CIENCIASMEDICASNEWS: NCI Drug Dictionary - National Cancer Institute

NCI Drug Dictionary - National Cancer Institute

257 results found for: B

brentuximab vedotin: An antibody-drug conjugate (ADC) directed against the tumor necrosis factor (TNF) receptor CD30 with potential antineoplastic activity. Brentuximab vedotin is generated by conjugating the humanized anti-CD30 monoclonal antibody SGN-30 to the cytotoxic agent monomethyl auristatin E (MMAE) via a valine-citrulline peptide linker. Upon administration and internalization by CD30-positive tumor cells, brentuximab vedotin undergoes enzymatic cleavage, releasing MMAE into the cytosol; MMAE binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and tumor cell apoptosis. Transiently activated during lymphocyte activation, CD30 (tumor necrosis factor receptor superfamily, member 8;TNFRSF8) may be constitutively expressed in hematologic malignancies including Hodgkin lymphoma and some T-cell non-Hodgkin lymphomas. The linkage system in brentuximab vedotin is highly stable in plasma, resulting in cytotoxic specificity for CD30-positive cells. Check for active clinical trials using this agent. (NCI Thesaurus)
brequinar: A synthetic quinolinecarboxylic acid analogue with antineoplastic properties. Brequinar inhibits the enzyme dihydroorotate dehydrogenase, thereby blocking de novo pyrimidine biosynthesis. This agent may also enhance the in vivo antitumor effect of antineoplastic agents such as 5-FU. Check for active clinical trials using this agent. (NCI Thesaurus)
Brevicon: (Other name for: ethinyl estradiol/norethindrone)
Bria-IMT: (Other name for: allogeneic GM-CSF-secreting breast cancer vaccine SV-BR-1-GM)
briciclib sodium: A benzyl styryl sulfone analog, and a disodium phosphate ester prodrug of ON 013100, with potential antineoplastic activity. Upon hydrolysis, briciclib sodium is converted to ON 013100, which blocks cyclin D mRNA translation and decreases protein expression of cyclin D. This may induce cell cycle arrest and apoptosis in cancer cells overexpressing cyclin D and eventually decrease tumor cell proliferation. This agent may exhibit synergistic antitumor activity in combination with other chemotherapeutic agents. Cyclin D, a member of the cyclin family of cell cycle regulators, plays a key role in cell cycle division and is often overexpressed in a variety of hematologic and solid tumors and is correlated with poor prognosis. Check for active clinical trials using this agent. (NCI Thesaurus)
Bridion: (Other name for: sugammadex sodium)
brigatinib: An orally available inhibitor of receptor tyrosine kinases anaplastic lymphoma kinase (ALK) and the epidermal growth factor receptor (EGFR) with potential antineoplastic activity. Brigatinib binds to and inhibits ALK kinase and ALK fusion proteins as well as EGFR and mutant forms. This leads to the inhibition of ALK kinase and EGFR kinase, disrupts their signaling pathways and eventually inhibits tumor cell growth in susceptible tumor cells. In addition, brigatinib appears to overcome mutation-based resistance. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development; ALK dysregulation and gene rearrangements are associated with a series of tumors. EGFR is overexpressed in a variety of cancer cell types. Check for active clinical trials using this agent. (NCI Thesaurus)
brilacidin oral rinse: An oral rinse containing brilacidin, a defensin mimetic, with potential antimicrobial and anti-mucositic activities. Upon rinsing with the brilacidin oral rinse, brilacidin imitates defensin as a human host defense protein (HDP), and binds to and disrupts the bacterial cell membrane. This causes bacterial cell membrane lysis and leakage of cellular cytoplasmic contents. This inhibits bacterial activity and may prevent or treat radiation-induced mucositis. Defensins, a family of antimicrobial and cytotoxic peptides expressed mainly by epithelial cells and neutrophils, play a key role in the natural human innate immunity against pathogens. Check for active clinical trials using this agent. (NCI Thesaurus)
