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Dictionary of drugs:B

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Dictionary of pharmaceutical drugs/medications sorted alphabetically

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Dictionary of drugs B

  • B16alphaGal melanoma vaccine A whole cell melanoma cancer vaccine with potential immunostimulating and antineoplastic activities. B16alphaGal melanoma vaccine contains three types of human melanoma cell lines that are genetically engineered to express the alpha(1,3)-galactosyl (alphaGal) epitope on cell surfaces. The agent stimulates a hyperacute rejection of whole melanoma cancer cells expressing alphaGal epitopes, initiated by opsonization by anti-alphaGal antibodies and followed by antibody-dependent cell-mediated cytotoxicity (ADCC) and cell lysis. This results in the stimulation of a broader cytotoxic T-lymphocyte response (CTL) directed against tumor antigens on melanoma cells that do not express alphaGal. AlphaGal is not normally expressed in humans because alpha(1,3)-galactosyltransferase (Alpha-GT), the enzyme that catalyzes the synthesis of alphaGal epitopes on glycoproteins and glycolipids, is not naturally present in humans and other primates.
  • B43-PAP immunotoxin A mouse-derived anti-human CD19 monoclonal antibody linked to pokeweed (Phytolacca americana) antiviral protein (PAP) with antileukemic activity. The monoclonal antibody portion specifically binds to the CD19 antigen, a cell surface molecule normally expressed only by B lymphocytes and follicular dendritic cells and over-expressed in B-lineage lymphocytic leukemia cells. Following internalization, PAP, a plant hemitoxin and a ribosome-inactivating protein, is cleaved from the immunoconjugate and released into the cytoplasm where it enzymatically removes a single adenine base from a conserved, surface exposed loop sequence of rRNA leading to inhibition of protein synthesis and cell growth, but not necessarily cell death.
  • B7-DC cross-linking antibody rHIgM12B7 A recombinant form of the monoclonal IgM antibody M12 isolated from a Waldenstrom macroglobulinaemia patient (rHIgM12) with potential immunomodulating activity. B7-DC cross-linking antibody rHIgM12B7 binds and crosslinks the B7 co-stimulatory family member B7-DC (PD-L2) on dendritic cells (DCs), antigen presenting cells (APCs) that play a crucial role in the human immune response. This results in enhanced activation of DCs; enhanced antigen-presenting activity; and increased production of immunomodulatory cytokines (especially interleukin 12); and may potentiate a specific cytotoxic T lymphocyte (CTL) response against Waldenstrom macroglobulinaemia B cells.
  • babaodan capsule An orally available mixed powder of traditional Chinese medicine containing eight constituents including natural calculus bovis, snake gall, antelope horn, pearl, musk, radix notoginseng, and other as of yet not disclosed ingredients, with potential antifibrotic, immunomodulatory, and antineoplastic activities. Upon oral administration, babaodan may ameliorate substance-induced liver injury and fibrosis, and inhibit lipopolysaccharide (LPS)-induced hepatic stellate cell (HSC) activation and proliferation through toll-like receptor 4 (TLR4)/nuclear factor-kappa B and TLR4/extracellular-signal-regulated kinase (ERK) pathways. Babaodan may, through an as of yet not elucidated mechanism, enhance the efficacy of chemotherapeutic drugs and may inhibit the occurrence and development of certain tumor types. Check for active clinical trialsusing this agent.
  • bacitracin A complex of cyclic polypeptide antibiotics, mainly bacitracin A, produced by spore-forming organisms belonging to the licheniformin group of the Bacillus subtilis with antibacterial activity. Bacitracin binds to C55-isoprenyl pyrophosphate, a biphosphate lipid transport molecule that carries the building blocks of the peptidoglycan bacterial cell wall. The binding interferes with the enzymatic dephosphorylation of the C55-isoprenyl pyrophosphate and prevents peptidoglycan synthesis, thereby inhibiting bacterial cell growth.
  • baclofen A synthetic chlorophenyl-butanoic acid derivative with muscle relaxant activity. Baclofen acts as a gamma-aminobutyric acid (GABA) agonist specific for GABA-B receptors in the central nervous system (CNS). At spinal and supraspinal sites, this agent reduces excitatory transmission.
  • baclofen/amitriptyline/ketamine gel A topical preparation of baclofen, amitriptyline, and ketamine compounded in a penetration-enhancing polaxamer-lecithin organogel (PLO) with potential antineuralgic activity. The gamma-aminobutyric acid (GABA) analogue baclofen appears to activate the inhibitory GABA(B) receptor, a G protein-coupled receptor, which may result in hyperpolarization of the neuronal cell membrane and inhibition of neurotransmitter release. Amitriptyline likely produces antineuralgic effects via modulation of multiple subtypes of glutamate (Glu) receptors, independent of its antidepressant actions. Ketamine displays complex pharmacologic actions including biogenic amine uptake inhibition, interaction with opioid receptors, and inhibition of N-methyl D-aspartate (NMDA) receptors. Stimulation of GABA(B) receptor activity, modulation of Glu receptor activity, and inhibition of NMDA receptor activity may be of benefit in managing neuropathic pain.
