A radioconjugate containing the D-galactose analogue 2-deoxy-2-fluoro-D-glucose (FDGal) labeled with the positron-emitting radioactive isotope fluorine F18, used for imaging upon positron emitting tomography (PET). With cell uptake much higher in tumor cells compared to normal cells, the F18 moiety of fluorodeoxygalactose F-18 can be visualized upon PET imaging and this agent can be used as a tracer for the evaluation of galactose tumor uptake and metabolism.
A radiopharmaceutical consisting of an estradiol analogue radiolabeled with the positron-emitting isotope fluorine F 18. F-18 16 alpha-fluoroestradiol is actively taken up in tumor cells expressing the estrogen receptor (ER), allowing visualization of ER-positive tumor cells with positron emiision tomography (PET). Uptake of this agent depends upon the ER status of target tissues.
An amino acid analog radiolabeled with fluorine F 18, a positron emitting isotope, used as a tracer in positron emission tomography (PET). Reflecting the increased amino acid transport capacity of tumor cells, F-18 fluroethyltyrosine (F-18 FET) is actively taken up in tumor cells via amino acid transport system L, but is neither incorporated into proteins nor readily degraded, resulting in high intracellular concentrations of this imaging agent. Radiolableled amino acid-based agents are useful in PET brain tumor imaging because F-18 fluoro-deoxyglucose (F-18 FDG), commonly used in PET tumor imaging, is relatively insensitive for detecting tumors in the brain due the high levels of glycolytic metabolism in the normal cortex and to a lesser extent in white matter.
An immunocytokine of the human monoclonal antibody fragment F16 (scFv) against the extra-domain A1 of tenascin-C fused, via a short 5-amino acid linker, to a recombinant form of the human cytokine interleukin-2 (IL-2) with potential immunostimulating and antineoplastic activities. The monoclonal antibody portion of the F16-IL2 fusion protein binds to tumor cells expressing the tumor associated antigen (TAA) tenascin-C. In turn, the IL-2 moiety of the fusion protein stimulates natural killer (NK) cells, macrophages and neutrophils and induces T-cell antitumor cellular immune responses thereby selectively killing tenascin-C-expressing tumor cells. In addition, F16-IL2 may potentiate the cytotoxicity of other chemotherapeutic agents. Tenascin-C, a glycoprotein of the extracellular matrix, is expressed in many cancer cell types.
A reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential antineoplastic and antithrombotic activities. FVII, a serine protease, becomes activated (FVIIa) upon binding with TF forming the FVIIa/TF complex, which induces intracellular signaling pathways by activating protease activated receptor 2 (PAR-2). Upon subcutaneous administration, factor VIIa inhibitor PCI-27483 selectively inhibits factor FVIIa in the VIIa/TF complex, which may prevent PAR-2 activation and PAR2-mediated signal transduction pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis of TF-overexpressing tumor cells. In addition, this agent inhibits both the extrinsic and intrinsic coagulation cascades, preventing blood clot formation. TF, a blood protein overexpressed on the cell surface of a variety of tumor cell types, may correlate with poor prognosis; PAR-2 (also known as thrombin receptor-like 1) is a G protein-coupled receptor (GPCR) and a protease-activated receptor.
The hydrochloride salt of the nonsteroidal aromatase inhibitor fadrozole with potential antineoplastic activity. Fadrozole specifically inhibits aromatase, blocking the aromatization of androstenedione and testosterone into estrone and estradiol, respectively, the final step in estrogen biosynthesis; the reduction in estrogen levels may inhibit growth in estrogen-dependent cancers. Aromatase, a member of the cytochrome P-450 superfamily, is found in many tissues; overexpression has been linked to the development of preneoplastic and neoplastic changes in breast tissue.
A focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor GSK2256098 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thereby inhibiting tumor cell migration, proliferation and survival, and tumor angiogenesis. The tyrosine kinase FAK is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.
An orally bioavailable small molecule and ATP-competitive focal adhesion kinase (FAK) inhibitor with potential antineoplastic and antiangiogenic activities. FAK inhibitor PF-00562271 inhibits the tyrosine kinase FAK, and to a lesser extent, proline-rich tyrosine kinase (PYK2), which may inhibit tumor cell migration, proliferation, and survival. As FAK is a signal transducer for integrins, inhibition of FAK by this agent may prevent integrin-mediated activation of several downstream signals including ERK, JNK/MAPK and PI3K/Akt. FAK and PYK2, upregulated in many tumor cell types, are involved in tumor cell invasion, migration and proliferation.
An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor PF-04554878 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation and survival. The tyrosine kinase FAK is , a signal transducer for integrins that is upregulated in many tumor cell types and is involved in tumor cell invasion, migration and proliferation.
An orally bioavailable, small-molecule focal adhesion kinase (FAK) inhibitor with potential antiangiogenic and antineoplastic activities. FAK inhibitor VS-6063 inhibits FAK, which may prevent the integrin-mediated activation of several downstream signal transduction pathways, including those involving RAS/MEK/ERK and PI3K/Akt, thus inhibiting tumor cell migration, proliferation, survival, and tumor angiogenesis. The tyrosine kinase FAK, a signal transducer for integrins, is normally activated by binding to integrins in the extracellular matrix (ECM) but may be upregulated and constitutively activated in various tumor cell types.
A cancer vaccine comprised of a recombinant fowlpox viral vector encoding the carcinoembryonic antigen (CEA), MUC-1, a transmembrane glycoprotein secreted by glandular epithelial tissues, and TRICOM, comprised of three co-stimulatory molecule transgenes (B7-1, ICAM-1 and LFA-3). This agent may enhance CEA and MUC-1 presentation to antigen-presenting cells (APC) and may activate a cytotoxic T-cell response against CEA- and MUC-1-expressing tumor cells.
An orally bioavailable receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Famitinib binds to and inhibits several RTKs, dysregulated in a variety of tumors, including stem cell factor receptor (c-Kit; SCFR), vascular endothelial growth factor receptor (VEGFR) 2 and 3, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinases Flt1 and Flt3. Inhibition of these RTKs may result in an inhibition of tumor growth and angiogenesis, and eventually tumor regression in tumor cells overexpressing these RTKs.
A propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli.
A preparation of CD8-positive T cells specific for human fibroblast activating protein (FAP) with potential immunopotentiating activity. T cells have been genetically modified to express a chimeric antigen receptor specific for FAP. Upon infusion, the FAP-specific CD8-positive T cells bind to FAP-expressing tumor cells and exhibit a selective toxicity to tumor cells. This may result in both tumor cell lysis and inhibition of tumor cell growth. FAP, a cell surface glycoprotein, is overexpressed on tumor-associated fibroblasts but minimally expressed on normal, healthy cells.
(Other name for: toremifene)
(Other name for: panobinostat)
A humanized, immunoglobulin G1 monoclonal antibody with potential antitumor activity. Farletuzumab specifically targets at glycoprotein 3 (GP-3), a cell surface antigen that is overexpressed on many epithelial-derived cancer cells. Upon binding to the GP-3 antigen, farletuzumab triggers a host immune response against GP-3 expressing cells resulting in cell lysis.
A recombinant, soluble, hexameric fusion protein consisting of three human Fas ligand (FasL) extracellular domains fused to the dimer-forming collagen domain of human adiponectin with potential pro-apoptotic and antineoplastic activities. Assembled into a soluble hexameric structure mimicking the ligand clustering of endogenous active FasL, Fas receptor agonist APO010 activates the Fas receptor, resulting in caspase-dependent apoptosis in susceptible tumor cell populations. FasL is a transmembrane protein of the tumor necrosis factor (TNF) superfamily and a pro-apoptotic ligand for the death receptor Fas.
(Other name for: tinidazole)
(Other name for: fulvestrant)
An orally-active pyrimidine analogue of an aza-substituted cytidine in which the ribose moiety is replaced by an arabinose sugar. Similar in action to cytarabine, fazarabine is phosphorylated by deoxycytidine kinase to a triphosphate form which competes with thymidine for incorporation into DNA; its incorporation into DNA inhibits DNA synthesis, resulting in tumor cell death and tumor necrosis. The presence of deoxycytidine kinase in a tumor is a determinant of tumor sensitivity to this drug.
