33 expressed on myeloid leukemia cells; upon internalization, the DM4 moiety is released, binds tubulin, and disrupts microtubule assembly/disassembly dynamics, resulting in the inhibition of cell division and cell growth in myeloid leukemia cells that express CD33. CD33 is expressed on normal non-pluripotent hematopoietic stem cells as well as on myeloid leukemia cells.

anti-CD37 antibody-drug conjugate IMGN529

An immunoconjugate that consists of a humanized IgG1 antibody K7153A against the cell-surface antigen CD37 that is covalently linked via the uncleavable, maleimide-derived thioether-based linker SMCC to the maytansinoid DM1, with potential pro-apoptotic and cytotoxic activities. The antibody moiety of IMGN529 binds to CD37 on tumor B cells and induces an antibody-dependent cell-mediated cytotoxicity (ADCC) and complement-dependent cytotoxicity (CDC), thereby showing pro-apoptotic activity. In addition, after the internalization of this agent and lysosomal degradation, the DM1 moiety binds to tubulin and inhibits tubulin polymerization and microtubule assembly, resulting in a disruption of microtubule activity and cell division, and eventually causing cell death in CD37-positive B cells. CD37, a transmembrane glycoprotein, is overexpressed in B-cell malignancies. Compared to reducible, cleavable linkers, the non-reducible SMCC linker shows increased stability in plasma.

anti-CD37 single-chain polypeptide TRU-016

A recombinant single-chain polypeptide engineered to exhibit the full binding and activity of an anti-CD37 monoclonal antibody with potential immunostimulatory and antineoplastic activities. Anti-CD37 single-chain polypeptide TRU-016 binds to CD37 on B-cells, which may result in antibody-dependent cell-mediated cytotoxicity (ADCC) and apoptosis. CD37 is a transmembrane glycoprotein expressed at high-levels on B cells and to a lesser extent on T cells and myeloid cells. This agent may have a longer half-life in vivo than conventional monoclonal antibodies.

anti-CD38 monoclonal antibody MOR03087

A fully human monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. Anti-CD38 monoclonal antibody MOR03087 specifically binds to CD38 on CD38-positive tumor cells. This may trigger antitumoral antibody-dependent cellular cytotoxicity (ADCC) and may eventually lead to cell lysis in CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.

anti-CD38 monoclonal antibody SAR650984

A humanized IgG1 monoclonal antibody directed against the cell surface glycoprotein CD-38 with potential antineoplastic activity. Anti-CD38 monoclonal antibody SAR650984 specifically binds to CD38 on CD38-positive tumor cells. This may trigger antitumoral antibody-dependent cellular cytotoxicity (ADCC), complement-dependent cytotoxicity (CDC) and apoptosis eventually leading to cell lysis in CD38-expressing tumor cells. CD38, a type II transmembrane glycoprotein, is present on various immune cells and hematologic malignancies, and its expression has been correlated with poor prognosis.

anti-CD40 monoclonal antibody Chi Lob 7/4

An IgG1 chimeric monoclonal antibody agonist of the cell surface receptor CD40 with potential immunostimulatory and antineoplastic activities. Upon intravenous administration, anti-CD40 monoclonal antibody Chi Lob 7/4 binds to CD40 on a variety of immune cell types, triggering the cellular proliferation and activation of antigen-presenting cells (APCs), activating B cells and T cells, and enhancing the immune response; in addition, this agent binds to the CD40 antigen present on the surfaces of some solid tumor cells, resulting in complement-dependent cytotoxicity (CDC) and antibody-dependent cytotoxicity (ADCC) eventually resulting in decreased tumor growth. CD40, a member of the tumor necrosis factor (TNF) receptor superfamily, is expressed on various immune cells, many B-cell malignancies, and many solid tumors, mediating both indirect tumor cell death through the activation of the immune system and direct tumor cell apoptosis.

anti-CD45 monoclonal antibody

A monoclonal antibody directed against the receptor-like leukocyte cell surface glycoprotein CD45 with leukocyte-depleting activity. Upon administration, anti-CD45 monoclonal antibody binds to leukocyte surface-expressed CD45, which may result in the transient depletion of circulating leukocytes including circulating T cell depletion (TCD). CD45, a receptor-like protein-tyrosine phosphatase that consists of several isoforms, is present on all differentiated hematopoietic cells except erythrocytes and plasma cells and is essential for T cell development and lymphocyte activation.

anti-CD45 monoclonal antibody AHN-12

A high affinity IgG1 monoclonal antibody with potential immunotherapeutic activity. Anti-CD45 monoclonal antibody AHN-12 recognizes CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells.

anti-CD45 monoclonal antibody BC8

A murine IgG1 anti-CD45 monoclonal antibody (MoAb) with immunotherapeutic activity. CD45 antigen, a receptor protein-tyrosine phosphatase essential for T cell development and lymphocyte activation, is expressed on virtually all leukocytes. MoAb BC8 has specificity for hematopoietic tissues and may be used in targeted immunotherapy.

anti-CD45 monoclonal antibody BC8-streptavidin conjugate

An immunoconjugate containing a monoclonal antibody directed against the CD45 antigen BC8, conjugated to streptavidin, a nonglycosylated homotetrameric protein that has four high affinity binding sites for biotin. Anti-CD45 BC8 antibody-streptavidin conjugate binds to CD45, a transmembrane protein tyrosine phosphatase that is expressed on the surface of normal and malignant hematopoietic cells. Upon administration of a biotin-based radioconjugate, the biotin moiety of the radioconjugate binds to the streptavidin moiety of anti-CD45 BC8 antibody-streptavidin conjugate and, upon cellular internalization, specifically delivers cytotoxic radiation to CD45-expressing tumor cells.

anti-CD70 antibody-drug conjugate MDX-1203

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody, directed against the extracellular domain of the human CD70 molecule, conjugated to a prodrug of a CC-1065 (rachelmycin) analogue via a stable peptide-based linker, with potential antineoplastic activity. The anti-CD70 antibody moiety of the anti-CD70 antibody-drug conjugate MDX-1203 selectively binds to the extracellular domain of CD70 on tumor cell surfaces. Upon internalization, the prodrug moiety is released and activated and binds to double-stranded B-DNA within the minor groove, thereby alkylating the 3 position of adenine, which may result in the inhibition of cellular proliferation of tumor cells that overexpress CD70. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on the surfaces of various types of cancer cells.The antitumor antibiotic CC-1065, a DNA minor-groove-binding alkylating agent, was originally isolated from the bacterium Streptomyces zelensis.

anti-CD70 monoclonal antibody ARGX-110

A defucosylated, humanized IgG1 monoclonal antibody directed against the extracellular domain of the human CD70 molecule with potential antineoplastic activity. Upon administration, anti-CD70 monoclonal antibody ARGX-110 selectively binds to, and neutralizes the activity of CD70, which may also induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD70-expressing tumor cells. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on a number of solid and hematological tumors. Its overexpression may play an important role in evasion of immune surveillance.

anti-CD70 monoclonal antibody MDX-1411

A glycoengineered, fully humanized IgG1 monoclonal antibody directed against the extracellular domain of the human CD70 molecule with potential antineoplastic activity. Anti-CD70 fully human monoclonal antibody MDX-1411 selectivity binds to the extracellular domain of CD70, which may induce an antibody-dependent cellular cytotoxicity (ADCC) response against CD70-expressing tumor cells. CD70, the ligand for the costimulatory receptor CD27 and a member of the tumor necrosis factor (TNF) family, is found on renal cell carcinoma (RCC) cells among other cancer cell types.

anti-CD79B monoclonal antibody-MMAE conjugate DCDS4501A

An antibody-drug conjugate (ADC) composed of a monoclonal antibody directed against B-cell antigen receptor complex-associated protein beta chain (CD79B) conjugated, via a protease-cleavable peptide linker, to monomethyl auristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. Upon administration, the monoclonal antibody moiety of DCDS4501A selectively binds to CD79B, a protein which is abundantly expressed on the surface of B-cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. CD79B, a component of the B-cell receptor (BCR), plays a key role in B-cell receptor signaling and is expressed on the surface of almost all types of malignant B-cells.

anti-CEA BiTE monoclonal antibody MEDI-565

A recombinant, proprietary bispecific T-cell engagers (BiTE) antibody directed against human carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. Anti-CEA BiTE monoclonal antibody MEDI-565 possesses two antigen-recognition sites, one for CEA and one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR). This bispecific monoclonal antibody brings CEA-expressing tumor cells and cytotoxic T lymphocytes (CTLs) and helper T lymphocytes (HTLs) together, which may result in the CTL- and HTL-mediated cell death of CEA-expressing cells. CEA, a tumor associated antigen, is overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers.

anti-CEA IgCD28TCR-transduced autologous T cells

A population of autologous tumor infiltrating lymphocytes (TIL) transduced with a retroviral vector encoding the chimeric gene IgCD28TCR with potential immunostimulating and antineoplastic activities. The chimeric IgCD28TCR gene consists of portions of CD28, the zeta chain of the T-cell receptor (TCRzeta), and a single chain antibody domain (sFv) specific for the tumor-associated antigen CEA. Upon administration, these gene-modified TIL bind to tumor cells expressing CEA, which may result in activation and proliferation of TIL and an enhanced cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. CEA may be overexpressed in various gastrointestinal and breast cancers. CD28, a T-cell surface-associated co-stimulatory molecule, is required for full T-cell activation, proliferation, and survival; expression of the CD28 fragment in this chimeric gene construct may impede activation-induced cell death (AICD) of TIL.

anti-CEA TCR retroviral vector-transduced autologous lymphocytes

Autologous human peripheral blood lymphocytes (PBLs), transduced with a retroviral vector encoding both the alpha and beta chains of a T cell receptor (TCR) specific for the carcinoembryonic antigen (CEA), with potential immunostimulating and antineoplastic activities. After transduction, expansion in culture, and reintroduction into the patient, anti-CEA TCR retroviral vector-transduced autologous lymphocytes bind to tumor cells expressing CEA, which may result in cytokine expression, activation and proliferation of T-cells, and a specific cytotoxic T-lymphocyte (CTL) response against CEA-expressing tumor cells. The tumor-associated antigen (TAA) CEA is overexpressed by a variety of cancer cell types, including those of the gastrointestinal tract, lung , and breast.