  • bacteriophage phi X 174 A bacteriophage that infects E. coli. Its genome is a circular DNA of 5386 bases.
  • Bactrim Brand name for trimethoprim-sulfamethoxazole
  • bafetinib An orally bioavailable 2-phenylaminopyrimidine derivative with potential antineoplastic activity. Bafetinib specifically binds to and inhibits the Bcr/Abl fusion protein tyrosine kinase, an abnormal enzyme produced by Philadelphia chromosomal translocation associated with chronic myeloid leukemia (CML). This agent also inhibits the Src-family member Lyn tyrosine kinase, upregulated in imatinib-resistant CML cells and in a variety of solid cancer cell types. The inhibitory effect of bafetinib on these specific tyrosine kinases may decrease cellular proliferation and induce apoptosis in tumor cells that overexpress these kinases. CML patients may be refractory to imatinib, which sometimes results from point mutations occurring in the kinase domain of the Bcr/Abl fusion product. Due to its dual inhibitory activity, the use of bafetinib has been shown to overcome this particular drug resistance.
  • Bag Balm Brand name for 8-hydroxyquinoline sulfate ointment
  • balanced crystalloid solution A multiple electrolyte, isotonic, crystalloid solution for intravenous infusion containing sodium chloride, sodium gluconate, sodium acetate, potassium chloride and magnesium chloride, which can restore electrolyte balance, normalize pH, and provide hydration. Upon intravenous administration, the balanced crystalloid solution will replace lost body fluids and electrolytes thereby providing hydration, normalizing electrolyte concentrations and regulating acid-base balance.
  • balixafortide An orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Balixafortide 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.
  • baltaleucel-T A preparation of autologous Epstein-Barr virus (EBV)-specific cytotoxic T lymphocytes (CTLs), which have specific reactivity to the EBV antigens, latent membrane proteins (LMP) 1 (LMP1) and 2 (LMP2), EBV nuclear antigen (EBNA) and BamHI-A rightward frame-1 (BARF1), with potential immunomodulating and antineoplastic activities. Upon administration, baltaleucel-T targets and binds to EBV-expressing cancer cells specifically expressing the targeted antigens. This may kill LMP1/LMP2/EBNA/BARF1-expressing EBV-associated cancer cells. LMP1, LMP2, EBNA and BARF1 are tumor-associated antigens (TAAs) that are specifically associated with EBV infection, and play key roles in the proliferation of a variety of tumors.
  • Balversa Brand name for erdafitinib
  • Balziva Brand name for ethinyl estradiol/norethindrone
  • banoxantrone A bioreductive, alkylaminoanthraquinone prodrug with antineoplastic activity. Under hypoxic conditions, often seen in solid tumors, banoxantrone (AQ4N) is converted and activated by cytochrome P450 enzymes, which are upregulated in certain tumors, to the cytotoxic DNA-binding agent AQ4. Banoxantrone intercalates into and crosslinks DNA, and inhibits topoisomerase II. This results in an inhibition of DNA replication and repair in tumor cells. Combined with conventional therapeutic agents, both oxygenic and hypoxic regions of tumors can be targeted.
  • Baraclude Brand name for entecavir
  • barasertib An orally bioavailable, small-molecule, dihydrogen phosphate prodrug of the pyrazoloquinazoline Aurora kinase inhibitor AZD1152–hydroxyquinazoline pyrazol anilide (AZD1152-HQPA) with potential antineoplastic activity. Upon administration and rapid conversion from the prodrug form in plasma, barasertib specifically binds to and inhibits Aurora kinase B, which results in the disruption of spindle checkpoint functions and chromosome alignment and, so, the disruption of chromosome segregation and cytokinesis. Consequently, cell division and cell proliferation are inhibited and apoptosis is induced in Aurora kinase B-overexpressing tumor cells. Aurora kinase B, a serine/threonine protein kinase that functions in the attachment of the mitotic spindle to the centromere, is overexpressed in a wide variety of cancer cell types.