brimonidine tartrate: The tartrate salt form of brimonidine, an imidazole derivative and a selective alpha-2 adrenergic receptor agonist. Upon ocular administration, brimonidine tartrate acts on the blood vessels causing them to constrict which leads to a decrease in the production of aqueous humor. Brimonidine tartrate also enhances the outflow of aqueous humor. This drug is used in the treatment of glaucoma to reduce intraocular pressure. Check for active clinical trials using this agent. (NCI Thesaurus)
brincidofovir: An alkoxyalkyl ester prodrug containing the synthetic, acyclic nucleoside monophosphate analog cidofovir linked, through its phosphonate group, to a lipid, 3-hexadecyloxy-1-propanol, with antiviral activity against double-stranded DNA viruses. Upon oral administration, brincidofovir crosses the intestinal wall and penetrates target viral-infected cells before being cleaved to the free antiviral agent cidofovir. In turn, cidofovir is phosphorylated by pyruvate kinases to its active metabolite cidofovir diphosphate. Cidofovir diphosphate, bearing structural similarity to nucleotides, competes with deoxycytosine-5-triphosphate (dCTP) for viral DNA polymerase and gets incorporated into the growing viral DNA strands. As a result, it prevents further DNA polymerization and disrupts DNA replication of viruses. Compared to cidofovir, which is given intravenously, hexadecyloxypropyl-cidofovir shows better oral bioavailability, less toxicity and enhanced cellular penetration. Check for active clinical trials using this agent. (NCI Thesaurus)
Brintellix: (Other name for: vortioxetine hydrobromide)
brivanib alaninate: The alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression. Check for active clinical trials using this agent. (NCI Thesaurus)
brivaracetam: An orally bioavailable levetiracetam derivative, with anticonvulsant activity. Although the exact mechanism through which brivaracetam exerts its effects is not fully known, this agent targets and binds to synaptic vesicle protein 2A (SV2A) in the brain. This prevents synaptic vesicle exocytosis and the synaptic release of certain, as of yet not fully known, excitatory neurotransmitters. This may inhibit impulse conduction across synapses, decrease neuronal (hyper-)excitability, and may modulate epileptogenesis. SV2A, a membrane glycoprotein present in neuronal synaptic vesicles, plays a key role in action potential-induced neurotransmitter release in the brain. Check for active clinical trialsusing this agent. (NCI Thesaurus)
Briviact: (Other name for: brivaracetam)
brivudine phosphoramidate: A small molecule phosphoramidate derivative of (E)-5-(2-bromovinyl)-2'-deoxyuridine with potential antineoplastic activity. Selectively active against tumor cells expressing high levels of thymidylate synthase (TS), brivudine phosphoramidate is converted intracellularly by TS to bromovinyldeoxyuridine monophosphate (BVdUMP) which competes with the natural substrate, deoxyuridine monophosphate, for binding to TS. Unlike TS inhibitors, this agent is a reversible substrate for TS catalysis. Thus, TS retains activity and converts BVdUMP into cytotoxic metabolites. As key enzyme in the de novo synthesis of dTMP, TS is an enzyme critical to DNA biosynthesis and is overexpressed in many solid tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
broad-spectrum human papillomavirus vaccine V505: A non-infectious recombinant cancer vaccine prepared from the human papillomavirus (HPV) with potential immunoprophylactic activity. Vaccination with broad-spectrum human papillomavirus vaccine V505 may stimulate the host immune system to mount humoral and cytotoxic T lymphocyte (CTL) responses against HPV-infected cells. HPV infection, the cause of genital warts, is a risk factor for the development of cancers of the cervix, vagina, vulva, anus, and penis. Check for active clinical trials using this agent. (NCI Thesaurus)
broccoli sprout extract: A cruciferous vegetable extract with potential chemopreventive activities. Broccoli sprout extract contains a high amount of sulforaphane, a naturally occurring isothiocyanate. Sulforaphane activates the transcription factor NF-E2-related factor 2 (Nrf2), a member of the basic leucine zipper family, which binds to and activates antioxidant-response elements (AREs). Subsequently, activated AREs mediate the transcription of antioxidant enzymes (particularly glutathione-S-transferase and quinone oxidoreductase), resulting in the detoxification of highly reactive carcinogens. AREs are cis-acting regulatory enhancer elements found in the 5’ flanking region of many phase II detoxification enzymes. Check for active clinical trials using this agent. (NCI Thesaurus)