anti-CEA/anti-DTPA-In (F6-734) bispecific antibody

A bispecific monoclonal antibody (BsMAb) consisting of the Fab fragment of an anti-CEA monoclonal antibody (F6) coupled to the Fab fragment of an anti-DTPA-In monoclonal antibody (734) with potential radioimmunotherapeutic activity. In a two-step "pretargeted" radioimmunotherapeutic approach, this BsMAb, localizing to CEA-expressing tumor cells via the F6 Fab fragment, is introduced into patient first, followed by injection of indium 131-radiolabeled DTPA, which is recognized by the 734 Fab fragment of the BsMAb. Accordingly, a potentially lethal dose of indium 131 is delivered specifically to CEA-expressing tumor cells while minimizing radiotoxicity to normal tissues. CEA (carcinoembryonic antigen) is a tumor antigen overexpressed in many cancer types, including gastrointestinal, breast, non-small cell lung, and thyroid cancers. DTPA (diethylenetriaminepentaacetic acid) is a bivalent hapten.

anti-CEA/anti-HSG bispecific monoclonal antibody TF2

A tri-Fab bispecific monoclonal antibody (BiMoAb) divalent for the carcinoembryonic antigen (CEA) and monovalent for histamine-succinyl-glycine (HSG) peptide-hapten. Anti-CEA/anti-HSG bispecific monoclonal antibody TF2 binds to the tumor associated antigen (TAA) CEA on CEA-expressing tumor cells. Subsequently, an HSG peptide-hapten carrying a radionuclide is administered, binding to the anti-HSG binding fragment on the BiMoAb. Depending on the characteristics of the radionuclide used, CEA-expressing tumor cells may then be radioimaged and/or treated radioimmunotherapeutically.

anti-CSF-1R monoclonal antibody IMC-CS4

A monoclonal antibody directed against colony stimulating factor 1 receptor (CSF1R) with potential antineoplastic activity. CSF1R monoclonal antibody IMC-CS4 binds to CSF1R which may trigger antitumoral antibody-dependent cell-mediated cytotoxicity (ADCC) in tumor cells overexpressing CSF1R. CSF1R, also known as macrophage colony-stimulating factor receptor (M-CSFR) and CD115 (cluster of differentiation 115), is a cell-surface receptor for its ligand colony stimulating factor 1 (CSF1); this receptor is overexpressed or mutated in certain tumor cell types and plays major roles in tumor cell proliferation and metastasis.

anti-CTGF monoclonal antibody FG-3019

A human monoclonal antibody targeting connective tissue growth factor (CTGF) with potential anti-fibrotic and antineoplastic activities. FG-3019 binds to CTGF thereby preventing the binding of the ligand to the receptor and subsequent receptor activation. As CTGF enhances the production of collagen and fibronectin, FG-319 may prevent and reverse fibrosis. In addition, FG-3019 may prevent tumor cell proliferation in CTGF-expressing tumor cells. CTGF, a member of the CCN family (CTGF, CYR61/CEF and NOV), is expressed in a variety of tumor cell types and is involved in processes such as cell proliferation, cell migration, cell adhesion, differentiation and angiogenesis.

anti-CTLA-4 mAb RNA-transfected autologous dendritic cell vaccine

An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. Anti-CTLA4 MoAb RNA-transfected autologous DC vaccine is prepared by transfecting DCs with RNAs encoding humanized heavy and light chains of the anti-CTLA4 (cytotoxic T-Lymphocyte-Associated Antigen 4); expression of anti-CTLA4 blocks the inhibitory effect of CTLA4 on the activation of T-lymphocytes. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.

anti-CTLA4 mAb RNA/GITRL RNA-transfected autologous dendritic cell vaccine

An autologous dendritic cell (DC) cancer vaccine with potential immunostimulatory activity. Anti-CTLA4 MoAb RNA/GITRL RNA-transfected DC vaccine is prepared by transfecting DCs with RNAs encoding humanized heavy and light chains of the anti-CTLA4 (cytotoxic T-Lymphocyte-Associated Antigen 4) monoclonal antibody and tumor necrosis factor (ligand) superfamily, member 18 (TNFSF18 or GlTRL); expression of anti-CTLA4 blocks the inhibitory effect of CTLA4 on the activation of T-lymphocytes, while expression of GlTRL modulates T lymphocyte survival in peripheral tissues. Co-vaccination of this vaccine with melanoma antigen specific vaccine may eliminate the adverse effects associated with systemic administration of immune modulators, while also enhancing vaccine-induced immune responses.

anti-CXCR4 monoclonal antibody MDX-1338

An orally bioavailable monoclonal antibody against CXC chemokine receptor 4 (CXCR4) with potential antineoplastic activity. CXCR4 monoclonal antibody MDX-1338 binds to the chemokine receptor CXCR4, preventing the binding of stromal derived factor-1 (SDF-1) to the CXCR4 receptor and subsequent receptor activation, which may result in decreased tumor cell proliferation and migration. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types.

anti-denatured collagen recombinant monoclonal antibody TRC093

A humanized, affinity-matured IgG1k antibody directed against denatured collagens (I-IV) with potential antiangiogenic and antineoplastic activities. Anti-denatured collagen recombinant monoclonal antibody TRC093 binds to multiple epitopes on denatured collagens, inhibiting proteolytic collagen-mediated signaling in the extracellular matrix (ECM) that is important to tumor angiogenesis, tumor growth, and metastasis. The epitopes on denatured collagen bound by this antibody are considered "cryptic" because, in vivo, they are accessible only on the subendothelial basement membrane of tumors or in normal tissues undergoing neovascularization.

anti-DKK-1 monoclonal antibody LY2812176

A human monoclonal antibody directed against the WNT antagonist dickkopf homolog 1 (DKK1), with potential anti-osteolytic activity. Anti-DKK1 monoclonal antibody LY2812176 binds to and inhibits DKK1, thereby restoring signaling through the WNT pathway, which may result in osteoblast differentiation and activation within the bone matrix and the reversal of tumor-induced osteolytic disease. DKK1, overexpressed by myeloma cells, is an inhibitor of the WNT signaling pathway and prevents the mediated formation of bone.

anti-DKK1 monoclonal antibody BHQ880

A humanized monoclonal antibody directed against Wnt antagonist Dickkopf-1 (DKK1) with potential anti-osteolytic activity. Anti-DKK1 monoclonal antibody BHQ880 binds to and inhibits DKK1, enhancing signaling through the Wnt pathway, which may result in osteoblast differentiation and activation within the bone matrix and the reversal of tumor-induced osteolytic disease. DKK! is a potent Wnt signaling pathway antagonist.

anti-DLL4 monoclonal antibody MEDI0639

An immunoglobulin G1 lambda monoclonal antibody directed against the Notch ligand delta-like 4 (DLL4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody MEDI0639 specifically binds to DLL4 and prevents its interaction with Notch receptors, thereby inhibiting Notch-mediated signaling and gene transcription, which may block tumor angiogenesis and eventually the inhibition of tumor cell growth. Activation of Notch receptors by DLL4 stimulates proteolytic cleavage of the Notch intracellular domain (NICD); after cleavage, NICD is translocated to the nucleus and mediates the transcriptional regulation of a variety of genes involved in vascular development. The expression of DLL4 is highly restricted to the vascular endothelium; DLL4/Notch signaling is required for the development of functional tumor blood vessels.

anti-DLL4 monoclonal antibody REGN421

A human monoclonal antibody directed against Delta-like ligand-4 (DLL4) with potential antineoplastic activity. Anti-DLL4 monoclonal antibody REGN421 specifically binds to human DLL4, preventing its binding to Notch receptors and inhibiting Notch signaling, which may result in defective tumor vascularization and, so, the inhibition of tumor cell growth. DLL4 is the only Notch ligand selectively expressed on endothelial cells; DLL4/Notch signaling is required for the development of functional tumor blood vessels.

anti-DR5 agonist monoclonal antibody TRA-8

An agonist mouse monoclonal antibody directed against TRAIL death receptor type 5 (DR5) with potential antineoplastic activity. Anti-DR5 agonist monoclonal antibody TRA-8 binds DR5, which may induce apoptosis in DR5-expressing tumor cells. DR5 is a tumor cell surface ligand that crosslinks with death receptor type 4 (DR4) when bound by TRAIL [Tumor necrosis (TNF)-related apoptosis-inducing ligand], triggering apoptosis via a death receptor signaling pathway. The apoptotic activity of this antibody may not require DR4/DR5 crosslinking.

anti-EGFL7 monoclonal antibody MEGF0444A

A humanized IgG1 monoclonal antibody directed against the epidermal growth factor-like domain multiple 7 (EGFL7) with potential antineoplastic activity. Anti-EGFL7 monoclonal antibody MEGF0444A binds to EGFL7, thereby preventing the activities of EGFL7 on endothelial cells and inhibiting the survival and migration of endothelial cells during angiogenesis. EGFL7, a vascular-restricted extracellular matrix protein that is upregulated during angiogenesis and that regulates vascular development, may be overexpressed on the cell surfaces of various solid tumor cell types.

anti-EGFR monoclonal antibody ABT-806

A humanized monoclonal antibody (MoAb) against human epidermal growth factor receptor (EGFR) with antineoplastic activity. MoAb ABT-806 targets the EGFR deletion variant, de2-7 EGFR as well as wild-type EGFR expressed in cells overexpressing the receptor, thereby preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization result in an inhibition in signal transduction and anti-proliferative effects. This MoAb targets cells expressing aberrant EGFR, hence making it an ideal candidate for generation of radioisotope or toxin conjugates.