  • bardoxolone A synthetic triterpenoid compound with potential antineoplastic and anti-inflammatory activities. Bardoxolone blocks the synthesis of inducible nitric oxide synthase (iNOS) and inducible cyclooxygenase (COX-2), two enzymes involved in inflammation and carcinogenesis. This agent also inhibits the interleukin-1 (IL-1)-induced expression of the pro-inflammatory proteins matrix metalloproteinase-1 (MMP-1) and matrix metalloproteinase-13 (MMP-13) and the expression of Bcl-3; Bcl-3 is an IL-1-responsive gene that preferentially contributes to MMP-1 gene expression.
  • baricitinib An orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. Upon administration, baricitinib binds to JAK1/2, which inhibits JAK1/2 activation and leads to the inhibition of the JAK-signal transducers and activators of transcription (STAT) signaling pathway. This decreases the production of inflammatory cytokines and may prevent an inflammatory response. In addition, baricitinib may induce apoptosis and reduce proliferation of JAK1/2-expressing tumor cells. JAK kinases are intracellular enzymes involved in cytokine signaling, inflammation, immune function and hematopoiesis; they are also upregulated and/or mutated in various tumor cell types.
  • barium sulfate The sulfate salt of barium, an alkaline, divalent metal. Barium sulfate is quite insoluble in water, and is used as a radiopaque agent to diagnose gastrointestinal medical conditions. Barium sulfate is taken by mouth or given rectally.
  • Barseb HC Brand name for therapeutic hydrocortisone
  • Basen Brand name for voglibose
  • basiliximab A recombinant, chimeric, human-murine monoclonal antibody directed against the alpha subunit of the interleukin-2 receptor (IL-2R alpha) with immunosuppressant activity. Basiliximab selectively binds to and blocks IL-2R alpha, expressed on the surface of activated T-lymphocytes, thereby preventing interleukin-2 binding and inhibiting the interleukin-2-mediated activation of lymphocytes. Check for active clinical trialsusing this agent.
  • batabulin sodium A synthetic pentafluorophenylsulfonamide with potential antineoplastic activity. Batabulin sodium covalently binds to and selectively modifies the beta 1, beta 2, beta 3, and beta 4 isotypes of beta tubulin at a conserved cysteine residue, resulting in disruption of microtubule polymerization, collapse of the cytoskeleton, an increase in chromosomal ploidy, cell cycle arrest, and tumor cell apoptosis.
  • Bavencio Brand name for avelumab
  • bavituximab An IgG3 monoclonal antibody directed against anionic phospholipids with potential antineoplastic activity. Chimeric anti-phosphotidylserine monoclonal antibody binds to anionic phospholipids in a beta 2-glycoprotein I-dependent manner, inhibiting tumor growth by stimulating antibody-dependent cellular cytotoxicity (ADCC) to tumor vessels.
  • BAY 56-3722 A water-soluble camptothecin derivative conjugated to a carbohydrate moiety exhibiting antineoplastic activity. BAY 56-3722 stabilizes the topoisomerase I-DNA covalent complex and forms an enzyme-drug-DNA ternary complex. As a consequence of the formation of this complex, both the initial cleavage reaction and religation steps are inhibited and subsequent collision of the replication fork with the cleaved strand of DNA results in inhibition of DNA replication, double strand DNA breakage and triggering of apoptosis. The peptide carbohydrate moiety of this agent stabilizes the lactone form of camptothecin in blood.
  • BayGam Brand name for therapeutic immune globulin
  • bazedoxifene An indole derivative and third-generation selective estrogen receptor modulator (SERM) with potential antineoplastic activity. Upon administration, bazedoxifene specifically binds to estrogen receptors in responsive tissues, including liver, bone, breast, and endometrium. The resulting ligand-receptor complex is translocated to the nucleus where, depending on the tissue type, it either promotes or suppresses the transcription of estrogen-regulated genes. Bazedoxifene acts as an estrogen antagonist in uterine and breast tissue, thereby blocking the proliferative effects of estrogen-binding to ER-positive cells in these tissues. Bazedoxifene functions as an estrogen agonist in lipid metabolism, thereby decreasing total and LDL cholesterol levels. In bone, it decreases bone resorption and bone turnover and increases bone mineral density.
  • BC-819 plasmid/polyethylenimine complex A plasmid DNA encoding for the A fragment of Diphtheria Toxin (DTA) under the control of the H19 gene promoter (BC-819 or DTA-H19) and mixed with the transfectant polyethylenimine (PEI), with potential antineoplastic activity. Upon administration, the PEI moiety enhances the entry of the agent into rapidly dividing cells. Upon cell entry, activation of the H19 gene promoter-containing plasmids and DTA expression are limited to tumor cells, as high levels of H19 expression are only found in tumor cells. DTA disrupts protein synthesis. Tumor-cell selective expression of this toxin leads to the selective destruction of the tumor while sparing healthy, normal cells. H19, an oncofetal, regulatory RNA, is overexpressed in certain cancer cells while its expression in normal cells is minimal or absent; it plays a key role in cancer progression, angiogenesis and metastasis.