An orally available, non-purine inhibitor of xanthine oxidase with uric acid lowering activity. Upon oral administration, febuxostat selectively and noncompetitively inhibits the activity of xanthine oxidase, an enzyme that converts oxypurines, including hypoxanthine and xanthine, into uric acid. By inhibiting xanthine oxidase, uric acid production is reduced and serum uric acid levels are lowered. Febuxostat may provide protection against acute renal failure caused by the excessive release of uric acid that occurs upon massive tumor cell lysis resulting from the treatment of some malignancies.
A chemotherapy regimen consisting of fluorouracil, epirubicin 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)
(Other name for: piroxicam)
(Other name for: letrozole)
(Other name for: conjugated estrogens)
(Other name for: ethinyl estradiol)
A synthetic phenoxy-isobutyric acid derivate and prodrug with antihyperlipidemic activity. Fenofibrate is hydrolyzed in vivo to its active metabolite fenofibric acid that binds to and activates perioxisome proliferator activated receptor alpha (PPARalpha), resulting in the activation of lipoprotein lipase and reduction of the production of apoprotein C-III, an inhibitor of lipoprotein lipase activity. Increased lipolysis and a fall in plasma triglycerides, in turn, leads to the modification of the small, dense low density lipoporotein (LDL) particles into larger particles that are catabolized more rapidly due to a greater affinity for cholesterol receptors. In addition, activation of PPARalpha also increases the synthesis of apoproteins A-I, A-II, and high density lipoprotein (HDL)-cholesterol. Overall, fenofibrate reduces total cholesterol, LDL cholesterol, apolipoprotein B, total triglycerides and triglyceride rich lipoprotein (VLDL) while increasing HDL cholesterol.
An orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties.
An orally bioavailable powder formulation of a synthetic phenylretinamide analogue of retinol with potential chemopreventive and antineoplastic activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types, including those of the colon, breast, prostate, and neuroblastoma. Independent of RAR activation, this agent also modulates gene expression that leads to ceramide-induced, caspase-independent programmed cell death (PCD) via effectors such as ganglioside GD3 and reactive oxygen species (ROS). Compared to the capsule form, the powder contains a mixture of wheat flour, fats, and sugar that may contribute to the enhanced bioavailability of fenretinide.
(Other name for: fenretinide lipid matrix)
A transmucosal formulation consisting of a small, mucoadhesive, bioerodible polymer disc formulated with the citrate salt of fentanyl, a synthetic anilidopiperidine opioid with analgesic activity. Upon application, fentanyl buccal soluble film rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates.
The citrate salt of fentanyl, a synthetic opioid related to the phenylpiperidines with analgesic and anesthetic properties. Fentanyl exerts its analgesic effect by selectively binding to the mu-opioid receptor in the central nervous system (CNS), thereby mimicking the effects of endogenous opiates. Additional pharmacological effects of fentanyl include anxiolysis, euphoria, feelings of relaxation, respiratory depression, constipation, miosis, and cough suppression.
A tablet formulation containing the citrate salt of the synthetic anilidopiperidine opiate fentanyl with analgesic activity. Upon contact with the buccal mucosa, fentanyl citrate buccal tablet rapidly releases fentanyl which is quickly absorbed into the systemic circulation. Fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opioids.
A pectin-based, aqueous nasal spray containing the citrate salt of fentanyl, a synthetic lipophilic phenylpiperidine opioid, with analgesic activity. Fentanyl binds to and stimulates mu-opioid receptors in the central nervous system (CNS), mimicking the analgesic effect of endogenous opiates. Upon intranasal administration of this agent and contact with the nasal mucosa, pectin in low-viscosity aqueous solution gels in the presence of mucosal calcium ions; from this intranasal gel delivery platform, fentanyl is released into the systemic circulation in a relatively rapid but controlled and sustained manner.
A transdermal formulation containing the synthetic phenylpiperidine opioid agonist fentanyl, with analgesic activity. Upon topical administration, fentanyl diffuses from the transdermal patch through the skin, is transported via the systemic circulation, and selectively binds to the mu-receptor in the central nervous system (CNS), mimicking the effects of endogenous opiates. Stimulation of the mu-receptor inhibits adenyl cyclase activity, induces opening of G-protein-coupled inwardly rectifying potassium (GIRK) channels, and blocks the opening of N-type voltage-gated calcium channels, resulting in hyperpolarization and reduced neuronal excitability; in addition, neuronal release of neurotransmitters such as substance P, GABA, dopamine, acetylcholine and noradrenaline may decrease.
A sublingual preparation of a short-acting, synthetic anilidopiperidine opioid with analgesic activity. After rapid sublingual transmucosal absorption, the active ingredient fentanyl selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opiates.
(Other name for: fentanyl citrate buccal tablet)
(Other name for: ferumoxytol)
(Other name for: ferumoxides injectable solution)
A fermented soybean-derived phytochemical beverage with potential antineoplastic activity. Fermented soybean protein beverage is reported to exhibit immunostimulatory, anti-viral, pro-apoptotic, anti-angiogenic, anti-proliferative, and anti-inflammatory activities and to enhance the cytotoxic effects of natural killer (NK) cells. The fermentation process is reported to hydrolyze many soybean proteins into amino acids and nitrogen-rich compounds and to protect and enhance the activities of isoflavones such as genistein, protease inhibitors, saponins, phytosterols, inositol hexaphosphate, and other beneficial dietary nutrients and micronutrients found in soybeans.
An extract of fermented wheat germ containing a concentrated, standardized amount of methoxy-substituted benzoquinones with immunomodulatory and potential antineoplastic activities. Fermented wheat germ extract (FWGE) inhibits the activities of several enzymes involved in de novo nucleic acid synthesis and in supplying the dNTP pool required for DNA replication. This agent also induces caspase-3- mediated inactivation of poly(ADP)ribose polymerase (PARP), a key enzyme in DNA repair that is overexpressed in many cancers; cleavage of PARP prevents DNA repair and induces apoptosis. The benzoquinones may contribute to the immunomodulatory effects of FWGE, down-regulating major histocompatibility complex class I (MHC-1) protein on the surface of cancer cells, allowing natural killer (NK) cell surveillance; and up-regulating the expression of intracellular adhesion molecule 1 (ICAM-1) on tumor endothelial cells.
A parenteral iron solution containing ferric iron complexed with carboxymaltose polymers, used in parenteral iron-replacement therapy. Upon administration, ferric carboxymaltose is removed from plasma by the reticuloendothelial system. Subsequently, ferric iron binds to transferrin or is stored as ferritin. Transferrin-bound iron is transported in the plasma to the liver, spleen and bone marrow, where it is incorporated into hemoglobin, and to muscle, where it is incorporated into myoglobin.
(Other name for: sodium ferric gluconate complex in sucrose)
A sulfate salt of mineral iron formulated for oral administration and used as a dietary supplement, ferrous sulfate is absorbed in the stomach and small intestine and combines with apoferritin to form ferritin, which is stored in the liver, spleen, red bone marrow, and intestinal mucosa. Important in transport of oxygen by hemoglobin to the tissues, iron is also found in myoglobin, transferrin, and ferritin, and is a component of many enzymes such as catalase, peroxidase, and cytochromes.
An injectable, aqueous colloid solution containing a non-stoichiometric magnetite core of superparamagnetic iron oxide (SPIO) coated with dextran administered as a magnetic resonance imaging (MRI) contrast media. Upon intravenous administration, ferumoxides accumulates in phagocytic reticuloendothelial system (RES) cells of the liver (Kupffer cells). When exposed to a strong external magnetic field, ferumoxides exhibits enhanced T2 relaxation, resulting in signal loss in normal tissues (image darkening) on mid T1/T2 or strongly T2-weighted images. Tissues with decreased RES function such as metastases, primary liver cancer, cysts and various benign tumors, adenomas, and hyperplasia, retain their native signal intensity, consequently the contrast between normal tissue (with image darkening) and abnormal tissue is increased.
An orally administered aqueous suspension of silicone-coated,superparamagnetic iron oxide used as a magnetic resonance imaging (MRI) contrast agent. After oral administration, ferumoxsil fills the stomach and intestines. Upon exposure to the strong external magnetic field during MRI, ferumoxsil exhibits strong T1 relaxation properties and a strongly varying local magnetic field; T2 relaxation is enhanced, thereby darkening the contrast agent-containing portion of the gastrointestinal tract. Delineation of the bowel is thus enhanced, distinguishing bowel fromorgans and tissues adjacent to the upper regions of the gastrointestinaltract.