broccoli sprout/broccoli seed extract supplement: A tablet-based nutritional supplement composed of a mixture of sprout and seed extracts of the cruciferous vegetable broccoli, with potential chemopreventive and antioxidant activities. Broccoli sprout/broccoli seed extract contains a high amount of both the glucosinolate glucoraphanin and the enzyme myrosinase, which catalyzes the production of glucoraphanin to sulforaphane. Upon administration of the broccoli sprout/broccoli seed extract, sulforaphane activates the transcription factor NF-E2-related factor 2 (Nrf2), a member of the basic leucine zipper family, which binds to and activates antioxidant-response elements (AREs). Subsequently, activated AREs promote the transcription of antioxidant and detoxifying enzymes, particularly glutathione-S-transferase and NAD(P)H dehydrogenase [quinone] 1 (NAD(P)H:quinone oxidoreductase; NQO1), resulting in the detoxification of highly reactive carcinogens. This accelerates the elimination of carcinogens, may protect against cellular damage, and prevents cancer formation. AREs are cis-acting regulatory enhancer elements found in the 5' flanking region of many phase II detoxification enzymes.
bromelain: A proteolytic enzyme obtained from the pineapple plant that cleaves sulhydryl groups. The enzyme is adsorbed intact through the gastrointestinal tract and has demonstrated therapeutic benefit. Bromelain has the ability to modulate cytokines, and has also demonstrated anti-inflammatory activity, immune response activity, and fibrinolytic activity. Check for active clinical trials using this agent. (NCI Thesaurus)
bromocriptine mesylate: The mesylate salt of bromocriptine, a semisynthetic ergot alkaloid with dopaminergic, antidyskinetic, and antiprolactinemic activities. Bromocriptine selectively binds to and activates postsynaptic dopamine D2 receptors in the corpus striatum of the central nervous system (CNS). Activation of these D2 receptors activate inhibitory G-proteins, which inhibit adenylyl cyclase, preventing signal transduction mediated via cAMP and resulting in the inhibition of neurotransmission and an antidyskinetic effect. Ths agent also stimulates dopamine D2 receptors in the anterior pituitary gland, which results in the inhibition of prolactin secretion and lactation and may inhibit the proliferation of prolactin-dependent breast cancer cells. Check for active clinical trials using this agent. (NCI Thesaurus)
bromodeoxyuridine: A halogenated thymidine analogue with potential antineoplastic and radiosensitizing activities. Bromodeoxyuridine competes with thymidine for incorporation into DNA, resulting in DNA mutation and the inhibition of cell proliferation. As a radiosensitizer, this agent is associated with the inhibition of repair of radiation-induced DNA double-strand breaks (DSBs). Check for active clinical trials using this agent. (NCI Thesaurus)
bromodomain inhibitor ABBV-075: An inhibitor of one or more as of yet undisclosed bromodomain (BRD)-containing protein(s), with potential antineoplastic activity. Upon administration, the bromodomain inhibitor ABBV-075 binds to the acetyl-lysine binding site in the BRD of certain BRD-containing protein(s), thereby preventing the interaction between those proteins and acetylated histones. This disrupts chromatin remodeling, prevents the expression of certain growth-promoting genes, and leads to an inhibition of cell growth in susceptible tumors. Check for active clinical trials using this agent. (NCI Thesaurus)
bromovinyl-deoxyuridine: A uridine derivative and nucleoside analog with pro-apoptotic and chemosensitizing properties. In vitro, bromovinyl-deoxyuridine (BVDU) has been shown to downregulate the multifunctional DNA repair enzyme APEX nuclease 1, resulting in the inhibition of DNA repair and the induction of apoptosis. In addition, this agent may inhibit the expression of STAT3 (signal transducer and activator of transcription 3), which may result in the downregulation of vascular endothelial growth factor (VEGF). BVDU has also been found to inhibit the upregulation of chemoresistance genes (Mdr1 and DHFR) during chemotherapy. Overall, the gene expression changes associated with BVDU treatment result in the decrease or prevention of chemoresistance. In addition, this agent has been shown to enhance the cytolytic activity of NK-92 natural killer cells towards a pancreatic cancer cell line in vitro. Check for active clinical trials using this agent. (NCI Thesaurus)