  • BCG solution A solution containing an attenuated, live culture preparation of the Bacillus Calmette Guerin (BCG) strain of Mycobacterium bovis with potential immunostimulating activity. Although the precise mechanism of action is unknown, upon intravesical administration, attenuated, live BCG bacteria in the solution come into direct contact with the bladder wall, inciting an antitumor granulomatous inflammatory reaction.
  • BCG Tokyo-172 strain solution A solution containing an attenuated, live culture preparation of the bacillus Calmette-Guerin (BCG) strain of Mycobacterium bovis obtained from the Pasteur Institute in 1924, with potential immunostimulating and antineoplastic activities. Although the precise mechanism of action is unknown, upon intravesical instillation through a catheter, the attenuated, live BCG bacteria in the BCG Tokyo-172 strain solution come into direct contact with the bladder wall and elicits a local, multifaceted immune response against the BCG antigens, which kills the bladder cancer cells. Previous vaccination with a systemic BCG vaccine may enhance the immune system's response against the BCG antigens.
  • BCG Tokyo-172 strain vaccine A vaccine containing bacillus Calmette-Guerin (BCG), a live, attenuated strain of Mycobacterium bovis obtained from the Pasteur Institute in 1924, with non-specific immunoadjuvant and immunotherapeutic activities. Upon intradermal administration, BCG Tokyo-172 strain vaccine activates the immune system and enhances a specific, systemic BCG antigen immune response. This results in active immunization against tuberculosis and primes the immune system against future administered BCG antigens.
  • BCG vaccine A vaccine containing bacillus Calmette-Guerin (BCG), an attenuated strain of Mycobacterium bovis, with non-specific immunoadjuvant and immunotherapeutic activities. Although the mechanism of its anti-tumor activity is unclear, immunization with BCG vaccine likely activates a Th1 cytokine response that includes the induction of interferon. Vaccination with BCG vaccine may be immunoprotective against infection with Mycobacterium tuberculosis.
  • Bcl-2 inhibitor APG 2575 An orally bioavailable and selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon oral administration, Bcl-2 inhibitor APG 2575 targets, binds to and inhibits the activity of Bcl-2. This restores apoptotic processes in tumor cells. Bcl-2 is overexpressed in many cancers and plays an important role in the negative regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival. Check for active clinical trialsusing this agent.
  • Bcl-2 inhibitor BCL201 A selective inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon administration, Bcl-2 inhibitor BCL201 binds to and inhibits the activity of Bcl-2. This restores apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in many cancers and plays an important role in the negative regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival.
  • Bcl-2 inhibitor S65487 An inhibitor of the anti-apoptotic protein B-cell lymphoma 2 (Bcl-2), with potential pro-apoptotic and antineoplastic activities. Upon intravenous administration, Bcl-2 inhibitor S65487 binds to and inhibits the activity of Bcl-2, thereby restoring apoptotic processes in tumor cells. Bcl-2 protein is overexpressed in many cancer types and plays an important role in the negative regulation of apoptosis; its expression is associated with increased drug resistance and tumor cell survival.
  • Bcl-2/Bcl-XL inhibitor APG-1252 A Bcl-2 homology (BH)-3 mimetic and selective inhibitor of the anti-apoptotic proteins B-cell lymphoma 2 (Bcl-2) and Bcl-XL, with potential pro-apoptotic and antineoplastic activities. Upon administration, Bcl-2/Bcl-XL inhibitor APG-1252 specifically binds to and inhibits the activity of the pro-survival proteins Bcl-2 and Bcl-XL. This restores apoptotic processes and inhibits cell proliferation in Bcl-2/Bcl-XL-dependent tumor cells. Bcl-2 and Bcl-XL, proteins belonging to the Bcl-2 family that are overexpressed in many cancers, play an important role in the negative regulation of apoptosis; tumor expression is associated with increased drug resistance and cancer cell survival.
  • BCMA x CD3 T-cell-engaging antibody CC-93269 A bispecific T-cell engager (BiTE) antibody composed of two single-chain variable fragments (scFv), one directed against the tumor-associated antigen (TAA) human B-cell maturation antigen (BCMA; TNFRSF17), and one that is directed against the CD3 antigen found on T lymphocytes, with potential immunostimulating and antineoplastic activities. Upon administration of anti-BCMA/CD3 T-cell engaging antibody CC-93269, this bispecific antibody binds to both CD3 on cytotoxic T lymphocytes (CTLs) and BCMA found on BCMA-expressing tumor cells. This activates and redirects CTLs to BCMA-expressing tumor cells, which results in the CTL-mediated death of BCMA-expressing tumor cells. BCMA, a member of the tumor necrosis factor receptor superfamily that is specifically overexpressed on malignant plasma cells, plays a key role in promoting plasma cell survival.