anti-EGFR monoclonal antibody mixture MM-151

An oligoclonal therapeutic composed of three fully human monoclonal antibodies targeting epidermal growth factor receptor (EGFR or ErbB1), with potential antineoplastic activity. Upon administration of MM-151, the three antibodies bind to distinct, non-overlapping epitopes of EGFR, thereby preventing the binding of a full range of both high and low affinity EGFR ligands and inhibiting EGFR-ERK-mediated signaling. This eventually inhibits tumor cell proliferation in EGFR-overexpressing tumor cells. Furthermore, multi antibody-antigen bindings cause crosslinking of EGFR and downregulate receptor signalings that are mediated via heterodimerization of EGFR with other members of the EGFR family. EGFR, a receptor tyrosine kinase overexpressed in a variety of cancer cell types, is a key regulator of cancer cell proliferation, apoptosis, invasion, and metastasis.

anti-EGFR monoclonal antibody mixture sym004

A mixture of two recombinant IgG1 antibodies directed against different epitopes in the epidermal growth factor receptor (EGFR) extracellular domain III, with potential antineoplastic activity. Anti-EGFR monoclonal antibody mixture Sym004 binds to the extracellular domain of EGFR, thereby preventing ligand binding. This may prevent activation and subsequent dimerization of the receptor; the decrease in receptor activation may result in an inhibition of downstream ERK and JNK signaling pathways and thus inhibition of EGFR-dependent tumor cell proliferation and metastasis. In addition, binding of Sym004 to EGFRs causes EGFR internalization and degradation. EGFR, a receptor tyrosine kinase, often is overexpressed on the cell surfaces of various solid tumor cell types.

anti-EGFR monoclonal antibody RO5083945

A glycoengineered monoclonal antibody directed against the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. anti-EGFR monoclonal antibody RO5083945 binds to the extracellular domain of EGFR, preventing the activation and subsequent dimerization of the receptor; the decrease in receptor activation and dimerization may result in an inhibition of downstream ERK and JNK signaling pathways and so inhibition of EGFR-dependent tumor cell proliferation and metastasis. EGFR, a member of the epidermal growth factor family of extracellular protein ligands, may be overexpressed on the cell surfaces of various solid tumor cell types.

anti-EGFRvIII antibody drug conjugate AMG 595

An immunoconjugate consisting of a human monoclonal antibody directed against the deletion-mutant of epidermal growth factor receptor, EGFRvIII, conjugated via a non-cleavable linker to the cytotoxic agent maytansinoid DM1, with potential antineoplastic activity. The monoclonal antibody moiety of this immunoconjugate binds to EGFRvIII on tumor cell surfaces. After internalization, the DM1 moiety binds to tubulin, thereby disrupting microtubule assembly/disassembly dynamics and inhibiting cell division and the proliferation of cancer cells that express the EGFRvIII mutant. EGFRvIII, a deletion mutation of exons 2-7 in the epidermal growth factor receptor gene, is overexpressed by a variety of cancers, including glioblastoma multiforme, non-small cell lung carcinoma, and breast carcinoma.

anti-EGFRvIII immunotoxin MR1-1

A recombinant immunotoxin consisting of single-chain variable domain fragment antibody directed against the tumor-specific antigen EGFRvIII (MR1scFv) fused to domains II and III of the Pseudomonas exotoxin (PE38KDEL), with potential antineoplastic activity. Upon administration, the antibody moiety of anti-EGFRvIII immunotoxin MR1-1 binds to EGFRvIII; upon internalization, the exotoxin portion inhibits protein synthesis, resulting in a reduction in tumor cell proliferation of EGFRvIII- expressing tumor cells. EGFRvIII, a type III in-frame deletion mutation of the epidermal growth factor receptor (EGFR) gene, is expressed by a variety of cancers, including glioblastoma multiforme, non-small lung carcinoma, and breast carcinoma. Compared to intact IgG antibodies, single-chain antibodies such as MR1scFv are smaller and may penetrate tumors better. Pseudomonas exotoxin PE38KDEL was modified to remove the natural cell binding domain.

anti-EGP-2 immunotoxin MOC31-PE

An immunotoxin consisting of a monoclonal antibody directed against epithelial glycoprotein-2 (EP-2, or epithelial cell adhesion molecule (EpCAM)) conjugated to the bacterial toxin Pseudomonas exotoxin A (PE) with potential antineoplastic activity. Upon administration of anti-EGP-2 immunotoxin MOC31-PE, the monoclonal antibody moiety targets and binds to EP-2. Upon internalization, the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in EP-2-expressing cells. EP-2, a tumor-associated antigen, is overexpressed in a variety of cancer cell types.

anti-endoglin monoclonal antibody TRC105

A human/murine chimeric monoclonal antibody directed against endoglin (CD105) with potential antiangiogenic and antineoplastic activities. Anti-endoglin monoclonal antibody TRC105 binds to endoglin, which may result in inhibition of tumor angiogenesis and decreased tumor cell proliferation. The glycoprotein endoglin is a transforming growth factor beta-1 (TGF beta-1) accessory receptor that is highly expressed on tumor vessel endothelial cells and appears to be essential for angiogenesis.

anti-endosialin/TEM1 monoclonal antibody MORAb-004

A humanized IgG1 monoclonal antibody directed against human endosialin/TEM1 (tumor endothelial marker;CD248) with potential anti-angiogenic and antineoplastic activities. Anti-endosialin/TEM1 monoclonal antibody MORAb-004 binds to and inhibits the activity of cell surface protein endosialin/TEM1, which may result in the inhibition of angiogenesis, tumor cell proliferation and metastasis. Endosialin/TEM1 plays a key role in angiogenesis and may be overexpressed on tumor stromal cells and endothelial cells.

anti-ENPP3 antibody-drug conjugate AGS-16C3F

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody (AGS-16C) directed to the ectonucleotide pyrophosphatase/phosphodiesterase family member 3 (ENPP3), conjugated via a non-cleavable linker to monomethyl auristatin F (MMAF), an auristatin derivative and a potent microtubule inhibitor, that has potential antineoplastic activity. Upon intravenous administration of ADC AGS-16C3F, the monoclonal antibody moiety of this conjugate selectively binds to ENPP3 then is internalized and undergoes proteolytic cleavage to release MMAF. MMAF binds to and inhibits tubulin polymerization, resulting in G2/M phase arrest and tumor cell apoptosis. While normally expressed at low levels in the proximal tubules of the kidney, the type II transmembrane glycoprotein ENPP3 has been found to be overexpressed in renal neoplasms.

anti-EpCAM antibody fragment -Pseudomonas exotoxin fusion protein

A fusion protein immunotoxin consisting of a humanized, single-chain monoclonal antibody fragment specific for the epithelial cell adhesion molecule (EpCAM) conjugated with a truncated form of Pseudomonas exotoxin A with potential antineoplastic activity. Anti-EpCAM-Pseudomonas-exotoxin fusion protein binds to Ep-CAM-positive tumor cells, thereby delivering the Pseudomonas exotoxin A moiety specifically; the Pseudomonas exotoxin A moiety then inactivates elongation factor 2 (EF-2) through ADP ribosylation, resulting in inhibition of protein synthesis in target cells. EpCAM, a cell surface protein, is expressed by a variety of tumor cells and is frequently found in head and neck cancers.

anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547

An auristatin analogue immunoconjugate directed against Eph receptor A2 (EphA2)-positive cancer cells with potential antineoplastic activity. Anti-EphA2 monoclonal antibody-MMAF immunoconjugate MEDI-547 is generated by conjugating the fully human IgG1 anti-EphA2 monoclonal antibody (1C1) to the small-molecule microtubule inhibitor monomethyl auristatin phenylalanine (MMAF) via the stable linker maleimidocaproyl (mc) (1C1-mcMMAF). The monoclonal antibody moiety of this agent selectively binds to cells expressing the EphA2 receptor. After internalization and enzymatic cleavage of the immunoconjugate within the tumor cell cytosol, free MMAF binds to tubulin and inhibits its polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. The cell-surface receptor EphA2, a member of the ephrin family of receptor tyrosine kinases (RTKs) involved in mammalian development, is overexpressed by a variety of different cancer cell types.

anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111

A bispecific monoclonal antibody directed against the human epidermal growth factor receptors ErbB2 (Her2) and ErbB3 (Her3) with potential antineoplastic activity. The anti-ErB2 targeting arm of anti-ErbB2/anti-ErbB3 bispecific monoclonal antibody MM-111 binds to ErbB2 on tumor cells with high affinity while the anti-Erb3 therapeutic arm binds to ErbB3, which may result in the inhibition of cellular proliferation and differentiation in ErbB2-overexpressing tumor cells via inhibition of ErbB3-dependent signal transduction pathways. ErbB2 and ErB3 are members of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases and are frequently overexpressed in solid tumors.

anti-ErbB3 monoclonal antibody AV-203

A humanized monoclonal antibody (MoAb) directed against the human receptor tyrosine-protein kinase ErbB-3 (HER3) with potential antineoplastic activity. Anti-ErbB3 MoAb AV-203 binds to and inhibits both ligand neuregulin-1 (NRG-1)-dependent and ligand-independent ErbB3 activation, which may result in inhibition of ErbB3-dependent PI3K/Akt signaling and may lead to inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family, is frequently overexpressed in solid tumors and its overexpression generally correlates with poor prognosis and tumor resistance; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do.

anti-ErbB3 monoclonal antibody REGN1400

A human monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) with potential antineoplastic activity. Anti-ErbB3 receptor monoclonal antibody REGN1400 binds to ErbB3 and prevents neuregulin 1 ligand binding to ErbB3, which may result in an inhibition of ErbB3-dependent phosphatidylinositol-3 kinase (PI3K)/Akt signaling. This eventually leads to the inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in a variety of solid tumors and its overexpression generally correlates with poor prognosis and tumor resistance.

