jueves, 31 de mayo de 2018

NCI Drug Dictionary - National Cancer Institute | f/F/2

NCI Drug Dictionary - National Cancer Institute

National Cancer Institute

249 results found for: F
FOLFOX regimen
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)
folic acid
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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(Other name for: recombinant human chorionic gonadotropin)
(Other name for: pralatrexate)
(Other name for: diethylstilbestrol)
fondaparinux sodium
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. Check for active clinical trialsusing this agent. (NCI Thesaurus)
(Other name for: isoflurane)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
Forfivo XL
(Other name for: bupropion hydrochloride)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
formoterol fumarate oral
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 formoterol’s 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. Check for active clinical trialsusing this agent. (NCI Thesaurus)
formoterol fumarate/roxithromycin
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. Check for active clinical trials using this agent. (NCI Thesaurus)
forodesine hydrochloride
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(Other name for: metformin hydrochloride)
(Other name for: ceftazidime sodium)
(Other name for: alendronate sodium)
fosbretabulin disodium
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 cell–specific junctional molecule vascular endothelial-cadherin (VE-cadherin) and so the activity of the VE-cadherin/β-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. Check for active clinical trials using this agent. (NCI Thesaurus)
fosbretabulin tromethamine
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. Check for active clinical trials using this agent. (NCI Thesaurus)
fosfomycin tromethamine
The tromethamine salt form of fosfomycin, a synthetic broad-spectrum antibiotic. Fosfomycin tromethamine binds to and inactivates the enzyme enolpyruvyl transferase. This leads to an irreversible blockage of the condensation of uridine diphosphate-N-acetylglucosamine with p-enolpyruvate, which is one of the first steps of bacterial cell wall synthesis, thereby eventually causing cell lysis. In addition, fosfomycin tromethamine reduces the adherence of bacteria to uroepithelial cells.
fosnetupitant/palonosetron hydrochloride
A combination formulation containing the prodrug of netupitant, fosnetupitant, a selective neurokinin 1 receptor (NK1R; TACR1) antagonist, and the hydrochloride salt form of palonosetron, a selective serotonin (5-hydroxytrytamine; 5-HT) receptor subtype 3 (5-HT3R) antagonist, with potential antiemetic activity. Upon intravenous administration, fosnetupitant is converted by phosphatases to its active form netupitant. Netupitant competitively binds to and blocks the activity of NK1Rs in the central nervous system (CNS), by inhibiting binding of the endogenous tachykinin-derived neuropeptide substance P (SP) to NK1R. This prevents delayed emesis, which is associated with SP secretion. Palonosetron competitively blocks the interaction of 5-HT with 5-HT3Rs located on vagal afferent nerves in the chemoreceptor trigger zone (CTZ). This inhibits acute emesis associated with 5-HT secretion and subsequent 5-HT3R activation. Altogether, this results in inhibition of acute and delayed nausea and vomiting, and may prevent chemotherapy-induced nausea and vomiting (CINV).
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. Check for active clinical trials using this agent. (NCI Thesaurus)
fostamatinib disodium
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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trialsusing this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
fowlpox virus vaccine vector
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. Check for active clinical trials using this agent. (NCI Thesaurus)
fowlpox-NY-ESO-1 vaccine
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(Other name for: dalteparin sodium)
Fragmin V
(Other name for: dalteparin sodium)
freeze-dried black raspberry bioadhesive gel
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. Check for active clinical trials using this agent. (NCI Thesaurus)
French maritime pine bark extract
A nutritional supplement containing an extract obtained from the French maritime pine bark Pinus pinaster, with potential immunomodulating and antioxidant activities. The French maritime pine bark extract contains high amounts of the phytochemicals proanthocyanidins. Proanthocyanidins are able to scavenge free radicals, and therefore may inhibit cellular damage. This extract may also ameliorate the symptoms of lymphedema and improve blood flow. It might also stimulate the immune system and have antioxidant effects. Check for active clinical trials using this agent. (NCI Thesaurus)
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, which 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. Check for active clinical trials using this agent. (NCI Thesaurus)
fructooligosaccharide supplement
A supplement containing oligosaccharide fructans, with gastrointestinal (GI) protective and immumopotentiating activities. Upon oral administration of the supplement, the oligosaccharides stimulate the growth of certain GI bacteria and activate the immune system. This improves the intestinal microflora, strengthens the immune system and increases the protective function of the GI barrier. Check for active clinical trials using this agent. (NCI Thesaurus)
fructooligosaccharide/Lactobacillus paracasei/Lactobacillus rhamnosus/Lactobacillus acidophilus/Bifidobacterium lactis
A synbiotic nutritional supplement containing fructooligosaccharides (FOS), which are linear chains of fructose units that are linked by beta (2-1) bonds, and probiotic cultures of Lactobacillus paracasei (L. paracasei), L. rhamnosus, L. acidophilus and Bifidobacterium lactis (B. lactis), with gastrointestinal (GI) protective and immunomodulating activities. Upon oral administration, the bacteria in this probiotic supplement help maintain adequate colonization of the GI tract and modulate the composition of the normal microflora. Upon colonization of the GI tract, the probiotic bacteria form a protective barrier that helps maintain the integrity of the epithelial barrier. This will interfere with the attachment of pathogenic bacteria and other harmful substances, prevent inflammation and improve GI function. Additionally, the reconstituted microflora may metabolize FOS, which may promote calcium mobilization into the bloodstream by maintaining a neutral pH in the lower gut. Check for active clinical trials using this agent. (NCI Thesaurus)
fruit and vegetable extracts
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. Check for active clinical trials using this agent. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (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. Check for active clinical trials using this agent. (NCI Thesaurus)
FU-LV regimen
A regimen consisting of fluorouracil and leucovorin, used in both the adjuvant and metastatic disease setting, for the treatment of colorectal cancer. This regimen is also combined with radiation for the treatment of gastric and esophageal cancer. (NCI Thesaurus)
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(Other name for: crofelemer)
fumagillin-derived polymer conjugate XMT-1107
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(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. Check for active clinical trials using this agent. (NCI Thesaurus)
A nutritional supplement and vitamin B1 derivative, with potential antineoplastic activity. Upon oral administration, fursultiamine inhibits the expressions of octamer-binding transcription factor 4 (OCT-4), SRY (sex determining region Y)-box 2 (SOX-2), and Nanog homeobox (NANOG) in cancer stem cells (CSCs). This may inhibit the proliferation of CSCs thereby preventing tumor cell growth. In addition, fursultiamine inhibits the expression of ATP-binding cassette (ABC) transporters subfamily B member 1 (ABCB1) and subfamily G member 2 (ABCG2) in cancer CSCs, which may abrogate resistance to chemo- and radiotherapy in CSCs. CSCs promote tumor initiation, progression and metastasis; they play a key role in cancer recurrence and resistance to chemotherapy and radiation. Check for active clinical trials using this agent. (NCI Thesaurus)
fusidic acid/betamethasone valerate topical cream
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. Check for active clinical trials using this agent. (NCI Thesaurus)
(Other name for: leucovorin calcium)
(Other name for: levoleucovorin calcium)
(Other name for: perampanel)

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