brontictuzumab: A humanized monoclonal antibody directed against the Notch-1 receptor with potential antineoplastic activity. Upon administration, brontictuzumab binds to Notch-1 on the cell surface, thereby inhibiting Notch-mediated signaling and tumor cell proliferation. Notch 1, a type 1 transmembrane protein belonging to the Notch family, functions as a receptor for membrane bound ligands and has various roles during development; dysregulated Notch signaling is associated with increased cell growth and chemoresistance in cancers.
brostallicin: A synthetic, alpha-bromoacrylic, second-generation minor groove binder (MGB), related to distamycin A, with potential antineoplastic activity. Brostallicin binds to DNA minor groove DNA, after having formed a highly reactive glutathione (GSH)-brostallicin complex in the presence of the enzyme glutathione S-transferase (GST), which is overexpressed in cancer cells; DNA replication and cell division are inhibited, resulting in tumor cell death. Compared to typical MGBs, this agent appears to bind covalently to DNA in a different manner and its activity does not depend on a functional DNA mismatch repair (MMR) mechanism. Accordingly, brostallicin may be effective against MMR-defective tumors that are refractory to various anticancer agents. Check for active clinical trials using this agent. (NCI Thesaurus)
bruceantin: A triterpene quassinoid antineoplastic antibiotic isolated from the plant Brucea antidysenterica. Bruceantin inhibits the peptidyl transferase elongation reaction, resulting in decreased protein and DNA synthesis. Bruceantin also has antiamoebic and antimalarial activity. Check for active clinical trials using this agent. (NCI Thesaurus)
Brussels sprout: A leafy green vegetable and a member of the Gemmifera group of cabbages that contains high amounts of phytochemicals, with potential chemopreventive activity. Brussels sprouts contain high amounts of the glycosinolate glucobrassicin. Upon consumption of brussels sprouts, the phytochemicals in the vegetable, and some of their metabolites, are able to induce the expression of various hepatic cytochrome P450 monooxygenases, scavenge free radicals and may inhibit the activation of various signal transduction pathways. Check for active clinical trials using this agent. (NCI Thesaurus)
bryostatin 1: A macrocyclic lactone isolated from the bryozoan Bugula neritina with antineoplastic activity. Bryostatin-1 binds to and inhibits the cell-signaling enzyme protein kinase C, resulting in the inhibition of tumor cell proliferation, the promotion of tumor cell differentiation, and the induction of tumor cell apoptosis. This agent may act synergistically with other chemotherapeutic agents. Check for active clinical trials using this agent. (NCI Thesaurus)
BTK inhibitor ARQ 531: An orally available reversible inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, ARQ 531 non-covalently binds to and inhibits the activity of both the wild-type and the C481S mutated form of BTK, a resistance mutation in the BTK active site in which cysteine is substituted for serine at residue 481. This prevents the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. Compared to other BTK inhibitors, ARQ 531 does not require interaction with the BTK C481 site and inhibits the proliferation of cells harboring the BTK C481S mutation. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed or mutated in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B lymphocytes. Check for active clinical trials using this agent. (NCI Thesaurus)
BTK inhibitor CC-292: An orally bioavailable, selective inhibitor of Bruton’s agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, AVL-292 targets and covalently binds to BTK, thereby preventing its activity. By irreversibly inhibiting BTK, administration of this agent may lead to an inhibition of B cell receptor (BCR) signaling and may inhibit cell proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. Check for active clinical trialsusing this agent. (NCI Thesaurus)