A synthetic ultrasmall superparamagnetic iron oxide composed of dextran-coated iron oxide nanoparticles (also known as 'ultrasmall particulate iron oxides' or USPIO). Ferumoxtran-10, which accumulates in non-cancerous lymphatic tissue, is used as a molecular resonance imaging (MRI) contrast agent.
A superparamagnetic iron oxide nanoparticle coated with a low molecular weight semi-synthetic carbohydrate, polyglucose sorbitol carboxymethyl ether, with potential anti-anemic and imaging properties. After intravenous administration, ferumoxytol replaces iron stores with fewer side effects compared to the use of oral iron. In addition, this agent generates T1 relaxation, producing a magnetic field and enhancing T2 relaxation, thereby darkening contrast media-containing structures in magnetic resonance imaging (MRI). Due to small particle size, ferumoxytol remains in the intravasculature for a prolonged period and so may be used as a blood pool agent.
The fumarate salt form of fesoterodine, a competitive muscarinic receptor antagonist with muscle relaxant and urinary antispasmodic properties. Fesoterodine is rapidly hydrolyzed in vivo into its active metabolite 5-hydroxymethyltolterodine, which binds and inhibits muscarinic receptors on the bladder detrusor muscle, thereby preventing bladder contractions or spasms caused by acetylcholine. This results in the relaxation of bladder smooth muscle and greater bladder capacity, in addition to a reduction in involuntary muscle contractions and involuntary loss of urine. The active metabolite does not interact with alpha-adrenergic, serotonergic, histaminergic and excitatory amino acid receptors and is eliminated via renal excretion.
An orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with potential antineoplastic activity. FGFR inhibitor AZD4547 binds to and inhibits FGFR, which may result in the inhibition of FGFR-related signal transduction pathways, and, so, the inhibition of tumor cell proliferation and tumor cell death. FGFR, up-regulated in many tumor cell types, is a receptor tyrosine kinase essential to tumor cellular proliferation, differentiation and survival.
A soluble fusion protein consisting of the extracellular domain of human fibroblast growth factor receptor 1 (FGFR1) fused to the Fc portion of human immunoglobulin G1 (IgG1) with potential antineoplastic and anti-angiogenic activities. FGFR1 receptor antagonist FP-1039 prevents FGFR ligands, such as FGF1, FGF2, FGF4, from binding to their cognate receptors, thereby inhibiting the activation of the related FGFR tyrosine kinases. Inhibition of FGFR1 by this agent may retard tumor cell proliferation and induce tumor cell death. FP-1039 may also inhibit vascular endothelial growth factor (VEGF)-induced angiogenesis. FGFR1 is a receptor tyrosine kinase upregulated in certain tumor cells and involved in tumor cellular proliferation, differentiation, angiogenesis, and survival; most ligands that bind to FGFR1 also bind tothe related receptors FGFR3 and FGFR4.
A plasma-derived fibrin biomatrix preparation consisting of two separate solutions that are combined on application. The sealer protein solution contains clottable human fibrinogen and bovine aprotinin, a fibrinolysis inhibitor; the thrombin solution contains human thrombin and calcium chloride. When the solutions are combined, a clot is formed, reproducing the final stages of the coagulation cascade.
(Other name for: fibrin sealant)
A monoclonal antibody directed against human hepatocyte growth factor (HGF) with potential antineoplastic activity. Ficlatuzumab binds to the soluble ligand HGF, preventing the binding of HGF to its receptor c-Met and activation of the HGF/c-Met signaling pathway, which 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.
A narrow-spectrum, 18-membered macrolide antibiotic isolated from the actinomycete Dactylosporangium aurantiacum subsp. hamdenensis with potential antibacterial activity. Although the exact mechanism of action has yet to be fully elucidated, fidaxomicin may bind to and inhibit bacterial DNA-dependent RNA polymerase, thereby inhibiting the initiation of bacterial RNA synthesis. When orally administered, this agent is minimally absorbed into the systemic circulation, acting locally in the gastrointestinal tract. Tiacumicin B appears to be active against pathogenic Gram-positive bacteria, such as clostridia, enterococci, and staphylococci, but does not appear to be active against other beneficial intestinal bacteria.
(Other name for: prasterone)
A human monoclonal antibody directed against the insulin-like growth factor type I receptor (IGF1R) with potential antineoplastic activity. Figitumumab selectively binds to IGF1R, preventing insulin-like growth factor type 1 (IGF1) from binding to the receptor and subsequent receptor autophosphorylation. Inhibition of IGF1R autophosphorylation may result in a reduction in receptor expression on tumor cells that express IGF1R, a reduction in the anti-apoptotic effect of IGF, and inhibition of tumor growth. IGF1R is a receptor tyrosine kinase expressed on most tumor cells and is involved in mitogenesis, angiogenesis, and tumor cell survival.
A recombinant, non-glycosylated cytokine which is chemically identical to or similar to the endogenous cytokine human granulocyte colony-stimulating factor (G-CSF) isoform B, with immunomodulating activity. Filgrastim binds to and activates G-CSF receptors with the same biological activity and stability as the endogenous cytokine, thereby controlling the production, differentiation, and function of neutrophilic granulocyte progenitors.
Peripheral blood progenitor cells (PBPC) primed with a recombinant form of the human granulocyte colony-stimulating factor (filgrastim). As a hematopoietic growth factor, filgrastim is able to mobilize hematopoietic progenitor cells (HPCs) into the peripheral blood which allows for an increased number of HPCs upon collection by leukapheresis. Administration of filgrastim-primed PBPCs following hematopoietic stem cell transplantation provides increased numbers of progenitor cells which may prevent pancytopenia and relapse.
A synthetic 4-azasteroid compound. Finasteride competitively binds to and inhibits steroid type II 5-alpha-reductase in the prostate gland, liver, and skin, thereby interfering with the enzymatic conversion of testosterone to 5-dihydrotestosterone (DHT) and reducing serum DHT levels. The reduction in serum DHT levels results in diminished stimulation of androgen receptors in the nuclei of prostate cells and, so, diminished prostate cell proliferation.
An injectable, nutritional lipid emulsion composed of 10% fish oil and high amounts of the fish oil-derived polyunsaturated omega-3 fatty acids eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA). Additionally, the fish oil/glycerol/egg lecithin-based emulsion contains myristic acid, palmitic acid, palmitoleic acid, stearic acid, oleic acid, linoleic acid, linolenic acid, octadecatetraenoic acid, eicosaenoic acid, arachidonic acid, docosaenoic acid, and docosapentaenoic acid. This agent supplies essential fatty acids that can be incorporated into cell membranes. The fatty acids may decrease the production of certain pro-inflammatory cytokines, including interleukin 1 (IL-1), IL-6 and tumor necrosis factor (TNF). In addition to fish oil, this lipid emulsion contains egg phospholipids to maintain membrane integrity; glycerol to provide energy through glycolysis; and the antioxidant alpha-tocopherol (vitamin E).
(Other name for: metronidazole hydrochloride)
A monoclonal antibody directed against the melanosomal membrane protein gp75 (or Tyrosinase-Related Protein 1 [TRP1]) with potential immunostimulatory and antineoplastic activities. Flanvotumab targets and binds to gp75. This may lead to the induction of cytotoxic T cell immune and antibody-mediated immune responses against melanoma cells expressing gp75. gp75, a pigmentation-associated antigen, is expressed in melanosomes of human melanocytes and melanomas.
A synthetic flavonoid with vascular targeting properties. Flavone acetic acid exhibits an antiproliferative effect on endothelial cells as a result of a superoxide-dependent mechanism, which induces changes in permeability of the vasculature of the tumor. This agent may stimulate tumor necrosis and promote shunting of blood flow to viable regions of the tumor, increasing their oxygenation and rendering them more susceptible to the antitumor effects of hyperthermia and ionizing radiation.