anti-ErbB3 receptor monoclonal antibody MM-121

A fully human monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) with potential antineoplastic activity. Anti-ErbB3 receptor monoclonal antibody MM-121 binds to binds to and inhibits ErbB3 activation, which may result in inhibition of ErbB3-dependent PI3K/Akt signaling and so inhibition of cellular proliferation and differentiation. ErbB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in solid tumors, including breast, lung, and colorectal tumors of epithelial origin; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do.

anti-ErbB3/anti-IGF-1R bispecific monoclonal antibody MM-141

A bispecific monoclonal antibody directed against the human epidermal growth factor receptor ErbB3 (Her3) and the human insulin-like growth factor-1 receptor (IGF-1R), with potential antineoplastic activity. The anti-IGF-1R targeting arm of anti-IGF-1R/anti-ErbB3 bispecific monoclonal antibody MM-141 binds to IGF-1R on tumor cells thereby preventing the binding of the natural ligands IGF-1, 2 and heregulin (HRG) to IGF-1R; the anti-ErbB3 therapeutic arm prevents the binding of neuregulin (NRG) to ErbB3. This prevents the activation of the PI3K/AKT signal transduction pathway and may result in both the induction of apoptosis and a decrease in cellular proliferation in IGF-1R and ErbB3-overexpressing tumor cells. IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily, and ErB3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, are frequently overexpressed in solid tumors.

anti-FLT-1 ribozyme

A nuclease-stabilized synthetic ribozyme (ribonucleic acid enzyme) with potential anti-angiogenesis activity. Ribozyme RPI.4610 specifically recognizes the mRNA for FLT1 (vascular endothelial growth factor receptor 1; VEGFR1), and hydrolyzes the mRNA, thereby preventing VEGFR1 proteins from being made. This may prevent VEGF-stimulated angiogenesis in cancerous tissue and metastasis.

anti-FLT3 monoclonal antibody IMC-EB10

A fully human, IgG1 monoclonal antibody directed against the FLT3 tyrosine kinase receptor (CD135) with potential antineoplastic activity. Upon binding to FLT3, anti-FLT3 monoclonal antibody IMC-EB10 blocks FLT3 ligand binding to FLT3 and subsequent FLT3 phosphorylation, which may result in the inhibition of FLT3-mediated signal transduction pathways. In addition, this agent may stimulate an anti-FLT3 antibody-dependent cell-mediated cytotoxicity (ADCC) against FLT3-expressing tumor cells, which may result in the inhibition of cellular proliferation and survival in FLT3-expressing cells. FLT3 (FLK2), a class III tyrosine kinase receptor, is overexpressed or mutated in most B lineage and acute myeloid leukemias.

anti-FOLR1 monoclonal antibody-maytansinoid conjugate IMGN853

An immunoconjugate consisting of the humanized monoclonal antibody M9346A against folate receptor 1 (FOLR1) conjugated, via the disulfide-containing cleavable linker sulfo-SPDB, to the cytotoxic maytansinoid DM4, with potential antineoplastic activity. The anti-FOLR1 monoclonal antibody moiety of IMGN853 targets and binds to the cell surface antigen FOLR1. After antibody-antigen interaction and internalization, the immunoconjugate releases DM4, which binds to tubulin and disrupts microtubule assembly/disassembly dynamics, thereby inhibiting cell division and cell growth of FOLR1-expressing tumor cells. FOLR1, a member of the folate receptor family is overexpressed on a variety of epithelial-derived cancer cells. The sulfo-SPDB linker prevents cleavage in the bloodstream and may improve this agents efficacy in multidrug resistant tumor cells.

anti-ganglioside GM2 monoclonal antibody BIW-8962

A humanized anti-ganglioside GM2 (GM2) monoclonal antibody with potential antineoplastic and immunomodulating activities. Upon administration, anti-ganglioside GM2 monoclonal antibody BIW-8962 may activate an antibody dependent cellular cytotoxicity (ADCC) against GM2-expressing tumor cells. GM2 is a tumor associated antigen (TAA) overexpressed on the surface of many cancer cells, such as multiple myeloma (MM) cells and neuroblastoma cells.

anti-GCC antibody-drug conjugate MLN0264

An antibody-drug conjugate (ADC) containing a monoclonal antibody directed against guanylyl cyclase C (GCC or GUCY2C) conjugated to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. The monoclonal antibody moiety of MLN0264 selectively binds to GCC, a transmembrane receptor normally found on intestinal cells and dopamine neurons in the brain, but is also overexpressed on the surface of gastrointestinal cancers. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis in GCC-expressing tumor cells.

anti-GD2 monoclonal antibody hu14.18K322A

A monoclonal antibody directed against human glycosphingolipid GD2 with potential antineoplastic activity. Upon binding to the GD2 antigen, anti-GD2 monoclonal antibody hu14.18K322A triggers a host immune response against GD2-expressing tumor cells, which may result in tumor cell death. GD2, an O-acetylated disialoganglioside with expression in normal tissues restricted primarily to the cerebellum and peripheral nerves, is commonly expressed at high levels on tumors of neuroectodermal origins such as melanomas and neuroblastomas.

anti-GD2 monoclonal antibody MORAb-028

A human IgM monoclonal antibody directed against disialoganglioside GD2 with potential immunomodulating activity. Upon administration, anti-GD2 monoclonal antibody MORAb-028 may stimulate the immune system to exert a complement-mediated cytotoxic response against GD2-expressing tumor cells. The glycosphingolipid GD2 is a tumor associated antigen (TAA) overexpressed on the surface of many cancer cells.

anti-GnRH vaccine PEP223

A peptide vaccine derived from the synthetic peptide pyroEHWSYGLRPG, corresponding to amino acids 22-31 of mouse gonadotropin releasing hormone (GnRH), with potential immunocastration activity. PEP223 is dimerized and contains a D-lysine (k) substitution at position 6 (pyroEHWSYkLRPG) to increase its immunogenicity. Anti-GnRH vaccine PEP223 may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response against GnRH, neutralizing its activity. In turn, testosterone production and tumor cell growth may be inhibited in testosterone-sensitive tumors.

anti-GPC3 monoclonal antibody GC33

A humanized monoclonal antibody directed against the cell surface oncofetal protein glypican-3 (GPC3) with potential antineoplastic activity. Anti-GPC3 monoclonal antibody GC33 binds to GPC3 and triggers a host immune response against GPC3-expressing tumor cells, which may result in tumor cell death. GPC3, a heparin sulfate proteoglycan, is frequently upregulated in hepatocellular carcinoma and mesoderm-derived organs such as the liver, lungs, and kidney.

anti-GRP78 monoclonal antibody PAT-SM6

A IgM monoclonal antibody (MoAb) against 78-kDa glucose-regulated protein (GRP78; also called BiP or HSPA5), with potential proapoptotic and antineoplastic activities. Upon intravenous administration of the anti-GRP78 monoclonal antibody PAT-SM6, the MoAb strongly binds to GRP78, thereby preventing the activation of multiple GRP78-mediated pathways and blocking the GRP78-induced suppression of apoptotic pathways. This eventually leads to the induction of tumor cell apoptosis and a reduction in tumor cell proliferation. GRP78, the endoplasmic reticulum (ER) chaperone and unfolded protein response (UPR) regulator, is overexpressed on the surface of a variety of cancer cell types; its expression is associated with increased tumor cell survival and proliferation, as well as angiogenesis and resistance to chemotherapy.

anti-HB-EGF monoclonal antibody KHK2866

A proprietary fucose-free monoclonal antibody directed against human heparin-binding EGF-like growth factor (HBEGF) with potential antineoplastic activity. Anti-HB-EGF monoclonal antibody KHK2866 binds to HBEGF, thereby blocking its binding to the EGF receptors. This prevents EGF receptor activation and the subsequent induction of cell growth signaling. HBEGF is mitogenic for fibroblasts and smooth muscle and may be involved in macrophage-mediated cellular proliferation. The fucose-free monoclonal antibodies enhance antigen dependent cellular cytotoxicity (ADCC), and increase binding affinity to the Fc receptor to overcome genetic polymorphism.

anti-HBEGF monoclonal antibody U3-1565

A humanized monoclonal antibody directed against human heparin-binding EGF-like growth factor (HBEGF) with potential antineoplastic activity. Anti-HBEGF monoclonal antibody U3-1565 binds to HBEGF and blocks the binding of HBEGF to the EGF receptors. This prevents EGF receptor activation and the subsequent induction of cell growth signaling. HBEGF is mitogenic for fibroblasts and smooth muscle and may be involved in macrophage-mediated cellular proliferation.

anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes

Autologous human peripheral blood lymphocytes (PBLs) transduced with a retroviral vector encoding an anti-Her-2 (epidermal growth factor receptor 2) chimeric T cell receptor (chimeric antigen receptor or CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous PBLs from a patient with Her-2-positive cancer are pulsed with a retroviral vector that encodes the CAR gene specific for Her-2. After expansion in culture and reintroduction into the patient, anti-Her-2-CAR retroviral vector-transduced autologous peripheral blood lymphocytes, expressing anti-Her-2-CAR on their cell surfaces, bind to Her-2 antigen on tumor cell surfaces; subsequently, Her-2-expressing tumor cells may be lysed. Her-2 (ErbB-2), a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, belongs to the EGFR superfamily and plays key roles in tumor cell proliferation and tumor angiogenesis.

anti-HER2 monoclonal antibody CT-P6

A monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activity. After binding to HER2 on the tumor cell surface, anti-HER2 monoclonal antibody CT-P6 may induce a cytotoxic T-lymphocyte (CTL) as well as an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells that overexpress HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types.

anti-HER2 monoclonal antibody MGAH22

A Fc-domain optimized IgG monoclonal antibody directed against the human epidermal growth factor receptor 2 (HER2) with potential immunomodulating and antineoplastic activities. After binding to HER2 on the tumor cell surface, anti-HER2 monoclonal antibody MGAH22 may induce an antibody-dependent cell-mediated cytotoxicity (ADCC) against tumor cells overexpressing HER2. HER2, a tyrosine kinase receptor, is overexpressed by many cancer cell types. Compared to other anti-HER2 monoclonal antibodies, the Fc domain of MGAH22 is optimized with increased binding to the activating Fcgamma receptor IIIA (CD16A), expressed on cells such as natural killer (NK) cells and macrophages, thereby mediating an enhanced ADCC; the Fc domain also shows decreased binding to the inhibitory Fcgamma receptor IIB (CD32B).