BTK inhibitor CT-1530: An inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, CT-1530 binds to and inhibits the activity of BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed or mutated in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B lymphocytes. Check for active clinical trials using this agent. (NCI Thesaurus)
BTK inhibitor DTRMWXHS-12: An orally available inhibitor of Bruton's tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase), with potential antineoplastic activity. Upon administration, DTRMWXHS-12 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways. This leads to an inhibition of the growth of malignant B cells that overexpress BTK. BTK, a member of the src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in the development, activation, signaling, proliferation and survival of B lymphocytes. Check for active clinical trials using this agent. (NCI Thesaurus)
BTK inhibitor GDC-0853: An orally available inhibitor of Bruton's tyrosine kinase (BTK) with potential antineoplastic activity. Upon administration, GDC-0853 inhibits the activity of BTK and prevents the activation of the B-cell antigen receptor (BCR) signaling pathway. This prevents both B-cell activation and BTK-mediated activation of downstream survival pathways, which leads to the inhibition of the growth of malignant B-cells that overexpress BTK. BTK, a member of the Src-related BTK/Tec family of cytoplasmic tyrosine kinases, is overexpressed in B-cell malignancies; it plays an important role in B-lymphocyte development, activation, signaling, proliferation and survival. Check for active clinical trials using this agent. (NCI Thesaurus)
BTK inhibitor M7583: An orally bioavailable, selective inhibitor of Bruton's tyrosine kinase (BTK), with potential antineoplastic activity. Upon administration, M7583 targets and covalently binds to BTK, thereby preventing its activity. This leads to an inhibition of B cell receptor (BCR) signaling and inhibits cell proliferation of B-cell malignancies. BTK, a cytoplasmic tyrosine kinase and member of the Tec family of kinases, plays an important role in B lymphocyte development, activation, signaling, proliferation and survival. Check for active clinical trialsusing this agent. (NCI Thesaurus)
budesonide/formoterol fumarate dihydrate inhalation aerosol: An inhalation aerosol formulation containing budesonide and the fumarate dihydrate salt of formoterol with anti-inflammatory and bronchial smooth muscle-relaxing activities. The synthetic corticosteroid steroid budesonide binds to intracellular glucocorticosteroid receptors (GRs), exhibiting inhibitory activities against multiple cell types and mediators associated with allergic inflammation. The long-acting beta-adrenergic receptor agonist formoterol selectively binds to beta-2 adrenergic receptors in bronchial smooth muscle, activating intracellular adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP); increased intracellular cAMP result in the relaxation of bronchial smooth muscle and inhibition of the cellular release of mediators of immediate hypersensitivity, especially from mast cells. Check for active clinical trials using this agent. (NCI Thesaurus)
buformin hydrochloride: The hydrochloride salt form of buformin, an agent belonging to the biguanide class of antidiabetics with antihyperglycemic activity. Buformin is not metabolized and is excreted in the urine. This agent has an elevated risk of causing lactic acidosis, and has been withdrawn from the market. Check for active clinical trials using this agent. (NCI Thesaurus)
Bulkamid: (Other name for: polyacrylamide hydrogel)
bumetanide: A potent sulfamoylanthranilic acid derivative belonging to the class of loop diuretics. In the brain, bumetanide may prevent seizures in neonates by blocking the bumetanide-sensitive sodium-potassium-chloride cotransporter (NKCC1), thereby inhibiting chloride uptake thus, decreasing the internal chloride concentration in neurons and may block the excitatory effect of GABA in neonates. Check for active clinical trials using this agent. (NCI Thesaurus)
Bumex: (Other name for: bumetanide)