A tablet formulation of flavonoids with antioxidant and potential chemopreventive activities. Polyphenolic, soluble plant pigment flavonoids inactivate oxygen radicals, prevent lipid peroxidation, and inhibit DNA oxidation. In vitro, these agents have been shown to increase the rate of apoptosis, and inhibit cell proliferation and angiogenesis. Furthermore, flavonoids can induce conjugating enzymes, such as glutathione transferases and glucuronosyltransferases.
Seed isolated from one of several species of the plant genus Linum. Flaxseed-derived foods, lignans, and essential fatty acids such as alpha-linolenic acid, possess anti-inflammatory, lipid-lowering, antioxidant, and antineoplastic properties.
(Other name for: sodium biphosphate/sodium phosphate oral laxative)
(Other name for: tamsulosin hydrochloride)
(Other name for: fluticasone propionate)
(Other name for: tegafur)
(Other name for: fludrocortisone acetate)
(Other name for: fluticasone propionate)
A fluorinated pyrimidine monophosphate analogue of 5-fluoro-2'-deoxyuridine-5'-phosphate (FUDR-MP) with antineoplastic activity. As an antimetabolite, floxuridine inhibits thymidylate synthetase, resulting in disruption of DNA synthesis and cytotoxicity. This agent is also metabolized to fluorouracil and other metabolites that can be incorporated into RNA and inhibit the utilization of preformed uracil in RNA synthesis.
An orally bioavailable protein tyrosine kinase inhibitor for FMS-related tyrosine kinase 3 (FLT3; STK1) and stem cell factor receptor (SCFR; KIT), with potential antineoplastic activity. FLT3/KIT kinase inhibitor AKN-028 binds to and inhibits both the wild-type and mutated forms of FLT3 and SCFR. This may result in an inhibition of tumor cell proliferation in cancer cell types that overexpress these receptor tyrosine kinases.
A short chain synthetic antigenic peptide (GILGFVFTL) derived from the influenza virus A matrix protein and presented by HLA-A2 major histocompatibility complex (MHC) class I molecules. Flu matrix peptide p58-66 stimulates the lytic functions of cytotoxic T lymphocytes (CTLs), which may result in the eradication of virus-infected or malignant tumor cells.
A radiopharmaceutical compound of a small synthetic cyclic peptide containing an RGD-sequence (Arg-Gly-Asp) labeled with the positron-emitting isotope fluorine F 18 that may be used to selectively image tumor cells and tumor vasculature by PET imaging. The RGD motif of fluciclatide F 18 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and endothelial cells of tumor vasculature. This agent may be of use in visualizing and quantifying the development of tumor vascularity in response to antiangiogenic agents.
A synthetic triazole with antifungal activity. Fluconazole preferentially inhibits fungal cytochrome P-450 sterol C-14 alpha-demethylation, resulting in the accumulation of fungal 14 alpha-methyl sterols, the loss of normal fungal sterols, and fungistatic activity. Mammalian cell demethylation is much less sensitive to fluconazole inhibition.
A pyrimidine compound and a fluorinated cytosine analog exhibiting antifungal activity. After penetration into the fungal cells, flucytosine is deaminated to its active metabolite 5-fluorouracil. 5-fluorouracil replaces uracil during fungal RNA synthesis, thereby inhibiting fungal protein synthesis. In addition, fluorouracil is further metabolized to 5-fluorodeoxyuridylic acid monophosphate, which inhibits thymidylate synthetase, thereby interrupting nucleotide metabolism, DNA synthesis and ultimately protein synthesis.
(Other name for: fludarabine phosphate)
The phosphate salt of a fluorinated nucleotide antimetabolite analog of the antiviral agent vidarabine (ara-A) with antineoplastic activity. Fludarabine phosphate is rapidly dephosphorylated to 2-fluoro-ara-A and then phosphorylated intracellularly by deoxycytidine kinase to the active triphosphate, 2-fluoro-ara-ATP. This metabolite may inhibit DNA polymerase alpha, ribonucleotide reductase and DNA primase, thereby interrupting DNA synthesis and inhibiting tumor cell growth.
A positron-emitting radiopharmaceutical containing radioactive 2-deoxy-2-[18F] fluoro-D-glucose. With similar cell uptake as glucose (high in tumor cells), fludeoxyglucose F 18 is not dephosphorylated and further metabolized.
The acetate salt of a synthetic fluorinated corticosteroid with antiinflammatory and antiallergic activities. As a glucocorticoid-receptor agonist, fludrocortisone binds to cytoplasmic receptors, translocates to the nucleus, and subsequently initiates the transcription of glucocorticoid-responsive genes such as lipocortins to inhibit phospholipase A2 (PLA2). Inhibition of PLA2 activity prevents the release of arachidonic acid, a precursor of eicosanoids such as prostaglandins and leukotrienes; eicosanoids are important mediators in the pro-inflammatory response mechanism. As a mineralocorticoid-receptor agonist, this agent stimulates Na+ reabsorption and water retention and K+ and H+ secretion in the distal tubules and collecting ducts of the kidney.
(Other name for: trivalent live-attenuated influenza vaccine)
A synthetic glucocorticoid and derivative of fluocinolone acetonide with anti-inflammatory and antipruritic activities. Fluocinonide binds the glucocorticoid receptor, followed by translocation of the ligand-receptor complex to the nucleus and transcription activation of genes containing glucocorticoid-responsive elements. Lipocortin-1 is one factor induced by fluocinonide that interacts and inhibits cytosolic phospholipase 2 alpha, thereby preventing phospholipase translocation to the perinuclear membrane and subsequent release and conversion of arachidonic acid to inflammatory prostaglandins. In addition, MAPK phosphatase 1 is induced, thereby preventing the triggering of the MAPK cascade resulting in pro-inflammatory effects via Jun N-terminal kinase and c-Jun. Finally, fluocinonide binds to and inhibits nuclear factor kappa-B directly, resulting in inhibition of cyclooxygenase 2 transcription and subsequent prostaglandin synthesis.
An injectable form of the sodium salt of the fluorophore fluorescein. Fluorescein responds to electromagnetic radiation between the wavelengths of 465-490 nm and fluoresces, emitting light at wavelengths of 520-530 nm that can be detected visually.
(Other name for: fluorescein sodium injection)
A radioconjugate and glutamine analog consisting of the fluorine F 18 labeled 2S, 4R stereoisomer of 4-fluoroglutamine with potential use as a metabolic tracer for tumor imaging. Upon intravenous administration, fluorine F 18 4-L-fluoroglutamine (2S,4R) is preferentially taken up by cancer cells, possibly driven by c-Myc upregulation. Upon positron emission tomography (PET), cancer cells can be imaged. Tumor cells use the amino acid glutamine for nutritional purposes necessary for energy production and growth; as tumor cells proliferate more rapidly than normal healthy cells, glutamine uptake is higher in certain cancer cells.
A radioconjugate consisting of 6-fluorodopamine labeled with fluorine F18 (6-[18F]FDA), with potential diagnostic activity. Upon administration, 6-[18F]FDA is taken up by presynaptic sympathetic nerve endings via the norepinephrine transporter (NET) uptake-1. Once inside, 6-[18F]FDA is rapidly converted by dopamine-beta-hydroxylase into 6-[18F]fluoronorepinephrine (6-[18F]FNE) and stored into neuronal storage vesicles. Upon positron emission tomographic (PET) scanning of the F18, sympathetic innervated regions can be visualized, such as those in pheochromocytoma.
A radioconjugate composed of choline labeled with the positron-emitting isotope fluorine F 18, with potential tumor tracer activity using positron emission tomography (PET). Fluorine F 18 fluorocholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, that is integrated into the cell membrane as part of phosphatidylcholine. Since the proliferation of cancer cells is much higher than normal cells, tumor cells exhibit an increased rate of fluorine F 18 fluorocholine uptake and incorporation, facilitating imaging of the tumor using PET. Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently upregulated in human tumor cells. Choline is essential for the production of phosphatidylcholine, which is an important element of phospholipids in cell membranes.
A triazole containing pentapeptide labeled with the positron-emitting isotope fluorine F 18, used as a tracer for positron emitting tomography (PET) imaging. As a caspase-3 specific substrate, fluorine F 18 CP18 peptide is preferentially taken up by and accumulates in tumor cells with high caspase-3 activity. Upon PET imaging, apoptotic cells can be detected and apoptotic activity can be assessed. Caspase-3 is a cysteine protease that plays a key role in the induction of apoptosis.