  • BCMA-specific CAR-expressing T lymphocytes A preparation of autologous peripheral blood T-lymphocytes (PBTL) that have been genetically modified to express a chimeric antigen receptor (CAR) specific for the B cell maturation antigen (BCMA), with potential immunostimulating and antineoplastic activities. Upon administration, BCMA-specific CAR-expressing T-lymphocytes specifically recognize and kill BCMA-expressing tumor cells. BCMA, a tumor specific antigen and a receptor for both a proliferation-inducing ligand and B-cell activating factor, is a member of the tumor necrosis factor (TNF) receptor superfamily and plays a key role in plasma survival; it is found on the surfaces of plasma cells and overexpressed on malignant plasma cells.
  • bcr-abl (b2a2)-derived peptide vaccine A peptide vaccine consisting of the bcr-abl b2a2 fusion oncoprotein, frequently expressed in chronic myelogenous leukemia (CML), with potential antineoplastic activity. Vaccination with the bcr-abl (b2a2)-derived peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl b2a2 fusion protein. Fusion genes in CML typically result from the fusion of either BCR exon b2 or BCR exon b3 to ABL exon a2, a 'b3a2' or a 'b2a2' fusion.
  • bcr-abl (b3a2)-derived peptide vaccine A peptide vaccine consisting of the bcr-abl b3a2 fusion oncoprotein, frequently expressed in chronic myelogenous leukemia (CML), with potential antineoplastic activity. Vaccination with the bcr-abl (b3a2)-derived peptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl b3a2 fusion protein. Fusion genes in CML typically result from the fusion of either BCR exon b2 or BCR exon b3 to ABL exon a2, a 'b3a2' or a 'b2a2' fusion.
  • Bcr-Abl kinase inhibitor K0706 An orally bioavailable, Bcr-Abl tyrosine kinase inhibitor (TKI), with potential antineoplastic activity. Upon administration, Bcr-Abl kinase inhibitor K0706 selectively targets and binds to the Bcr-Abl fusion oncoprotein, including various Bcr-Abl mutant forms, such as those with the ‘gatekeeper’ resistance mutation T315I. This inhibits proliferation of Bcr-Abl-expressing tumor cells. The Bcr-Abl fusion protein is an aberrantly activated tyrosine kinase produced by certain leukemia cells. T315I, a threonine (T) to isoleucine (I) amino acid substitution at position 315 in the tyrosine-protein kinase ABL1 portion of the Bcr-Abl fusion protein, plays a key role in resistance to certain chemotherapeutic agents, and its expression is associated with poor prognosis.
  • Bcr-Abl kinase inhibitor PF-114 An orally bioavailable, Bcr-Abl tyrosine kinase inhibitor, with potential antineoplastic activity. Designed to overcome resistance of tumor cells to second generation Bcr-Abl inhibitors, PF-114 targets and binds to the Bcr-Abl fusion oncoprotein, including those fusion proteins with the ‘gatekeeper’ resistance mutation T315I, an amino acid substitution at position 315 in Bcr-Abl from a threonine (T) to an isoleucine (I). This inhibits Bcr-Abl-mediated proliferation of, and enhances apoptosis in, Philadelphia chromosome-positive (Ph+) hematologic malignancies. The Bcr-Abl fusion protein is an aberrantly activated tyrosine kinase produced by leukemia cells that contain the Philadelphia chromosome.
  • bcr-abl p210-b3a2 breakpoint-derived multipeptide vaccine A multipeptide vaccine consisting of five peptides derived from the bcr-abl p210-b3a2 breakpoint fusion protein with potential antineoplastic activity. Vaccination with bcr-abl p210-b3a2 breakpoint-derived multipeptide vaccine may stimulate the host immune system to mount a cytotoxic T lymphocyte (CTL) response against tumor cells that express the bcr-abl p210-b3a2 breakpoint fusion protein. In chronic myelogenous leukemia (CML), fusion genes typically result from the fusion of either bcr exon b2 or exon b3 to abl exon a2, resulting in either a b3a2 or a b2a2 gene fusion product.
  • bcr-abl peptide vaccine A multivalent antineoplastic vaccine comprised of the bcr-abl oncogene breakpoint fusion peptide that elicits a bcr-abl specific T-cell immune response.
  • BEACOPP regimen A chemotherapy regimen consisting of bleomycin, etoposide, doxorubicin hydrochloride (Adriamycin), cyclophosphamide, vincristine (Oncovin), procarbazine and prednisone, used for the treatment of advanced-stage Hodgkin lymphoma.