buparlisib: An orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. Buparlisib specifically inhibits class I PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials using this agent. (NCI Thesaurus)
Buphenyl: (Other name for: sodium phenylbutyrate)
bupivacaine hydrochloride: A long-acting, amide-type local anesthetic. Bupivicaine reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization; inhibition of depolarization and nerve impulse conduction; and a reversible loss of sensation. Check for active clinical trials using this agent. (NCI Thesaurus)
bupivacaine hydrochloride liposome injectable suspension: A liposome-encapsulated formulation of bupivacaine, which is an amide-type, long-acting local anesthetic. Upon administration, bupivacaine reversibly binds to specific sodium ion channels in the neuronal membrane, resulting in both a decrease in the voltage-dependent membrane permeability to sodium ions and membrane stabilization. This leads to inhibition of both depolarization and nerve impulse conduction, and a reversible loss of sensation. Compared to bupivacaine alone, liposomal delivery increases the duration of local anesthetic action and delays the peak plasma concentration of bupivacaine due to its slow release from the liposome. Check for active clinical trials using this agent. (NCI Thesaurus)
buprenorphine transdermal matrix patch: A transdermal matrix patch containing the synthetic opioid buprenorphine with analgesic and sedative activities. Buprenorphine binds to and activates the mu-opioid receptors in the central nervous system (CNS), thereby mimicking the effects of the endogenous opiates. Binding to opioid receptors stimulates exchange of GTP for GDP, inhibits adenylate cyclase, and decreases intracellular cAMP. This inhibits the release of various nociceptive neurotransmitters, such as substance P, gamma-aminobutyric acid (GABA), dopamine, acetylcholine, noradrenaline, vasopressin, and somatostatin. In addition, buprenorphine closes N-type voltage-gated calcium channels and opens calcium-dependent inwardly rectifying potassium channels, resulting in hyperpolarization, reduced neuronal excitability, analgesia and sedation. Buprenorphine is a partial agonist at the mu-opioid receptor and an antagonist at the kappa-opioid receptor in the CNS. Check for active clinical trials using this agent. (NCI Thesaurus)
bupropion hydrochloride: The hydrochloride salt of an aminoketone antidepressant. The molecular mechanism of the antidepressant effect of bupropion is unknown. This agent does not inhibit monoamine oxidase and, compared to classical tricyclic antidepressants, is a weak blocker of the neuronal uptake of serotonin and norepinephrine. Buproprion also weakly inhibits the neuronal re-uptake of dopamine. Check for active clinical trials using this agent. (NCI Thesaurus)
bupropion hydrochloride controlled-release: A controlled-release tablet formulation containing the hydrochloride salt of the aminoketone bupropion, with antidepressant activity and for potential use in promoting smoking cessation and improving sexual desire. Bupropion is a weak blocker of the neuronal uptake of serotonin, dopamine and norepinephrine and is a central nicotinic acetylcholine receptor antagonist. The controlled-release formulation results in a higher concentration of the drug in the body over an extended period of time, thereby permitting a reduction in the frequency of dosing
burixafor: An orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Burixafor binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation; this may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into blood. CXCR4, a chemokine receptor belonging to the G protein-coupled receptor (GPCR) gene family, plays an important role in chemotaxis and angiogenesis and is upregulated in several tumor cell types; CXCL12/CXCR4 interaction induces retention of hematopoietic cells in the bone marrow. Check for active clinical trials using this agent. (NCI Thesaurus)
buserelin: A synthetic analog of gonadotropin-releasing hormone (GnRH). Buserelin binds to and activates pituitary gonadotropin releasing hormone (GnRH) receptors. Prolonged administration of buserelin results in sustained inhibition of gonadotropin production, suppression of testicular and ovarian steroidogenesis, and reduced levels of circulating gonadotropin and gonadal steroids. Buserelin is more potent that GnRH. Check for active clinical trials using this agent. (NCI Thesaurus)