A radioconjugate comprised of the synthetic pyrimidine analogue 1-(2'-deoxy-2'-fluoro-beta-D-arabinofuranosyl)thymine (d-FMAU) labeled with the radioisotope fluorine F 18 (18F-d-FMAU), that can potentially be used as an imaging agent upon positron emission tomography (PET). Upon administration, fluorine F 18 d-FMAU is distributed and taken up by cells based on the rate of the cells DNA synthesis. Upon PET imaging, cell proliferation in tumors can be assessed as tumor cells have a higher rate of DNA synthesis than normal, healthy cells. This agent is not catabolized and has a long half-life compared to the radioconjugate carbon C 11 thymidine.
A radioconjugate containing a low molecular weight tracer, DCFBC, specific for prostate-specific membrane antigen (PSMA) and labeled with the positron-emitting isotope fluorine F 18 with potential prostate tumor imaging upon positron emission tomography (PET). Upon administration, the DCFBC moiety of fluorine F 18 DCFBC specifically targets and binds to the tumor associated antigen PSMA, thereby allowing the visualization of tumor cells expressing PSMA upon PET. PSMA is a transmembrane glycoprotein highly expressed on malignant prostate epithelial cells and vascular endothelial cells of various solid tumors.
A radioconjugate consisting of EF5, a fluorinated derivative of etanidazole, conjugated to fluorine F 18, a positron emitting isotope. EF5 binds to hypoxic tissue; conjugation to Fluorine F 18 allows imaging of hypoxic regions within tumors.
The anilinoquinazoline derivative FEQA radiolabeled with the positron-emitting radioisotope fluorine F 18 with epidermal growth factor receptor (EGFR) binding and radioisotopic activities. Fluorine F 18 FEQA irreversibly binds to (EGFR), allowing imaging of EGFR-positive tumor cells with positron emission tomography (PET).
A radiotracer containing a synthetic amino acid analogue of L-leucine radiolabeled with fluorine F 18 with potential diagnostic imaging use. Similar to most amino acids, fluorine F 18 fluciclovine (FACBC) appears to enter cells through the energy-independent L-type amino acid transporter (LAT) system. As an amino acid analogue, this agent is preferentially accumulated by tumor cells due to their increased metabolic needs; however, unlike naturally occuring amino acids, this non-natural amino acid-analogue radiotracer is not metabolized. Accordingly, FACBC accumulates in tumor cells and can potentially be used to image tumors using positron emission tomography (PET).
The progesterone derivative fluoro furanyl norprogesterone (FFNP), radiolabeled with fluorine F 18, with positron-emitting radioligand activity. Upon injection, fluorine F 18 fluoro furanyl norprogesterone (F18-FFNP) binds to progesterone receptors (PgR) in progesterone-responsive tissues. In PgR-positive breast cancer, positron emission tomography (PET) may then be used to quantitate hormone receptor status.
A radioconjugate containing the tracer PEG6-IPQA labeled with fluorine F 18 for potential tumor imaging using positron emission tomography (PET). Upon administration, the IPQA moiety of fluorine F 18 fluoro-PEG6-IPQA selectively targets and irreversibly binds to the constitutively active mutant L858R of epidermal growth factor receptor (EGFR) kinase, thereby allowing the visualization of tumor cells expressing the active mutant L858R EGFR using PET. This can be used to select EGFR kinase inhibitors that bind in a similar manner as this tracer and may allow individualized therapy for patients that respond well to these types of EGFR kinase inhibitors. The presence of the L858R EGFR mutation in non-small cell lung cancer (NSCLC) cells is correlated with a better response to EGFR kinase inhibitors compared to wild-type (WT) or L858R/T790M EGFR dual-mutant.
The amino acid analog fluorodopa (FDOPA) labeled with fluorine F 18, a positron-emitting isotope, with potential tumor tracer property. Fluorine F 18 fluorodopa is able to cross the blood-brain barrier and is taken up by brain tumor cells. As uptake is higher in tumor cells, tumors may then be imaged using positron emission tomography (PET). Assessing tumor uptake of FDOPA may be beneficial for diagnosis, localization and in determining further treatment.
Ethylcholine labeled with fluorine F 18, a positron-emitting isotope. Fluorine F 18 fluoroethylcholine incorporates into tumor cells through an active, carrier-mediated transport mechanism for choline and then is phosphorylated intracellularly by choline kinase, yielding a phosphoryl derivative, and finally is integrated into cellular phospholipids, probably primarily into a phosphatidyl derivative; concentration of this agent in tumor cells as various fluorine F 18 fluoroethylcholine derivatives enables tumor imaging using positron emission tomography (PET). Choline kinase, the enzyme responsible for the phosphorylation of choline, is frequently up-regulated in human tumor cell lines.
A radiotracer containing paclitaxel labeled with the radioisotope fluorine F 18 with potential use as an imaging agent. After cellular uptake, the paclitaxel moiety of fluorine F18 fluoropaclitaxel binds to tubulin. Upon uptake, the radioisotope moiety may be detected using positron emission tomography (PET), thereby allowing imaging and quantification of the biodistribution of paclitaxel. This could identify multidrug resistant (MDR) status of tumor cells and select patients that will likely respond to paclitaxel treatment.
A radioconjugate consisting of a thymidine analogue radiolabeled with fluorine F 18, a positron emitting isotope. Phosphorylated by S-phase-specific thymidine kinase 1, fluorine F 18 fluorothymidine is trapped intracellularly by entering the salvage pathway of DNA synthesis without incorporation into DNA. 18F-FLT serves a marker of tumor cell proliferation for imaging with positron emission tomography (PET); as a marker of proliferation rather than metabolism, it is more specific to tumor tissue than 2-deoxy-2-[18F] fluoro-D-glucose (18F-FDG). This agent is metabolically stable, accumulates in the normal bone marrow and the liver, and does not cross the blood-brain barrier.
A radioconjugate containing a derivative of the androgen testosterone (FMDHT) and labeled with the radioisotope fluorine F 18, with potential use as an imaging agent for positron emission tomography (PET). Upon administration, fluorine F 18 FMDHT binds to the androgen receptor (AR). Upon PET imaging, AR-expressing prostate tumor cells can be imaged and assessed.
A radioconjugate consisting of the benzamide ligand ISO-1 labeled with the radioisotope fluorine F18 with positron-emitting radioisotope activity. Upon administration, fluorine [F18]ISO-1 binds to sigma-2 receptors, located on tumor cells, allowing visualization of sigma-2 receptor-expressing tumor cells with positron emission tomography (PET). Sigma-2 receptors, expressed in a variety of normal healthy tissues such as liver, kidneys, endocrine glands, and in the central nervous system, may be overexpressed in tumor cells.
A small synthetic peptide containing an RGD-sequence (Arg-Gly-Asp) attached to the positron-emitting isotope fluorine F 18 that may be used to selectively image tumor cells and tumor vasculature by PET imaging. The RGD motif of fluorine F 18 RGD-based integrin peptide-polymer AH111585 selectively binds to the alphaVbeta3 integrin receptor, commonly upregulated on the surfaces of tumor cells and tumor vasculature endothelial cells. This agent may be of use in visualizing and quantifying a decrease in tumor vascularity in response to antiangiogenic agents.
A radiotracer composed of a cyclic triazole-containing the Arg-Gly-Asp (RGD) peptide (RGD-K5) radiolabeled with fluorine F 18, with potential alphaVbeta3 integrin imaging activity upon positron emission topography (PET). Upon administration, the RGD moiety of fluorine F 18 RGD-K5 selectively binds to alphaVbeta3 integrin. During PET, alphaVbeta3-expressing tumor cells can be visualized and the degree of tumor angiogenesis can be determined. AlphaVbeta3 integrin, a cell adhesion and signaling receptor, is upregulated in tumor vessel endothelial cells and has been associated with neovascularization, differentiation, proliferation of tumor cells, and metastasis.
A radiopharmaceutical consisting of the sodium salt of fluorine F 18 fluoride with radioisotopic and bone mineralizing activities. Fluoride binds to calcium ions in hydroxyapatite crystals in bone. The uptake and incorporation of positron-emitting fluorine F 18 fluoride into bone can be imaged using positron emission tomography (PET) or single-photon emission computed tomography (SPECT), allowing visualization of malignant bone lesions in which regional blood flow and bone turnover are increased.