anti-HER2-CAR autologous CMV-specific cytotoxic T lymphocytes

Autologous human cytomegalovirus (CMV)-specific human cytotoxic T lymphocytes (CTLs) transduced with a retroviral vector encoding a human anti-HER2 (epidermal growth factor receptor 2) chimeric T cell receptor (CAR) gene with potential immunostimulatory and antineoplastic activities. Autologous CTLs from a patient with HER2- and CMV-positive glioblastoma multiforme (GBM) are genetically modified to express CAR gene specific for HER2 on their cell surfaces. After expansion in culture and reintroduction into the patient, the anti-HER2-CAR autologous CMV-specific CTLs bind to HER2 antigen on tumor cell surfaces; subsequently, HER2-positive tumor cells and stem cells may be lysed. HER2 (ErbB2), a receptor tyrosine kinase (RTK) overexpressed by a variety of cancer cell types, plays key roles in tumor cell proliferation and tumor angiogenesis. CMV is present in the majority of GBM tumors.

anti-HER3 monoclonal antibody LJM716

A human monoclonal antibody directed against the human epidermal growth factor receptor HER3 (ErbB3) with potential antineoplastic activity. Anti-HER3 monoclonal antibody LJM716 possesses a novel mechanism of action; LJM716 binds to and locks HER3 in the inactive conformation and does not interfere with its interaction with neuregulin (NRG). The inactivated form of HER3 blocks the PI3K/Akt signaling pathway, thereby inhibiting cellular proliferation in HER2 or NRG expressing tumor cells. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in tumors; it has no active kinase domain but is activated through heterodimerization with other members of the EGFR receptor family, such as HER2.

anti-HER3 monoclonal antibody U3-1287

A fully human monoclonal antibody directed against the membrane-bound receptor HER3 (ERBB3) with potential antineoplastic activity. Anti-HER3 monoclonal antibody U3-1287 binds to and inhibits HER3 activation, which may result in inhibition of HER3-dependent PI3K/Akt signaling and so inhibition of cellular proliferation and differentiation. HER3, a member of the epidermal growth factor receptor (EGFR) family of receptor tyrosine kinases, is frequently overexpressed in solid tumors, including breast, lung, and colorectal tumors of epithelial origin; it has no active kinase domain itself but is activated through heterodimerization with other members of the EGFR receptor family that do.

anti-HGF monoclonal antibody TAK-701

A humanized monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Anti-HGF monoclonal antibody TAK-701 binds to the soluble ligand HGF, preventing HGF binding to and activation of the HGF receptor c-Met and so the activation of the c-Met signaling pathway; this may result in the induction of cell death in c-Met-expressing tumor cells. c-Met, a receptor tyrosine kinase overexpressed or mutated in a variety of tumor cell types, plays a key role in cancer cell growth, survival, angiogenesis, invasion, and metastasis.

anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968

A synthetic antisense oligodeoxynucleotide (AS ODN) targeting hypoxia-inducible factor-1alpha (HIF-1alpha) with potential antineoplastic activity. Anti-HIF-1alpha LNA antisense oligonucleotide EZN-2968 hybridizes with HIF-1alpha mRNA and blocks t HIF-1 alpha protein expression, which may result in the inhibition of angiogenesis, the inhibition of tumor cell proliferation, and apoptosis. HIF-1alpha, normally activated in response to hypoxia-induced stress, is a key transcription regulator of a large number of genes important in cellular adaptation to low-oxygen conditions, including angiogenesis, cell proliferation, apoptosis, and cell invasion.

anti-HLA-DR monoclonal antibody IMMU-114

A humanized IgG4 monoclonal antibody that targets the human leukocyte antigen HLA-DR, with potential antineoplastic activity. Upon administration, anti-HLA-DR monoclonal antibody IMMU-114 binds to HLA-DR on HLA-DR-expressing tumor cells and, although the exact mechanism has yet to be fully elucidated, appears to induce hyperactivation of ERK- and JNK-dependent mitogen activated protein kinase signaling pathways. This may lead to mitochondrial membrane depolarization and reactive oxygen species (ROS) generation. This eventually leads to an induction of tumor cell apoptosis and a reduction in tumor cell proliferation. IMMU-14 may be beneficial in the treatment of graft versus host disease (GVHD) as it appears to suppress T-lymphocyte proliferation and natural killer (NK) cell activation. As the Fc region of the orgnial IgG1 MoAb was replaced with the IgG4 isotype, IMMU-114 does not induce a complement cytotoxicity (CDC) or an antibody-dependent cell-mediated cytotoxicity (ADCC) . HLA-DR, a MHC class II molecule, is found on various B-cell hematologic malignancies and in autoimmune diseases as well as on normal cells.

anti-human chorionic gonadotropin vaccine

A peptide vaccine consisting of the whole or partial beta subunit of human chorionic gonadotrophin hormone (hCG), linked to an adjuvant carrier of bacterial or viral origin, with anti-fertility activity. Anti-human chorionic gonadotropin vaccine blocks the activity of hCG which is naturally produced by the trophectoderm of the pre-implantation embryo within a few days of fertilization. hCG is required for the maintenance of the corpus luteum in the ovary thus ensuring its continued production of progesterone, which is required for the successful completion of implantation of the blastocyst. Without progesterone, the corpus luteum regresses, and menstruation is initiated.

anti-human GITR monoclonal antibody TRX518

A humanized, Fc disabled anti-human glucocorticoid-induced tumor necrosis factor receptor (GITR) monoclonal antibody (MoAb) with immunomodulating activity. Anti-human GITR MoAb TRX518 blocks the interaction of GITR, found on multiple types of T cells, with its ligand, thereby inducing both the activation of tumor-antigen-specific T effector cells, as well as abrogating the suppression induced by inappropriately activated T regulatory cells. This agent is shown to act synergistically with chemotherapeutic drugs in multiple cancer models.

anti-human integrin alpha v subunit monoclonal antibody EMD 525797

A humanized monoclonal antibody directed against the human alpha v integrin subunit with potential antiangiogenic and antineoplastic activities. Anti-human integrin alpha v subunit monoclonal antibody EMD 525797, a chimeric antibody which includes the antigen binding sites of the anti-integrin mouse antibody 17E6, binds to and inhibits the activity of alphavbeta3 integrin (vitronectin receptor); this may result in the inhibition of endothelial cell-cell interactions, endothelial cell-matrix interactions, and integrin-mediated tumor angiogenesis and metastasis in alphavbeta3-expressing tumor cells. Alphavbeta3 integrin, a cell adhesion and signaling receptor, is expressed on the surface of tumor vessel endothelial cells and plays a crucial role in endothelial cell adhesion and migration.

anti-ICAM-1 monoclonal antibody BI-505

A fully human IgG1 monoclonal antibody directed against intercellular adhesion molecule-1 (ICAM-1 or CD54), with potential antineoplastic activity. Anti-ICAM-1 monoclonal antibody BI-505 selectively binds to the adhesion protein ICAM-1, which may result in antibody-dependent cellular cytotoxicity (ADCC), hyper-cross-linking-induced apoptosis, and a decrease in cellular proliferation of ICAM-1-expressing tumor cells. ICAM-1, normally expressed on leukocytes and endothelial cells, may be overexpressed in a variety of cancers.

anti-IGF-1 receptor human monoclonal antibody R1507

A recombinant, fully human monoclonal antibody directed against the insulin-like growth factor-1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R human monoclonal antibody R1507 binds to membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the activation of PI3K/AKT signal transduction; downregulation of the PI3K/AKT survival pathway may result in the induction of apoptosis and decreased cellular proliferation. The activation of IGF-1R, a receptor tyrosine kinase of the insulin receptor superfamily, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been implicated in tumorigenesis and metastasis.

anti-IGF-1R monoclonal antibody AVE1642

A humanized monoclonal antibody directed against the human insulin-like growth factor-1 receptor (IGF-1R/CD221) with potential antineoplastic activity. Anti-IGF-1R monoclonal antibody AVE1642 specifically binds to and blocks membrane-bound IGF-1R, preventing the binding of the natural ligand IGF-1 and the subsequent activation of PI3K/AKT signal transduction, which may result in the induction of apoptosis and a decrease in cellular proliferation. Activation of IGF-1R , a receptor tyrosine kinase of the insulin receptor superfamily overexpressed by various cancer cell types, stimulates cell proliferation, promotes angiogenesis, enables oncogenic transformation, and suppresses apoptosis.

anti-IGF-1R recombinant monoclonal antibody BIIB022

A recombinant, human monoclonal antibody directed against the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Anti-IGF-1R recombinant monoclonal antibody BIIB022 binds to membrane-bound IGF-1R, preventing binding of the ligand IGF-1 and the subsequent triggering of the PI3K/Akt signaling pathway; inhibition of this survival signaling pathway may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. The activation of IGF-1R, a tyrosine kinase and a member of the insulin receptor family, stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis; IGF-1R signaling has been highly implicated in tumorigenesis and metastasis.

anti-IGF1/2 monoclonal antibody MEDI-573

A humanized monoclonal antibody directed against insulin-like growth factors 1 and 2 (IGF-1/2) with potential antineoplastic activity. Anti-IGF1/2 monoclonal antibody MEDI-573 inhibits IGF1- and IGF2-stimulated activation of membrane-bound IGF receptors and the subsequent triggering of proliferation and survival signaling pathways. This may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF1/2 ligands stimulate cell proliferation, enable oncogenic transformation, and suppress apoptosis; IGF1/2 signaling has been highly implicated in tumorigenesis and metastasis.