Buspar: (Other name for: buspirone hydrochloride)
buspirone hydrochloride: The hydrochloride salt of an anxiolytic agent chemically and pharmacologically unrelated to benzodiazepines, barbiturates, or other sedative/hypnotic drugs. Although its exact mechanism of action is unknown, buspirone may exert its anti-anxiety effects via serotonin (5-HT1A) and dopamine receptors (D2) and may indirectly affect other neurotransmitter systems. Unlike typical benzodiazepine anxiolytics, this agent does not exert anticonvulsant or muscle relaxant effects and lacks prominent sedative effects. Check for active clinical trials using this agent. (NCI Thesaurus)
busulfan: A synthetic derivative of dimethane-sulfonate with antineoplastic and cytotoxic properties. Although its mechanism of action is not fully understood, busulfan appears to act through the alkylation of DNA. Following systemic absorption of busulfan, carbonium ions are formed, resulting in DNA alkylation and DNA breaks and inhibition of DNA replication and RNA transcription. Check for active clinical trials using this agent. (NCI Thesaurus)
busulfan-melphalan regimen: A chemotherapeutic regimen composed of busulfan and melphalan used as a conditioning regimen for stem cell transplantation (SCT). (NCI Thesaurus)
Busulfex: (Other name for: busulfan)
buthionine sulfoximine: A synthetic amino acid. Buthionine sulfoximine irreversibly inhibits gamma-glutamylcysteine synthetase, thereby depleting cells of glutathione, a metabolite that plays a critical role in protecting cells against oxidative stress, and resulting in free radical-induced apoptosis. Elevated glutathione levels are associated with tumor cell resistance to alkylating agents and platinum compounds. By depleting cells of glutathione, this agent may enhance the in vitro and in vivo cytotoxicities of various chemotherapeutic agents in drug-resistant tumors. Buthionine sulfoximine may also exhibit antiangiogenesis activity. Check for active clinical trials using this agent. (NCI Thesaurus)
butylscopolamine bromide: An orally available bromide salt form of butylscopolamine, a quaternary ammonium derivative of the alkaloid scopolamine, with anticholinergic property. Upon oral administration, hyoscine butylbromide binds to and blocks muscarinic receptors located on postganglionic parasympathetic nerve endings and on smooth muscle cells. This blocks the activity of acetylcholine (Ach) and causes its antispasmodic effect in the gastrointestinal (GI), urinary, uterine, and biliary tracts. This agent may also facilitate radiologic visualization of the GI tract. Check for active clinical trials using this agent. (NCI Thesaurus)
BXQ-350 nanovesicle formulation: A stable, nanovesicle formulation composed of a synthetic form of the human glycoprotein saposin C (SapC) linked to the phospholipid dioleoylphosphatidylserine (DOPS), with potential antineoplastic activity. Upon intravenous administration, the BXQ-350 nanovesicle formulation selectively targets and preferentially accumulates in tumor vessels and cells, due to the leaky nature of tumor vasculature and the presence of phosphatidylserine (PS) lipids in tumor cell membranes. Upon binding to the phospholipids in the tumor cell membrane, SapC fuses with the membrane and is internalized leading to its accumulation within the internal membrane. SapC becomes active in the acidic tumor microenvironment and as a lysosomal sphingolipid activator protein, activates lysosomal enzymes, such as beta-glucosidase, acid sphingomyelinase, and beta-galactosylceramidase. This leads to the degradation of glucosylceramide and sphingomyelin, and the conversion of galactosylceramide to ceramide, respectively. This elevates intracellular ceramide levels, activates caspases and induces ceramide-mediated apoptosis, which together lead to an inhibition of tumor cell growth. SapC plays key roles in lipid transport and organization of biological membranes and has strong lipid membrane binding activity. Check for active clinical trials using this agent. (NCI Thesaurus)
Byetta: (Other name for: exenatide)