The hydrochloride salt form of a radioconjugate composed of a synthetic derivative of the amino acid methionine radiolabeled with fluoride F 18, with potential use as a tumor imaging agent during positron emission tomography (PET). Upon administration, fluorine F 18-labeled S-(3-fluoropropyl) homocysteine is preferentially taken up by tumor cells through an amino acid transporter, which is overexpressed by cancer cells. Because tumor cells have a higher rate of proliferation than normal cells, these cancer cells have increased rates of protein synthesis and thus an increased demand for amino acids. This allows for visualization of tumors cells upon PET.
(Other name for: tegafur)
(Other name for: fluorouracil)
An antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine with antineoplastic activity. Fluorouracil and its metabolites possess a number of different mechanisms of action. In vivo, fluoruracil is converted to the active metabolite 5-fluoroxyuridine monophosphate (F-UMP); replacing uracil, F-UMP incorporates into RNA and inhibits RNA processing, thereby inhibiting cell growth. Another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (F-dUMP), inhibits thymidylate synthase, resulting in the depletion of thymidine triphosphate (TTP), one of the four nucleotide triphosphates used in the in vivo synthesis of DNA. Other fluorouracil metabolites incorporate into both RNA and DNA; incorporation into RNA results in major effects on both RNA processing and functions.
An implant containing a sustained release particle of fluorouracil, an antimetabolite fluoropyrimidine analog of the nucleoside pyrimidine, with antineoplastic activity. Upon implantation and subsequent release, fluorouracil is converted into the active metabolite 5-fluoroxyuridine monophosphate that competes with the pyrimidine uracil during RNA synthesis while another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate, inhibits thymidylate synthase and thus DNA synthesis.
An injectable collagen matrix gel containing the antimetabolite fluorouracil and the sympathicomimetic agent epinephrine with potential antineoplastic activity. After intratumoral injection, fluorouracil is converted into the active metabolite 5-fluoroxyuridine monophosphate that competes with uracil during RNA synthesis while another active metabolite, 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate, inhibits thymidylate synthase and, so, DNA synthesis. Epinephrine, a potent vasoconstrictor, is added to the gel to enhance penetration of fluorouracil into tumor tissue and reduce dispersion to surrounding tissues, thus enhancing the local concentration of fluorouracil. Compared to systemic administration, the intratumoral injection of fluorouracil combined with epinephrine may increase fluorouracil's chemotherapeutic efficacy while minimizing systemic toxicity.
A halogenated derivative of 17-alpha-methyltestosterone. Similar to testosterone, fluoxymesterone binds to and activates specific nuclear receptors, resulting in an increase in protein anabolism, a decrease in amino acid catabolism, and retention of nitrogen, potassium, and phosphorus. This agent also may competitively inhibit prolactin receptors and estrogen receptors, thereby inhibiting the growth of hormone-dependent tumor lines. Fluoxymesterone is approximately five times more potent than methyltestosterone.
The hydrochloride salt of fluphenazine, a phenothiazine with antipsychotic activity and potential antineoplastic activity. Fluphenazine blocks postsynaptic dopamine D2 receptors in the limbic system, cortical system and basal ganglia, resulting a reduction of schizophrenia-associated hallucinations and delusions. In addition, as a serotonin antagonist, this agent may inhibit lymphocyte and myeloma cell proliferation by blocking 5-hydroxytrptamine type 1B (5-HT type 1B) receptors for serotonin.
A derivative of propionic acid, and a phenylalkanoic acid derivative of non-steroidal antiinflammatory drugs (NSAIDs) with analgesic, antiinflammatory and antipyretic effects. Flurbiprofen non-selectively binds to and inhibits cyclooxygenase (COX). This results in a reduction of arachidonic acid conversion into prostaglandins that are involved in the regulation of pain, inflammation and fever. This NSAID also inhibits carbonic anhydrase, thereby reducing the production of hydrogen and bicarbonate ions. Upon ocular administration, flurbiprofen may reduce bicarbonate ion concentrations leading to a decrease in the production of aqueous humor, thereby lowering intraocular pressure.
(Other name for: tarenflurbil)
(Other name for: trivalent influenza vaccine)
A toluidine derivative and nonsteroidal antiandrogen that is structurally related to bicalutamide and nilutamide. Flutamide and its more potent active metabolite 2-hydroxyflutamide competitively block dihydrotestosterone binding at androgen receptors, forming inactive complexes which cannot translocate into the cell nucleus. Formation of inactive receptors inhibits androgen-dependent DNA and protein synthesis, resulting in tumor cell growth arrest or transient tumor regression.
The propionate salt form of fluticasone, a synthetic trifluorinated glucocorticoid receptor agonist with antiallergic, antiinflammatory and antipruritic effects. Binding and activation of the glucocorticoid receptor results in the activation of lipocortin that in turn inhibits cytosolic phospholipase A2, which triggers cascade of reactions involved in synthesis of inflammatory mediators, such as prostaglandins and leukotrienes. Secondly, mitogen-activated protein kinase (MAPK) phosphatase 1 is induced, thereby leads to dephosphorylation and inactivation of Jun N-terminal kinase directly inhibiting c-Jun mediated transcription. Finally, transcriptional activity of nuclear factor (NF)-kappa-B is blocked, thereby inhibits the transcription of cyclooxygenase 2, which is essential for prostaglandin production.
The sodium salt of a synthetic lipid-lowering agent with potential antineoplastic activity. Fluvastatin competitively inhibits hepatic 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyzes the conversion of HMG-CoA to mevalonate, a key step in cholesterol synthesis. This agent lowers plasma cholesterol and lipoprotein levels, and modulates immune responses through the suppression of MHC II (major histocompatibility complex II) on interferon gamma-stimulated, antigen-presenting cells such as human vascular endothelial cells. Through the inhibition of mevalonate synthesis, statins, like fluvastatin, have been shown to inhibit the production of dolichol, geranylpyrophosphate (GPP) and farnesylpyrophosphate (FPP) and the isoprenylation of the intracellular G-proteins Ras and Rho, which may result in antiangiogenic, apoptotic, and antimetastatic effects in susceptible tumor cell populations.
(Other name for: trivalent influenza vaccine)
The maleate salt form of fluvoxamine, a 2-aminoethyl oxime ether of aralkylketones, with antidepressant, antiobsessive-compulsive, and antibulimic activities. Fluvoxamine blocks serotonin reuptake by inhibiting the serotonin reuptake pump of the presynaptic neuronal membrane leading to an increase of serotonin levels within the synaptic cleft. This results in facilitated serotonergic transmission and decreased serotonin turnover leading to antidepressant and antiobsessive-compulsive effects.
(Other name for: trivalent influenza vaccine)
A small molecule and orally available inhibitor of colony-stimulating factor-1 receptor (CSF1R; FMS) with potential antineoplastic activity. FMS tyrosine kinase inhibitor JNJ-40346527 blocks the receptor-ligand interaction between FMS and its ligand CSF1, thereby preventing autophosphorylation of FMS. As a result, unphosphorylated FMS cannot activate FMS-mediated signaling pathways, thus potentially inhibiting cell proliferation in FMS-overexpressed tumor cells. FMS, a tyrosine kinase receptor, is overexpressed in certain tumor cell types and plays an essential role in macrophage differentiation, recruitment, and activation as well as the regulation of cell proliferation.
The tosylate salt form of PLX7486, a selective inhibitor of the receptor tyrosine kinases colony-stimulating factor-1 receptor (CSF1R; fms) and neurotrophic tyrosine kinase receptor types 1, 2 and 3 (TrkA, TrkB, and TrkC, respectively) with potential antineoplastic activity. Upon administration, PLX7486 binds to and inhibits the activity of these tyrosine kinases. This inhibits Fms and Trk-mediated signaling transduction pathways that are upregulated in certain cancer cell types. This may eventually halt tumor cell proliferation in Fms and TrkA, TrkB, and/or TrkC-overexpressing tumor cells. Fms and TrkA, TrkB, and TrkC are receptor tyrosine kinases that are upregulated or mutated in a variety of tumors and promote tumor cell proliferation and survival.