  • Bead Block Compressible Microspheres Brand name for PVA microporous hydrospheres
  • becatecarin A synthetic diethylaminoethyl analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. Becatecarin intercalates into DNA and stabilizes the DNA-topoisomerase I complex, thereby interfering with the topoisomerase I-catalyzed DNA breakage-reunion reaction and initiating DNA cleavage and apoptosis.
  • beclomethasone dipropionate The dipropionate salt of a synthetic glucocorticoid with anti-inflammatory and immunomodulating properties. After cell surface receptor attachment and cell entry, beclomethasone enters the nucleus where it binds to and activates specific nuclear receptors, resulting in an altered gene expression and inhibition of proinflammatory cytokine production.
  • Beclovent Brand name for beclomethasone dipropionate
  • Beconase Brand name for beclomethasone dipropionate
  • Beesix Brand name for pyridoxine hydrochloride
  • BeetElite NeoShot Brand name for concentrated beet crystals
  • beetroot juice The juice of the beetroot, with potential antioxidant and protective activities. Beetroot juice contains antioxidants, including betacyanin, which scavenge free radicals. In addition, beetroot contains high levels of nitrates and folic acid. Consumption of beetroot juice leads to the conversion of nitrate to nitric oxide (NO) in the body. This juice may have a beneficial effect on blood flow and blood pressure through the induction of NO-mediated vasodilation. Additionally, this agent may decrease fatigue and increase physical performance.
  • Begedina Brand name for begelomab
  • begelomab A monoclonal antibody against the human dipeptidyl peptidase 4 (dipeptidylpeptidase IV, DPPIV, DPP4; CD26), with potential activity against graft-versus-host disease (GvHD). Upon administration, begelomab binds to CD26 expressed on T-cells. This inhibits the stimulation of T-cells and may prevent GvHD. CD26, a membrane-bound glycoprotein with dipeptidyl peptidase activity, plays a key role in T-cell activation and immune regulation.
  • belagenpumatucel-L A transforming growth factor beta2 (TGF-beta2) antisense gene-modified allogeneic tumor cell vaccine with potential immunostimulatory and antineoplastic activities. Belagenpumatucel-L is prepared by transfecting allogeneic non-small cell lung cancer (NSCLC) cells with a plasmid containing a TGF-beta2 antisense transgene, expanding the cells, and then irradiating and freezing them. Upon administration, this agent may elicit a cytotoxic T lymphocyte (CTL) response against host NSCLC cells, resulting in decreased tumor cell proliferation; vaccine immunogenicity may be potentiated by suppression of tumor TGF-beta2 production by antisense RNA expressed by the vaccine plasmid TGF-beta2 antisense transgene. Elevated levels of TGF-beta2 are frequently linked to immunosuppression in cancer patients and may be inversely correlated with prognosis in patients with NSCLC.
  • Beleodaq Brand name for belinostat
  • belimumab A fully human IgG1 monoclonal antibody directed against B-Lymphocyte stimulator protein (BlyS or TNFSF13B) with potential immunomodulating activity. Belimumab specifically recognizes and inhibits the biological activity of BlyS, thereby preventing the binding of BlyS to B-lymphocytes. This inhibits the maturation of B-lymphocytes and may induce apoptosis in B-lymphocytes. In addition, it may decrease B-lymphocyte proliferation and/or survival. BlyS, a member of TNF family supporting B-lymphocyte maturation and survival, has been implicated in the pathogenesis of autoimmune diseases and B-lymphocyte malignancies. Check for active clinical trialsusing this agent.
  • belinostat A novel hydroxamic acid-type histone deacetylase (HDAC) inhibitor with antineoplastic activity. Belinostat targets HDAC enzymes, thereby inhibiting tumor cell proliferation, inducing apoptosis, promoting cellular differentiation, and inhibiting angiogenesis. This agent may sensitize drug-resistant tumor cells to other antineoplastic agents, possibly through a mechanism involving the down-regulation of thymidylate synthase.
  • belotecan hydrochloride The hydrochloride salt of the semi-synthetic camptothecin analogue belotecan with potential antitumor activity. Belotecan binds to and inhibits the activity of topoisomerase I, stabilizing the cleavable complex of topoisomerase I-DNA, which inhibits the religation of single-stranded DNA breaks generated by topoisomerase I; lethal double-stranded DNA breaks occur when the topoisomerase I-DNA complex is encountered by the DNA replication machinery, DNA replication is disrupted, and the tumor cell undergoes apoptosis. Topoisomerase I is an enzyme that mediates reversible single-strand breaks in DNA during DNA replication.