anti-IL-1 alpha monoclonal antibody CA-18C3

A "true human" (cloned from human B lymphocytes) monoclonal antibody directed against interleukin-1 alpha (IL1a) with potential antineoplastic activity. Anti-IL-1 alpha monoclonal antibody CA-18C3 binds to IL1a and may block the activity of IL1a. IL1a, an inflammatory mediator, plays a key role in interleukin-mediated tumor cell activity such as angiogenesis, tissue matrix remodeling, metastasis and tumor cell invasion.

anti-IL-1 alpha monoclonal antibody MABp1

A human IgG1 monoclonal antibody directed against interleukin-1 alpha (IL1a) with potential antineoplastic activity. Anti-IL-1 alpha monoclonal antibody MABp1 binds to IL1a and may prevent IL 1a activity. In addition, this agent may induce antibody-dependent cellular cytotoxicity (ADCC) or complement-mediated killing (CMK). IL 1a, an inflammatory mediator, plays a key role in interleukin-mediated tumor cell activity such as metastasis and tumor cell invasion.

anti-IL-13 humanized monoclonal antibody TNX-650

A humanized monoclonal antibody directed against interleukin-13 (IL-13) with potential antineoplastic activity. Anti-IL-13 humanized monoclonal antibody TNX-650 binds to and blocks the activity of IL-13, which may result in the inhibition of Hodkin lympoma cell proliferation. IL-13 cytokine, an important mediator in allergic inflammation, may be an autocrine growth factor for Hodgkin lymphoma cells.

anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388

An immunoconjugate consisting of an anti-integrin monoclonal antibody covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-integrin monoclonal antibody-DM4 immunoconjugate IMGN388 binds to tumor cell surface integrins; upon internalization, the DM4 moiety is released from the immunoconjugate, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in inhibition of cell division and cell growth of integrin-expressing tumor cells. Integrins, a class of transmembrane cell surface receptors, link the extracellular matrix (ECM) to intracellular signaling pathways that control cell proliferation and differentiation.

anti-interleukin 6 monoclonal antibody ALD518

A humanized monoclonal antibody directed against the pro-inflammatory cytokine interleukin-6 (Il-6) with potential immunomodulating activity. Upon administration, anti-interleukin 6 monoclonal antibody ALD518 binds to and blocks the activity of IL-6, which may mitigate the catabolic effects of IL-6.

anti-KIR monoclonal antibody IHP 2101

A human monoclonal antibody directed against the human inhibitory killer IgG-like receptor (KIR) with potential immunostimulating and antineoplastic activities. Anti-KIR monoclonal antibody IPH 2101 binds to the KIR receptor expressed on human natural killer (NK) cells, which may prevent KIR-mediated inhibition of NK cells and permit NK cell-mediated anti-tumor cytotoxicity. KIRs are surface glycoproteins that bind to major histocompatibility complex (MHC)/human leukocyte antigen (HLA) class I subtypes on target cells; binding of KIRs inhibits NK cell-mediated cytotoxicity.

anti-KIR monoclonal antibody IPH2102

A fully humanized monoclonal antibody against killer-cell immunoglobulin-like receptors (KIR), with potential antineoplastic activity. Upon administration, anti-KIR monoclonal antibody IPH2102 binds to KIR, thereby preventing the binding of KIR ligands to KIR on natural killer (NK) cells. By blocking these inhibitory receptors, NK cells become activated and attack cancer cells leading to tumor cell death. KIR, a member of the immunoglobulin superfamily, is expressed on the surface of NK cells.

anti-LOXL2 monoclonal antibody GS-6634

A humanized monoclonal antibody against lysyl oxidase-like 2 (LOXL2), with potential antineoplastic activity. Anti-LOXL2 monoclonal antibody AB0024 targets and specifically binds to the scavenger receptor cysteine rich domain 4 (SRCR-4) on LOXL2, thereby preventing the crosslinking of collagen and inhibiting the recruitment and activation of fibroblasts. Inhibiting fibroblast activation and the subsequent production of growth factors and chemokines may lead to an inhibition of tumor cell proliferation. LOXL2, a member of the lysyl oxidase (LO) gene family, is an extracellular, copper-dependent enzyme overexpressed in a variety of tumor cell types, and contributes to tumor cell invasion and metastasis.

Anti-M-CSF monoclonal antibody MCS110

A humanized monoclonal antibody directed against macrophage colony-stimulating factor (M-CSF) with potential anti-osteolytic activity. Anti-M-CSF monoclonal antibody MCS110 binds to M-CSF and blocks M-CSF-mediated signaling through the M-CSF receptor CD116 expressed on osteoclasts, which may result in inhibition of M-CSF-induced osteoclast differentiation and so osteoclastic bone resorption. Osteoclasts are derived through the fusion of cells of the monocyte/macrophage lineage. Osteoblasts and stromal cells may react to bone metastases by producing M-CSF and its osteoclastogenic cofactor RANKL (receptor activator of NF-kappaB ligand).

anti-macrophage migration inhibitory factor antibody

A human, recombinant monoclonal antibody (MoAb) against macrophage migration inhibitory factor (MIF), with potential immunomodulating, anti-inflammatory and antineoplastic activities. Upon intravenous administration, the anti-MIF MoAb binds to MIF, blocking its activity and preventing the MIF-mediated secretion of certain cytokines, including interleukin-1 beta and tumor necrosis factor-alpha. This may lead to an inhibition of cancer cell proliferation in MIF-overexpressing tumor cells. MIF, a pro-inflammatory cytokine overexpressed in some cancers, plays a key role in inflammation, immune responses and cancer cell proliferation

anti-mesothelin antibody-drug conjugate BAY 94-9343

A fully human IgG1 monoclonal antibody directed against the cell surface glycoprotein mesothelin and conjugated to the maytansinoid DM4 with potential antineoplastic activity. The monoclonal antibody moiety of anti-mesothelin antibody-drug conjugate BAY 94-9343 targets and binds to the tumor associated antigen mesothelin; upon internalization, the DM4 moiety binds to tubulin and disrupts microtubule assembly/disassembly dynamics, resulting in inhibition of cell division and cell growth of mesothelin-expressing tumor cells. Mesothelin is overexpressed on all mesotheliomas as well as many ovarian and pancreatic cancers while minimally expressed on normal tissue.

anti-mesothelin CIR mRNA-electroporated autologous T cells

Autologous chimeric immune receptor (CIR) T cells transfected with anti-mesothelin chimeric T cell receptor mRNA, with potential antineoplastic activity. The anti-mesothelin mRNA encodes a single chain antibody variable fragment (ScFv), the intracellular CD 3 zeta T cell receptor domain and the 4-1BB (cd137) costimulatory domain. Upon intravenous administration, the anti-mesothelin CIR mRNA-electroporated autologous T cells may attach to cancer cells expressing mesothelin. This may stimulate the secretion of multiple cytokines and may result in cell lysis of mesothelin-expressing cancer cells. Mesothelin is a cell surface glycoprotein involved in cell adhesion and is overexpressed in many epithelial-derived cancers.

anti-MMP-9 monoclonal antibody GS-5745

A humanized monoclonal antibody against matrix metalloproteinase 9 (MMP-9), with potential antineoplastic activity. Upon administration, anti-MMP-9 monoclonal antibody GS-5745 binds to MMP-9 and inhibits its enzymatic activity. This results in an inhibition of extracellular matrix protein degradation and, potentially, the inhibition of angiogenesis, tumor growth, invasion, and metastasis. MMP-9, a protein belonging to the MMP family, plays a key role in the degradation of collagens and proteoglycans; increased activity of MMP-9 has been associated with increased invasion and metastasis of cancer.

anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062

An immunoconjugate consisting of a monoclonal antibody directed against a highly-expressed myleoma cell surface antigen covalently attached to the maytansinoid DM4, a derivative of the cytotoxic agent maytansine (DM1), with potential antineoplastic activity. Anti-myeloma monoclonal antibody-DM4 immunoconjugate BT-062 binds to an unspecified cell surface antigen highly expressed on myeloma cells; upon internaliization the DM4 moiety is released, binding to tubulin and disrupting microtubule assembly/disassembly dynamics, which may result in the inhibition of cell division and cell growth of myeloma tumor cells.

anti-myostatin monoclonal antibody LY2495655

A monoclonal antibody against myostatin (MSTN) with potential anti-cachexia activity. Upon administration, anti-myostatin monoclonal antibody LY2495655 binds to and neutralizes the MSTN protein, thereby blocking the MSTN signalling pathway. This may help decrease muscle protein breakdown and muscle weakness and may attenuate cancer cachexia. MSTN, a member of the transforming growth factor-beta (TGF-beta) superfamily, is a negative regulator of muscle growth and development.

anti-Nectin-4 monoclonal antibody-drug conjugate AGS-22M6E

An antibody drug conjugate (ADC) containing a fully human monoclonal antibody AGS-22 targeting the cell adhesion molecule nectin-4 and conjugated, via a proprietary enzyme-cleavable linker, to the cytotoxic agent monomethyl auristatin E (MMAE) (AGS-22M6E), with potential antineoplastic activity. The monoclonal antibody moiety of AGS-22M6E selectively binds to nectin-4. After internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, which results in G2/M phase arrest and induces apoptosis in nectin-4 overexpressing tumor cells. Nectin-4, a tumor associated antigen belonging to the nectin family, is overexpressed in a variety of cancers, including breast, bladder, lung and pancreatic cancer.

anti-neuropilin-1 monoclonal antibody MNRP1685A

A human IgG1 monoclonal antibody directed against neuropilin-1 (NRP1), with potential antiangiogenic and antineoplastic activities. Upon intravenous administration, MNRP1685A specifically targets and binds to NRP1; the antibody-NRP1 complex prevents the subsequent coupling of NRP1 to VEGFR2, thereby potentially inhibiting VEGF-mediated signaling and potentially preventing angiogenesis. In combination with other anti-VEGF therapies, MNRP1685A may enhance their anti-angiogenic effect. NRP1 is a membrane-bound co-receptor normally expressed by endothelial cells and overexpressed by certain tumor cells, and plays a role in angiogenesis, cell survival, migration, and invasion.