A cancer vaccine comprised of human leukocyte antigen (HLA) A2 restricted folate binding protein (FBP) epitope E39 (amino acids 191 to 199), with potential immunostimulatory and antineoplastic activity. Upon intradermal injection, FBP E39 peptide vaccine may induce a specific cytotoxic T-lymphocyte (CTL) response against FBP-expressing tumor cell types. FBP is a membrane-bound, tumor-associated antigen highly overexpressed in various tumor cell types, such as in breast, ovarian and endometrial cancers; E 39 is a strong immunogenic peptide.
A folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation.
A folate receptor-targeting radiopharmaceutical consisting of a folate-containing tetrapeptide chelator to which technetium Tc 99m is linked. The folate component of folate receptor-targeted technetium Tc 99m EC20 binds to folic acid receptors, which are frequently upregulated in many types of tumor cells and activated macrophages. Gamma scintigraphy may then be used to image folate receptor-positive tumors.
A folate receptor-targeting cytotoxic drug conjugate consisting of a folate vitamin analogue linked to a vinca alkaloid microtubule destabilizing agent with potential antineoplastic activity. Mediated through its folate moiety, folate receptor-targeted Vinca alkaloid EC0489 delivers the cytotoxic vinca alkaloid moiety directly to cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. The relative tumor cell specificity of this agent reduces the toxicity profile of its Vinca alkaloid moiety.
A folate receptor-targeting cytotoxic agent with potential antineoplastic activity. Folate receptor-targeted vinca alkaloid/mitomycin C EC0225 contains two potent cytotoxic agents, a vinca alkaloid and mitomycin C, linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the cytotoxic agents directly into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the vinca alkaloid moiety binds to tubulin and disrupts microtubule assembly-disassembly dynamics, resulting in cell cycle arrest and apoptosis. Mitomycin C alkylates DNA, producing DNA cross-links and inhibiting DNA replication. The relative tumor cell specificity of EC0225 reduces the toxicity profiles of its cytotoxic agent moieties.
A conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity. Folate-FITC binds to folate receptors, which are overexpressed on the surfaces of many cancer cells including kidney and ovarian cancer cells. Once bound to the cancer cell through the folate moiety of the conjugate, curculating anti-fluorescein antibodies.may recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity.
(Other name for: methotrexate)
(Other name for: methotrexate)
A chemotherapy regimen consisting of leucovorin calcium (calcium folinate), 5-fluorouracil, and irinotecan used in the treatment of advanced-stage and metastatic colorectal cancer. (NCI Thesaurus)
A first-line chemotherapy regimen consisting of folinic acid (leucovorin), fluorouracil, irinotecan and bevacizumab used for the treatment of advanced-stage colorectal cancer. (NCI Thesaurus)
A chemoimmunotherapy regimen consisting of leucovorin (folinic acid), 5-fluorouracil, and irinotecan plus cetuximab used for the treatment of metastatic colorectal cancer that is positive for the expression of the epidermal growth factor receptor (EGFR) and the wild-type form of KRAS. (NCI Thesaurus)
A regimen consisting of leucovorin calcium, fluorouracil, irinotecan hydrochloride, and oxaliplatin used for the treatment of pancreatic cancer. (NCI Thesaurus)
One of several chemotherapy regimens that include leucovorin calcium (calcium folinate), 5-fluorouracil and oxaliplatin and which may be used in the treatment of advanced-stage and metastatic colorectal cancer. FOLFOX regimens differ in agent dosing and administration schedule and include FOLFOX 4, FOLFOX 6, modified FOLFOX 6 (mFOLFOX 6) and FOLFOX 7. (NCI Thesaurus)
A collective term for pteroylglutamic acids and their oligoglutamic acid conjugates. As a natural water-soluble substance, folic acid is involved in carbon transfer reactions of amino acid metabolism, in addition to and purine and pyrimidine synthesis, and is essential for hematopoiesis and red blood cell production.
A folate-based biomodulator with potential antineoplastic activity. Folitixorin stabilizes the covalent binding of the fluorouracil metabolite 5-5-fluoro-2'-deoxyuridine-5'-O-monophosphate (FdUMP) to its target enzyme, thymidylate synthase, which results in inhibition of thymidylate synthase, depletion of thymidine triphosphate (TTP), a necessary constituent of DNA, and tumor cell death. Unlike leucovorin, folitixorin, as the active form of folate, does not require metabolic activation and may increase the chemotherapeutic effects of fluorouracil with lower toxicity.
(Other name for: recombinant human chorionic gonadotropin)
(Other name for: pralatrexate)
(Other name for: diethylstilbestrol)
The sodium salt form of fondaparinux, a synthetic glucopyranoside with antithrombotic activity. Fondaparinux sodium selectively binds to antithrombin III, thereby potentiating the innate neutralization of activated factor X (Factor Xa) by antithrombin. Neutralization of Factor Xa inhibits its activity and interrupts the blood coagulation cascade, thereby preventing thrombin formation and thrombus development.
An orally bioavailable small molecule with potential antineoplastic activity. MET/VEGFR2 inhibitor GSK1363089 binds to and selectively inhibits hepatocyte growth factor (HGF) receptor c-MET and vascular endothelial growth factor receptor 2 (VEGFR2), which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. The proto-oncogene c-MET has been found to be over-expressed in a variety of cancers. VEGFR2 is found on endothelial and hematopoietic cells and mediates the development of the vasculature and hematopoietic cells through VEGF signaling.
A synthetic steroidal substance with antineoplastic activity. Formestane binds irreversibly to and inhibits the enzyme aromatase, thereby blocking the conversion of cholesterol to pregnenolone and the peripheral aromatization of androgenic precursors into estrogens.
The orally bioavailable fumarate salt of formoterol, a long-acting, selective beta2-adrenergic receptor agonist with bronchodilating and potential anti-cachexia and anabolic activities. In addition to formoterols bronchodilating activity, formoterol exhibits anti-cachexia activity through the inhibition of the ATP-ubiquitin-dependent proteolytic system, which may result in a decrease in protein degradation and muscle cell apoptosis. In addition, formoterol may also increase insulin-like growth factor (IGF) signaling, resulting in an increase in protein synthesis. This agent may also inhibit the calcium-dependent calpain system, resulting in the inhibition of muscle wasting.
A combination preparation of the fumarate salt of a beta2-adrenergic receptor agonist and a macrolide antibiotic, with muscle-sparing and anti-cachexia effects. Formoterol appears to antagonize cachexia by reducing proteolysis mediated through the ubiquitin-protease pathway. Roxithromycin strongly inhibits inflammatory cytokine production and secretion from T cells and macrophages in vitro and in vivo. The combination exhibits a greater muscle sparing effect than either drug given individually at comparable doses.
The hydrochloride salt of the synthetic high-affinity transition-state analogue forodesine. Forodesine binds preferentially to and inhibits purine nucleotide phosphorylase (PNP), resulting in the accumulation of deoxyguanosine triphosphate and the subsequent inhibition of the enzyme ribonucleoside diphosphate reductase and DNA synthesis. This agent selectively causes apoptosis in stimulated or malignant T-lymphocytes. A transition state analogue is a substrate designed to mimic the properties or the geometry of the transition state of reaction.
(Other name for: ceftazidime sodium)
(Other name for: alendronate sodium)
The disodium salt of a water-soluble phosphate derivative of a natural stilbenoid phenol derived from the African bush willow (Combretum caffrum) with potential vascular disrupting and antineoplastic activities. Upon administration, the prodrug fosbretabulin is dephosphorylated to its active metabolite, the microtubule-depolymerizing agent combretastatin A4, which binds to tubulin dimers and prevents microtubule polymerization, resulting in mitotic arrest and apoptosis in endothelial cells. In addition, this agent disrupts the engagement of the endothelial cellspecific junctional molecule vascular endothelial-cadherin (VE-cadherin) and so the activity of the VE-cadherin/-catenin/Akt signaling pathway, which may result in the inhibition of endothelial cell migration and capillary tube formation. As a result of fosbretabulin's dual mechanism of action, the tumor vasculature collapses, resulting in reduced tumor blood flow and ischemic necrosis of tumor tissue.