  • bemarituzumab A glycoengineered, humanized monoclonal antibody directed against the fibroblast growth factor receptor type 2b (FGFR2b), with potential antineoplastic activity. Upon administration, bemarituzumab specifically binds to and inhibits FGFR2b on tumor cell surfaces, which prevents FGFR2 from binding to its ligands, FGFR2b activation and the activation of FGFR2b-mediated signal transduction pathways. The binding of bemarituzumab to FGFR2b protein also induces antibody-dependent cell-mediated cytotoxicity (ADCC) against FGFR2b-expressing tumor cells. This results in the inhibition of cell proliferation and the induction of cell death of FGFR2-expressing tumor cells. FGFR2b, a specific isoform of the receptor tyrosine kinase FGFR2 upregulated in many tumor cell types, is essential to tumor proliferation, differentiation and survival. Glycoengineering enhances the FPA144-mediated ADCC.
  • bemiparin sodium The sodium salt of bemiparin, a second generation, synthetic, low-molecular-weight heparin (LMWH) with anticoagulant activity. Derived, after depolymerisation and fractionation, from medical-grade porcine unfractionated heparin (UFH), bemiparin has an average molecular weight of 3,600 daltons and has a higher anti-factor Xa/anti-factor IIa ratio (8:1) than first-generation LMWHs. This anticoagulant binds to antithrombin III, thereby enhancing the inactivation of activated Factor X (Factor Xa) and, to a lesser extent, activated factor II (Factor IIa). Compared to unfractionated heparins, the use of bemiparin is associated with lower incidences of major bleeding, osteoporosis, and heparin-induced thrombocytopenia. Bemiparin also promotes a greater release of tissue factor pathway inhibitor than UFH or dalteparin.
  • Benadryl Brand name for diphenhydramine hydrochloride
  • benazepril hydrochloride The hydrochloride salt of benazepril, a carboxyl-containing angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. As a prodrug, benazepril is metabolized to its active form benazeprilat. Benazeprilat competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II, resulting in vasodilation. Benazeprilat also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow.
  • bendamustine hydrochloride The hydrochloride salt of bendamustine, a bifunctional mechlorethamine derivative with alkylator and antimetabolite activities. Bendamustine possesses three active moieties: an alkylating group; a benzimidazole ring, which may act as a purine analogue; and a butyric acid side chain. Although its exact mechanism of action is unknown, this agent appears to act primarily as an alkylator. Bendamustine metabolites alkylate and crosslink macromolecules, resulting in DNA, RNA and protein synthesis inhibition, and, subsequently, apoptosis. Bendamustine may differ from other alkylators in that it may be more potent in activating p53-dependent stress pathways and inducing apoptosis; it may induce mitotic catastrophe; and it may activate a base excision DNA repair pathway rather than an alkyltransferase DNA repair mechanism. Accordingly, this agent may be more efficacious and less susceptible to drug resistance than other alkylators.
  • bendamustine-containing nanoparticle-based formulation RXDX-107 A nanoparticle-based formulation containing the alkyl ester of bendamustine, a bifunctional mechlorethamine derivative, encapsulated in human serum albumin (HSA), with potential alkylating and antineoplastic activities. Upon administration of the alkyl ester bendamustine-containing nanoparticle formulation RXDX-107, the nanoparticle formulation permits high concentrations of the alkyl ester of bendamustine be localized at the tumor site. The modified bendamustine alkylates and crosslinks macromolecules, resulting in DNA, RNA and protein synthesis inhibition, and, subsequently, apoptosis.
  • bendamustine-vorinostat fusion molecule EDO-S101 An alkylating histone-deacetylase inhibitor (HDACi) fusion molecule composed of the alkylating agent bendamustine fused to the pan-HDACi vorinostat, with potential bi-functional antineoplastic activity. Upon administration of the bendamustine-vorinostat fusion molecule EDO-S101, the vorinostat moiety targets and binds to HDACs. This leads to an accumulation of highly acetylated histones, which results in an induction of chromatin remodeling, a modulation of gene expression, an inhibition of tumor cell division and the induction of tumor cell apoptosis. The bendamustine moiety binds to, alkylates and crosslinks macromolecules, inhibiting DNA, RNA and protein synthesis, which also results in tumor cell apoptosis. Thus, EDO-S101 shows superior efficacy compared to the activity of either agent alone. In addition, the inhibition of HDAC6 activity by EDO-S101 induces the activation of inositol-requiring enzyme 1 (IRE-1), the key regulatory protein for the unfolded protein response (UPR). Induction of the UPR increases the sensitivity of certain cancer cell types to certain chemotherapeutic agents, such as proteasome inhibitors. Therefore, EDO-S101 may work synergistically with proteasome inhibitors. HDACs, enzymes that deacetylate chromatin histone proteins, are overexpressed in various cancers and play a key role in proliferation and resistance of tumor cells. Check for active clinical trialsusing this agent.