anti-Notch receptor monoclonal antibody OMP-59R5

A monoclonal antibody directed against the Notch receptor with potential antineoplastic activity. Anti-Notch receptor monoclonal antibody OMP-59R5 binds to Notch on the cell surface, thereby inhibiting Notch-mediated signaling and gene transcription, which may impede tumor angiogenesis. Notch receptors are important for cell-cell communication, which involves gene regulation mechanisms that control multiple cell differentiation processes during embryonic and adult life. Dysregulated Notch signaling is implicated in many diseases including T-ALL (T-cell acute lymphoblastic leukemia), CADASIL (cerebral autosomal dominant arteriopathy with sub-cortical infarcts and leukoencephalopathy), MS (multiple sclerosis), and many other disease states.

anti-Notch1 monoclonal antibody OMP-52M51

A humanized monoclonal antibody directed against the Notch-1 receptor with potential antineoplastic activity. Upon administration, anti-Notch1 monoclonal antibody OMP-52M51 binds to Notch-1 on the cell surface, thereby inhibiting Notch-mediated signaling and tumor cell proliferation. Notch 1, a type 1 transmembrane protein belonging to the Notch family, functions as a receptor for membrane bound ligands and has various roles during development; dysregulated Notch signaling is associated with increased cell growth and chemoresistance in cancers.

anti-nucleolin aptamer AS1411

A 26-base guanine-rich oligodeoxynucleotide aptamer with potential apoptotic induction activity. Upon administration, anti-nucleolin aptamer AS1411 targets and binds to nucleolin, a nucleolar phosphoprotein which is overexpressed on the surface of certain cancer cells. Via binding to cell surface nucleolin, AS1411 is internalized and may prevent nucleolin from binding to and stabilizing mRNA of the anti-apoptotic BCL2, thereby destabilizing BCL2 mRNA, leading to a reduction in BCL2 protein synthesis. This may lead to the induction of apoptosis.

anti-OX40 monoclonal antibody

An agonistic monoclonal antibody against receptor OX40 (CD134), with potential immunostimulatory activity. Mimicking the natural OX4 ligand (OX40L), anti-OX40 monoclonal antibody selectively binds to and activates the OX40 receptor. Receptor activation induces proliferation of memory and effector T lymphocytes. In the presence of tumor associated antigens (TAAs), this may promote an immune response against the TAA-expressing tumor cells. OX40, a cell surface glycoprotein and member of the tumor necrosis factor (TNF) receptor family, is expressed by CD4 T cells and provides a costimulatory signal for T cell activation.

anti-p53 T-cell receptor-transduced peripheral blood lymphocytes

Human autologous peripheral blood lymphocytes (PBLs) transduced with an anti-p53 T cell receptor gene with potential antineoplastic activity. PBLs are harvested from a patient and pulsed with a retroviral vector that encodes the T-cell receptor gene specific for a mutated form of p53. The transduced PBLs are then expanded in culture. When reintroduced to the patient, these modified PBLs express the anti-p53 T cell receptor which binds to mutant p53-overexpressing tumor cells; PBL-mediated tumor growth inhibition may follow. Many tumor cell types overexpress mutant p53 proteins, which are associated with the loss of apoptosis regulation and abnormal cell proliferation.

anti-PD-1 fusion protein AMP-224

An Fc-fusion protein containing a ligand of programmed death-1 (PD-1), with potential immunomodulating and antineoplastic activity. Anti-PD-1 fusion protein AMP-224 blocks the interaction between PD-1 and its ligands B7-DC (PD-L2 or programmed cell death-1 ligand 2) and B7-H1 (PD-L1 or CD274 molecule), thereby inhibiting the subsequent activation of PD-1. This may restore immune function and may result in the activation of T-cells and cell-mediated immune responses against tumor cells. PD-1, a transmembrane protein of Ig superfamily, negatively regulates T-cell activation and effector function when activated by its ligands, and plays an important role in tumor evasion from host immunity.

anti-PD-L1 monoclonal antibody MDX-1105

A fully human monoclonal antibody directed against the protein ligand PD-L1 (Programmed Death-1 Ligand 1) with immunomodulating and potential antineoplastic activities. Anti-PD-L1 monoclonal antibody MDX-1105 binds to PD-L1, blocking its binding to and activation of its receptor, PD-1 (Programmed Death 1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation in chronic infectious disease. PD-L1 is expressed broadly on hematopoietic and parenchymal tissues; PD-1, a transmembrane protein, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells.

anti-PD-L1 monoclonal antibody MPDL3280A

A human, Fc optimized, monoclonal antibody directed against the protein ligand PD-L1 (programmed cell death-1 ligand 1) with potential immunomodulating and antineoplastic activities. Anti-PD-L1 monoclonal antibody MPDL3280A binds to PD-L1, blocking its binding to and activation of its receptor, PD-1 (programmed death 1), which may enhance the T-cell-mediated immune response to neoplasms and reverse T-cell inactivation. In addition, by binding to PD-L1, MPDL3280A also prevents binding of this ligand to B7.1. PD-L1 is overexpressed on many human cancer cell types. PD-L1 binding to PD-1 on T-cells suppresses the immune system and results in increased immune evasion. PD-1, a transmembrane protein expressed on activated T-cells, is a negative regulator of the immune system that limits the expansion and survival of CD8+ T cells. The Fc region of MPDL3280A is modified in such a way that it does not induce either antibody-dependent cytotoxicity (ADCC) or complement-dependent cytotoxicity (CDC).

anti-PDGFR alpha monoclonal antibody MEDI-575

A humanized monoclonal antibody directed against the platelet-derived growth factor receptor (PDGFR) alpha with potential antineoplastic activity. Anti-PDGFR alpha monoclonal antibody MEDI-575 inhibits activation of the cell-surface tyrosine kinase PDGFR alpha subunit and subsequent triggering of mitogenic signaling pathways, including the JAK/STAT, PI3K/Akt, and MAP kinase pathways. PDGFR alpha acts as a mitogenic signaling receptor for cells of mesenchymal origin and inhibition of receptor activity may inhibit tumor cell proliferation.

anti-PGF monoclonal antibody RO5323441

A humanized IgG1 monoclonal antibody directed against the placenta growth factor (PGF), with potential anti-angiogenic and antineoplastic activities. Anti-PGF monoclonal antibody RO5323441 binds to both PGF-1 and -2, thereby inhibiting the binding of PGF-1 and -2 to the vascular endothelial growth factor receptor-1 (VEGFR-1) and subsequent VEGFR-1 phosphorylation. This may result in the inhibition of tumor angiogenesis and tumor cell proliferation. PGF, a member of the VEGF sub-family and a key molecule in angiogenesis and vasculogenesis, is upregulated in many cancers.

anti-PKN3 siRNA Atu027

A lipoplexed formulation consisting of short-interfering RNAs (siRNAs) directed against protein kinase N3 (PKN3) encapsulated in catiogenic and fusiogenic lipids with potential antineoplastic activity. Upon administration, catiogenic and fusiogenic lipids promote anti-PKN3 siRNA Atu02 uptake by tumor cells; the siRNAs moieties are subsequently released once inside the cell. The siRNAs bind to PKN3 mRNAs, which may result in the inhibition of translation and expression of the PKN3 protein and, so, growth inhibition of tumor cells that overexpress PKN3. The protein kinase C-related molecule PKN3, downstream in the phosphoinositide-3-kinase (PI3K) signaling pathway, is upregulated in many tumor cells and plays an important role in invasive cell growth and metastasis.

anti-PLGF monoclonal antibody TB-403

A humanized monoclonal antibody directed against placental growth factor (PLGF) with potential anti-angiogenic and antineoplastic acivities. Anti-PLGF monoclonal antibody TB-403 binds to PLGF, inhibiting the binding of PLGF to the vascular endothelial growth factor receptor, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation. PLGF is a protein that belongs to the family of vascular endothelial growth factors (VEGFs).

anti-prolactin receptor antibody LFA102

A neutralizing antibody against the prolactin receptor (PRLR) with potential antineoplastic activity. Upon administration, anti-prolactin receptor antibody LFA102 binds to PRLR and prevents the binding of the peptide hormone prolactin (PRL) to its receptor. This binding induces an antibody-dependent cellular cytotoxicity (ADCC) and may eventually prevent tumor cell proliferation in PRLR-positive cancer cells. PRLR/PRL signaling pathway is frequently overexpressed in breast and prostate cancer.

anti-PSCA fully human monoclonal antibody AGS-1C4D4

An IgG1k fully human monoclonal antibody directed against the human prostate stem cell antigen (PSCA) with potential antineoplastic activity. Anti-PSCA fully human monoclonal antibody AGS-1C4D4 selectively targets and binds to PSCA, triggering complement-dependent cell lysis and antibody-dependent cell-mediated cytotoxicity in tumor cells expressing PSCA. PSCA is a glycosyl-phosphatidylinositol (GPI)-linked cell surface antigen found in cancers of the bladder, pancreas, and prostate.

anti-PSMA monoclonal antibody-MMAE conjugate

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody directed against prostate-specific membrane antigen (PSMA), conjugated via a stable, enzyme-cleavable linker to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. The monoclonal antibody moiety of this conjugate selectively binds to PSMA, a protein which is abundantly expressed on the surface of metastatic and hormone-refractory prostate cancer cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis.

anti-PSMA monoclonal antibody-MMAE conjugate

An antibody-drug conjugate (ADC) containing a fully human monoclonal antibody directed against prostate-specific membrane antigen (PSMA), conjugated via a stable, enzyme-cleavable linker to monomethylauristatin E (MMAE), an auristatin derivative and a potent microtubule inhibitor, with potential antineoplastic activity. The monoclonal antibody moiety of this conjugate selectively binds to PSMA, a protein which is abundantly expressed on the surface of metastatic and hormone-refractory prostate cancer cells. Upon internalization and proteolytic cleavage, MMAE binds to tubulin and inhibits its polymerization, resulting in G2/M phase arrest and tumor cell apoptosis.