The tromethamine salt form of prodrug fosbretabulin, a water-soluble phosphate derivative of a stilbenoid phenol derived from the African bush willow (Combretum caffrum) with antineoplastic activities. Upon administration, fosbretabulin is dephosphorylated to its active metabolite, combretastatin A4, which targets and binds to tubulin dimers and prevents microtubule polymerization, thereby resulting in mitotic arrest and apoptosis in endothelial cells. As apoptotic endothelial cells detach from their substrata, tumor blood vessels collapse; the acute disruption of tumor blood flow may result in tumor necrosis.
A water-soluble pentacyclic pyrolloquinone analogue of mitoquidone with potential antineoplastic activity. Currently, the mechansim of action of fosquidone is unknown. In vitro studies indicate that this agent does not bind to DNA or inhibit topoisomerases.
An orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage.Syk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis.
An anti-tumor antibiotic isolated from the bacterium Streptomyces pulveraceus. Fostriecin inhibits topoisomerase II catalytic activity, resulting in protein-associated strand breaks and impaired DNA and RNA synthesis in various malignant cell types. This agent also inhibits serine/threonine protein phosphatase type 2A in some tumor cell types, thereby interfering with cellular proliferation and differentiation.
A chloroethylating nitrosourea with antineoplastic activity. Fotemustine alkylates guanine by forming chloroethyl adducts at the 6 position of guanine, resulting in N1-guanine and N3-cytosine cross linkages, inhibition of DNA synthesis, cell cycle arrest, and finally apoptosis. This agent is lipophilic and crosses the blood-brain barrier.
A recombinant fowlpox virus-based vaccine vector designed to express various tumor-associated peptide antigens. Strong CD8 cytotoxic T cell responses may be induced after prolonged immunization with fowlpox virus vaccines and have been associated with tumor regression. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it does not multiply in human tissues.
A cancer vaccine consisting of a recombinant fowlpox virus vector encoding an immunogenic peptide derived from the cancer-testis antigen NY-ESO-1, an antigen found in normal testis and various tumors, including bladder, breast, hepatocellular, melanoma, and prostate cancers. Vaccination with NY-ESO-1 peptide vaccine may stimulate the host immune system to mount a humoral and cytotoxic T lymphocyte (CTL) response against tumor cells expressing NY-ESO-1 antigen, resulting in tumor cell lysis.
A cancer vaccine consisting of a recombinant fowlpox virus encoding human prostate-specific antigen (PSA) and TRICOM, a combination of three immunostimulants (i.e., B7.1, ICAM-1, and LFA-3). Administration of this agent may induce a cytotoxic T cell response against PSA-expressing tumor cells. Dendritic cells infected with TRICOM vectors greatly enhance naive T-cell activation and peptide-specific T-cell stimulation. Fowlpox virus is an attractive vector because its genome is easy to manipulate and it is replication incompetent in mammalian cells.
(Other name for: dalteparin)
A bioadhesive gel containing 10% freeze-dried black raspberries (FBR) with potential chemopreventive and antioxidant activities. The four main constituent black raspberry anthocyanins that contribute significantly to the chemopreventive effects are cyanidin 3-glucoside (C3GLU), cyanidin 3-rutinoside (C3RUT), cyanidin 3-sambubioside (C3SAM) and cyanidin 3-(2(G)-xylosyl) rutinoside (C3XRUT). Upon mucosal application, the anthocyanins from the gel penetrate the oral mucosa and are able to modulate expression of certain proapoptotic and terminal differentiation genes, and reduce the expression of epithelial cyclooxygenase-2 (COX-2) protein. In addition, this gel may also reduce vascular densities in the superficial connective tissues.
A pan-specific, recombinant, fully human monoclonal antibody directed against human transforming growth factor (TGF) -beta 1, 2 and 3 with potential antineoplastic activity. Fresolimumab binds to and inhibits the activity of all isoforms of TGF-beta, whcih may result in the inhibition of tumor cell growth, angiogenesis, and migration. TGF-beta, a cytokine often over-expressed in various malignancies, may play an important role in promoting the growth, progression, and migration of tumor cells.
Extracts from fruits and vegetables that contain fiber, vitamins, minerals, and other natural substances with antioxidant, lipid-lowering, and antiproliferative properties. Used in chemoprevention therapy, these extracts may prevent the development or recurrence of cancer.
An orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, fruquintinib inhibits VEGF-induced phosphorylation of VEGFRs 1, 2, and 3 which may result in the inhibition of migration, proliferation and survival of endothelial cells, microvessel formation, the inhibition of tumor cell proliferation, and tumor cell death. Expression of VEGFRs may be upregulated in a variety of tumor cell types.
An adjuvant chemotherapy regimen consisting of fluorouracil and leucovorin, administered in various doses and schedules, used for the treatment of colorectal cancer. (NCI Thesaurus)
(Other name for: floxuridine)
A monoclonal antibody directed against nerve growth factor (NGF) with potential analgesic activity. Upon administration, fulranumab binds to NGF, preventing its binding to and activation of the NGF receptors TrkA and p75NTR. Inhibition of the NGF pathway may prevent the perception of pain and may induce analgesia. NGF, a neurotrophic factor that plays a key role in neuropathic and inflammatory-induced pain, promotes hyperalgesia and allodynia.
A synthetic estrogen receptor antagonist. Unlike tamoxifen (which has partial agonist effects) and the aromatase inhibitors (which reduce the estrogen available to tumor cells), fulvestrant binds competitively to estrogen receptors in breast cancer cells, resulting in estrogen receptor deformation and decreased estrogen binding. In vitro studies indicate that fulvestrant reversibly inhibits the growth of tamoxifen-resistant, estrogen-sensitive, human breast cancer cell lines.
A polymeric prodrug consisting of the fumagillol-derived small molecule XMT-1191 tethered to the hydrophilic, biodegradable70 kDa polymer poly[1-hydroxymethylethylene hydroxymethylformal] (PHF) with potential antiangiogenic and antineoplastic activities. Upon administration, fumagillin-derived polymer conjugate XMT-1107 releases XMT-1191, which may inhibit angiogenesis through the irreversible inhibition of the methionine aminopeptidase 2 (METAP2); although the exact mechanism of action has yet to be fully elucidated, this agent appears to induce cell cycle arrest in endothelial cells, inhibiting their proliferation and migration. Compared to an unconjugated fumagillin analog, XMT-1107 exhibits improved solubility and an extended half life due to its PHF backbone.METAP2, a member of the methionyl aminopeptidase family, binds two cobalt or manganese ions and protects the alpha subunit of eukaryotic initiation factor 2 (EIF2) from inhibitory phosphorylation by removing the amino-terminal methionine residue from nascent protein; this aminopeptidase may be overexpressed in a variety of tumor cell types.
(Other name for: amphotericin B deoxycholate)
An anthranilic derivative and loop diuretic with antihypertensive effect. Furosemide blocks the Na-K-Cl cotransporter (NKCC) in the luminal membrane of the thick ascending limb of the loop of Henle in the kidney, by binding to the Cl-binding site located in the cotransporter's transmembrane domain, thereby inhibiting reabsorption of sodium, chloride, potassium ions and water. This agent reduces plasma and extracellular fluid volume resulting in decreased blood pressure and cardiac output.
A topical cream formulation of the bacteriostatic antibiotic fusidic acid and the synthetic, long-acting glucocorticoid betametasone valerate with potential anti-bacterial and immunomodulating activities. Fusidic acid/betamethasone valerate topical cream inhibits Gram-positive bacterial protein synthesis and replication and inhibits the inflammatory response by preventing phospholipid release, inhibiting eosinophil activity, and decreasing pro-inflammatory cytokine production.
(Other name for: levoleucovorin calcium)
A proprietary fusion protein comprised of the cysteine-rich domain of frizzled family receptor 8 (Fzd8) fused to the human immunoglobulin Fc domain with potential antineoplastic activity. Upon intravenous administration, Fzd8 fusion protein OMP-54F28 competes with the membrane-bound Fzd8 receptor for its ligand, Wnt proteins, thereby antagonizing Wnt signaling. This may result in the inhibition of Wnt-driven tumor growth. Fzd8, a member of the Frizzled family of G protein-coupled receptors, is one of the components in the Wnt/beta-catenin signaling pathway that plays key roles in embryogenesis and cancer growth.