Drug Dictionary


F16-IL2 fusion protein

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. Check for active clinical trials using this agent. (NCI Thesaurus)

F-18 16 alpha-fluoroestradiol

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. Check for active clinical trials using this agent. (NCI Thesaurus)

F-18 fluoroethyltyrosine

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. Check for active clinical trials using this agent. (NCI Thesaurus)

FACT complex-targeting curaxin CBL0137

An orally available curaxin-based agent targeting the Facilitates Chromatin Transcription (FACT) complex, with potential antineoplastic activity. Upon administration, CBL0137 binds to FACT and sequesters the FACT complex on chromatin, which inhibits its activity. This prevents transcription of certain genes involved in cancer-associated signaling pathways; it specifically inhibits the transcription of both NF-kappa and heat shock transcription factor 1 (HSF1) and simultaneously activates p53. This causes an increase in tumor cell apoptosis and a decrease in tumor cell proliferation, in FACT-positive cancers. In addition, this agent is able to sensitize FACT-positive tumor cells to the cytotoxic effects of other chemotherapeutic agents. FACT, a transcription and replication factor composed of the Structure Specific Recognition Protein (SSRP1) and suppressor of Ty 16 (Spt16) proteins, is expressed in a variety of tumor cells while almost absent in normal cells; its expression is associated with increased tumor aggressiveness and poor prognosis. Check for active clinical trials using this agent.

factor VIIa inhibitor PCI-27483

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fadrozole hydrochloride

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. Check for active clinical trials using this agent. (NCI Thesaurus)

FAK inhibitor GSK2256098

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. Check for active clinical trials using this agent. (NCI Thesaurus)

FAK inhibitor PF-00562271

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. Check for active clinical trials using this agent. (NCI Thesaurus)

FAK inhibitor VS-4718

An orally bioavailable focal adhesion kinase (FAK) inhibitor with potential antineoplastic activity. Upon administration, VS-4718 inhibits FAK, blocks fibronectin-stimulated FAK autophosphorylation of Tyr397, and may prevent the integrin-mediated activation of several downstream signal transduction pathways, including ERK, JNK/MAPK and PI3K/Akt. This results in the reduction of the number of cancer stem cells (CSCs) and inhibits tumor cell migration, proliferation and survival. The cytoplasmic tyrosine kinase FAK is a signal transducer for integrins and is constitutively activated in various tumor cell types; it is involved in tumor cell invasion, migration and proliferation and plays a key role in the development, function and survival of CSCs. Check for active clinical trials using this agent. (NCI Thesaurus)

falimarev

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. Check for active clinical trials using this agent. (NCI Thesaurus)

famitinib

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. Check for active clinical trials using this agent. (NCI Thesaurus)

famotidine

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. Check for active clinical trials using this agent. (NCI Thesaurus)

FAP-specific CD8-positive T cells

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Fareston

(Other name for: toremifene)

Farestone

(Other name for: toremifene)

farletuzumab

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Farydak

(Other name for: panobinostat)

Fas receptor agonist APO010

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Fasigyn

(Other name for: tinidazole)

Faslodex

(Other name for: fulvestrant)

FASN inhibitor TVB-2640

An orally bioavailable fatty acid synthase (FASN) inhibitor, with potential antineoplastic activity. Upon administration, TVB-2640 binds to and blocks FASN, which prevents the synthesis of palmitate needed for tumor cell growth and survival. This leads to a reduction in cell signaling, an induction of tumor cell apoptosis and the inhibition of cell proliferation in susceptible tumor cells. FASN, an enzyme responsible for the de novo synthesis of palmitic acid, is overexpressed in tumor cells and plays a key role in tumor metabolism, lipid signaling, tumor cell survival and drug resistance; tumor cells are dependent on increased fatty acid production for their enhanced metabolic needs and rapid growth. Check for active clinical trials using this agent. (NCI Thesaurus)

fat emulsion

A liquid composed of two immiscible substances, typically some form of fat and water. In parenteral nutrition, a fat emulsion may contain phospholipids, triglycerides and essential fatty acids. Check for active clinical trials using this agent.

fazarabine

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. Check for active clinical trials using this agent. (NCI Thesaurus)

febuxostat

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. Check for active clinical trials using this agent.

FEC Regimen

A regimen consisting of fluorouracil, epirubicin and cyclophosphamide used in the adjuvant setting and also for the treatment of recurrent and metastatic breast cancer. (NCI Thesaurus)

Feldene

(Other name for: piroxicam)

Femara

(Other name for: letrozole)

Femest

(Other name for: conjugated estrogens)

Feminone

(Other name for: ethinyl estradiol)

fenofibrate

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fenretinide

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fenretinide lipid matrix

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. Check for active clinical trials using this agent. (NCI Thesaurus)

Fenretinide Lym-X-Sorb

(Other name for: fenretinide lipid matrix)

fentanyl buccal soluble film

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl citrate

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl citrate buccal tablet

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl citrate pectin-based nasal spray

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl citrate-containing nasal spray

A nasal spray containing a phosphate-buffered solution of the citrate salt form of fentanyl, a short-acting, synthetic, lipophilic anilidopiperidine opioid, with analgesic activity. Upon applying one puff in the nostril, the fentanyl is rapidly absorbed through the nasal mucosa and selectively binds to and activates mu-opioid receptors in the central nervous system (CNS), mimicking the effects of endogenous opiates. Due to its quick onset and short duration of action, the administration of fentanyl nasal spray may relieve breakthrough pain in adults already receiving maintenance opioid therapy for chronic pain. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl matrix transdermal patch

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. Check for active clinical trials using this agent. (NCI Thesaurus)

fentanyl sublingual spray

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. Check for active clinical trials using this agent. (NCI Thesaurus)

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