anti-PSMA/CD3 BiTE monoclonal antibody MT112

A recombinant T-cell engaging bispecific monoclonal antibody (BiTE) directed against human prostate specific membrane antigen (PSMA) and the CD3 epsilon subunit of the T cell receptor complex, with potential immunostimulating and antineoplastic activities. Anti-PSMA/CD3 BiTE monoclonal antibody MT112 possesses two antigen-recognition sites, one for PSMA, and one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR). This bispecific monoclonal antibody brings PSMA-expressing tumor cells and cytotoxic T lymphocytes (CTLs) together, which may result in the CTL-mediated cell death of PSMA-expressing cells. PSMA, a tumor associated antigen, is overexpressed on the surface of metastatic and hormone-refractory prostate cancer cells.

anti-SEMA4D monoclonal antibody VX15/2503

A humanized IgG4 monoclonal antibody against the semaphorin 4D (SEMA4D; CD100) with potential immunomodulating and antineoplastic activities. Upon administration, anti-SEMA4D monoclonal antibody VX15/2503 binds to and neutralizes SEMA4D, thereby preventing binding of SEMA4D to its receptor plexin-B1 (PLXNB1). By blocking the interaction of SEMA4D and PLXNB1, VX15/2503 may cause an inhibition of endothelial cell activation and migration, eventually leading to an inhibition of angiogenesis and tumor cell proliferation. Semaphorin 4D, a large cell surface antigen found on the resting T-cell and overexpressed in a variety of tumor cell types, plays an important role in vascular growth, tumor progression, invasion and immune cell regulation.

anti-TA-MUC1 monoclonal antibody PankoMab

A humanized monoclonal antibody recognizing the tumor-specific epitope of mucin-1 (TA-MUC1), with potential antineoplastic activity. Anti-TA-MUC1 monoclonal antibody PankoMab targets and binds to the TA-MUC1 epitopes expressed on the cell surface of tumor cells, thereby potentially activating the immune system to induce an antibody-dependent cellular cytotoxicity (ADCC) against the TA-MUC1-expressing tumor cells. TA-MUC1 is designated to MUC1 epitopes with O-glycosylated carbohydrate-induced conformational structures that are tumor-specific, thereby enabling PankoMab to differentiate between tumor MUC1 and non-tumor MUC1 epitopes.

anti-TF monoclonal antibody ALT-836

A recombinant human-mouse chimeric monoclonal antibody against human tissue factor (TF), with potential antiangiogenic, anticoagulant and anti-inflammatory activities. Upon administration, anti-TF monoclonal antibody ALT-836 binds to TF or the TF-Factor VIIa (FVIIa) complex preventing binding and activation of Factor X (FX) and Factor IX (FIX). This may prevent thrombin formation and cancer-associated venous thromboembolism, and may inhibit angiogenesis and tumor cell proliferation. TF, a transmembrane protein and procoagulant, is overexpressed in many tumor cell types, and is correlated with metastasis, angiogenesis, tumor growth and tumor-associated thrombosis.

anti-TGF-beta RII monoclonal antibody IMC-TR1

A monoclonal antibody directed against transforming growth factor-beta receptor type II (TGF-beta RII) with potential antineoplastic activity. Anti-TGF-beta RII monoclonal antibody IMC-TR1 specifically targets and binds to TGF-beta R11, thereby preventing the activation of TGF-beta RII-mediated signaling pathways. TGF-beta RII is mutated in a number of cancer cell types and is involved in cancer cell proliferation and tumor progression.

anti-thymocyte globulin

A purified gamma immunoglobulin (IgG) with immunosuppressive activity. Obtained from rabbits that have been immunized with human thymocytes, antithymocyte globulin specifically recognizes and destroys T lymphocytes. Although the exact mechanism of action is not completely understood, it appears to involve T lymphocyte clearance from the circulation and modulation of T lymphocyte activity. Administering antithymocyte globulin with chemotherapy prior to stem cell transplantation may reduce the risk of graft-versus-host disease.

anti-tissue factor monoclonal antibody MORAb-066

A humanized monoclonal antibody against human tissue factor (TF), with potential antiangiogenic, anticoagulant and anti-inflammatory activities. Upon administration, anti-TF monoclonal antibody MORAb-066 binds to TF and prevents Factor VIIa (FVIIa) from binding, thereby interfering with the activation of Factor X (FX) into FXa. This may prevent thrombin formation and cancer-associated venous thromboembolism, and may inhibit angiogenesis and tumor cell proliferation. TF, a transmembrane protein and initiator of the coagulation cascade, is overexpressed in many tumor cells and tumor endothelial cells; its expression is correlated with metastasis, angiogenesis, tumor cell growth and tumor-associated thrombosis.

anti-TROP-2 antigen antibody-drug conjugate IMMU-132

An antibody-drug conjugate containing the humanized monoclonal antibody, hRS7, against tumor-associated calcium signal transducer 2 (TACSTD2 or TROP2) and linked to the active metabolite of irinotecan, 7-ethyl-10-hydroxycamptothecin (SN-38), with potential antineoplastic activity. The antibody moiety of IMMU-132 selectively binds to TROP2. After internalization and proteolytic cleavage, SN-38 selectively stabilizes topoisomerase I-DNA covalent complexes, resulting in DNA breaks that inhibit DNA replication and trigger apoptosis. TROP2, also known as epithelial glycoprotein-1 (EGP-1), is a transmembrane calcium signal transducer that is overexpressed by a variety of human epithelial carcinomas; this antigen is involved in the regulation of cell-cell adhesion and its expression is associated with increased cancer growth, aggressiveness and metastasis.

anti-TWEAK monoclonal antibody RO5458640

A humanized monoclonal antibody directed against the apoptotic ligand TNF-like weak inducer of apoptosis (TWEAK) with potential antineoplastic activity. Anti-TWEAK monoclonal antibody RO5458640 binds to TWEAK and prevents the binding of TWEAK to its receptor, FGF-inducible molecule 14 (Fn14), thereby blocking the TWEAK/Fn14 signaling. This may prevent tumor cell proliferation, invasion, migration and angiogenesis. TWEAK has pleiotropic effects, mediating proinflammatory and pro-angiogenic activity as well as stimulation of invasion, migration, and survival mediated via its receptor Fn14; Fn14 is expressed at relatively low levels in normal tissues, but is elevated in tumor cells and locally in injured and diseased tissues.

anti-VEGF anticalin PRS-050-PEG40

A pegylated, proprietary lipocalin that targets human vascular endothelial growth factor (VEGF), with potential antineoplastic activity. Pegylated anti-VEGF anticalin PRS-050 specifically targets and binds to VEGF receptor 2 (VEGFR2 or KDR), thereby preventing its activity. This may inhibit angiogenesis and eventually reduce tumor cell growth.

anti-VEGF-C monoclonal antibody VGX-100

A fully human monoclonal antibody directed against the human vascular endothelial growth factor C (VEGFC or Flt4 ligand) with potential antiangiogenic activity. Anti-VEGFC monoclonal antibody VGX-100 specifically binds to and inhibits VEGFC protein, thereby preventing its binding to VEGFR3 (FLT4) or VEGFR2 (KDR or FLK1). This may prevent VEGFC-mediated signaling and may lead to the inhibition of vascular and lymphatic endothelial cell proliferation. The inhibition of tumor angiogenesis and lymphangiogenesis may eventually decrease tumor cell proliferation and prevent metastasis. VEGFC is overexpressed in a variety of cancer cells, and is associated with increased invasiveness and decreased survival.

anti-VEGFR3 monoclonal antibody IMC-3C5

A fully-human monoclonal antibody directed against human vascular endothelial growth factor receptor 3 (VEGFR-3; Flt-4) with antiangiogenic activity. Anti-VEGFR-3 monoclonal antibody IMC-3C5 specifically binds to and inhibits VEGFR-3, which may result in inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. VEGFR-3 plays a critical role in the embryonic vascular system development but is restricted postnatally to endothelial cells of lymphatic vessels and found to be expressed in many solid and hematologic malignancies.

anti-Wnt signaling pathway monoclonal antibody OMP-18R5

A monoclonal antibody directed against the Wnt signaling pathway with potential antineoplastic activity. Anti-Wnt signaling pathway monoclonal antibody OMP-18R5 binds to certain receptors in the Wnt signaling pathway thereby preventing the activation of the Wnt signaling pathway. This may result in an inhibition of cancer stem cell (CSC) activity and a subsequent inhibition of cancer cell proliferation. The Wnt signaling pathway is dysregulated in many cancer cell types and appears to play a major role in CSC regulation and activity; CSC are tumor initiating cells that are able to self-renew and are responsible for tumor growth and resistance.

antiangiogenic drug combination TL-118

A proprietary, oral suspension containing a combination of agents comprised of a nonsteroidal anti-inflammatory agent, an alkylating agent, a histamine H2 antagonist and a sulfonamide with potential anti-angiogenic and antineoplastic activities. Antiangiogenic drug combination TL-118 is administrated as a specific dosing regimen and may result in a synergistic effect and reduce angiogenesis and inhibit tumor cell proliferation.

antibiotic SQ109

An orally available, acid-stable diamine antibiotic, with potential antimicrobial activity against a variety of bacteria including Helicobacter pylori (H. pylori) and Mycobacterium tuberculosis (M. tuberculosis). As an ethambutol analogue with asymmetric structure, SQ109 does not act on the same target as ethambutol. However, this agent interferes with cell wall synthesis, thereby causing weakening of the cell wall and ultimately cell lysis.

antibody-drug conjugate BAY79-4620

A monoclonal antibody (MoAb) directed against the MN protein with potential antineoplastic activity. Upon administration of BAY79-4620, this MoAb may stimulate the immune system to mount a cytotoxic T-lymphocyte (CTL) response and an antibody mediated cellular cytotoxicity (ADCC) against MN-expressing tumor cells. MN, a transmembrane glycoprotein, is expressed in some human carcinomas and appears to be involved in cancer cell proliferation and transformation.

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