  • Bendeka Brand name for bendamustine hydrochloride
  • Bendopa Brand name for levodopa
  • Benefin Brand name for shark cartilage
  • benegrastim A recombinant dimeric fusion peptide of the human granulocyte colony-stimulating factor (G-CSF; filgrastim), with immunomodulating and hematopoietic activities. Benegrastim binds to the cell surface G-CSF receptors (G-CSFRs) inducing receptor dimerization and activation of signaling cascades such as the Jak-STAT and mitogen-activated protein kinase pathways. This stimulates neutrophil progenitor proliferation and differentiation. Compared to other preparations of monomer recombinant G-CSF, dimeric filgrastim may allow for stronger activation of G-CSFRs and a faster myeloid precursor response thus enhancing neutrophil recovery upon myelosuppressive therapy.
  • Benemid Brand name for probenecid
  • Beneo Synergy 1 Brand name for oligofructose-enriched inulin
  • Benlysta Brand name for belimumab
  • Benoquin Brand name for monobenzone
  • benralizumab An afucosylated, humanized monoclonal antibody against the alpha chain of the interleukin-5 receptor (IL-5Ra), with potential anti-asthmatic activity. Upon administration, benralizumab binds to IL-5Ra and elicits an antibody-directed cell cytotoxicity (ADCC) against IL-5Ra-expressing cells. This induces apoptosis in IL-5Ra-expressing cells and may reduce asthmatic episodes. IL-5Ra, expressed on both eosinophils and basophils, plays a key role in asthma.
  • benzaldehyde dimethane sulfonate A dimethane sulfonate derivative and alkylating agent with a structure similar to other alkylating agents such as chlorambucil, busulfan and melphalan, with potential antineoplastic activity. Although the exact mechanism of action has yet to be fully elucidated, benzaldehyde dimethane sulfonate alkylates DNA, which results in DNA double strand breaks, inhibition of DNA replication, cell cycle arrest and cell death. In addition, this agent is metabolized by the enzyme aldehyde dehydrogenase (ALDH) into the active carboxylic acid metabolite benzoic acid dimethane sulfonate (BA), which further contributes to its alkylating activity. Unlike other alkylating agents, benzaldehyde dimethane sulfonate has demonstrated antitumor activity in renal cell carcinoma.
  • benzoylphenylurea A low molecular weight agent with antineoplastic activity. Benzoylphenylurea binds to the colchicine binding site on tubulin, thereby blocking tubulin polymerization and disrupting mitotic function. This agent also inhibits DNA polymerase, and has been shown to arrest leukemia cells in the G1-S transition phase of the cell cycle.
  • benzydamine hydrochloride An indazole non-steroidal anti-inflammatory drug (NSAID) with analgesic, antipyretic, and anti-edema properties. Unlike other NSAIDs, benzydamine hydrochloride does not inhibit cyclooxygenases (COX) but stabilizes membranes, resulting in local anesthesia; inhibits the production of pro-inflammatory cytokines; inhibits the generation of reactive oxygen species by neutrophils; inhibits leukocyte aggregation and adhesion; and exhibits antimicrobial properties.
  • BEP regimen A chemotherapy regimen consisting of bleomycin, etoposide and cisplatin used for the treatment of ovarian and testicular germ cell tumors (GCTs).
  • berberine chloride The orally bioavailable, hydrochloride salt form of berberine, a quaternary ammonium salt of an isoquinoline alkaloid and active component of various Chinese herbs, with potential antineoplastic, radiosensitizing, anti-inflammatory, anti-lipidemic and antidiabetic activities. Although the mechanisms of action through which berberine exerts its effects are not yet fully elucidated, upon administration this agent appears to suppress the activation of various proteins and/or modulate the expression of a variety of genes involved in tumorigenesis and inflammation, including, but not limited to transcription factor nuclear factor-kappa B (NF-kB), myeloid cell leukemia 1 (Mcl-1), B-cell lymphoma 2 (Bcl-2), B-cell lymphoma-extra large (Bcl-xl), cyclooxygenase (COX)-2, tumor necrosis factor (TNF), interleukin (IL)-6, IL-12, inducible nitric oxide synthase (iNOS), intercellular adhesion molecule-1 (ICAM-1), E-selectin, monocyte chemoattractant protein-1 (MCP-1), C-X-C motif chemokine 2 (CXCL2), cyclin D1, activator protein (AP-1), hypoxia-inducible factor 1 (HIF-1), signal transducer and activator of transcription 3 (STAT3), peroxisome proliferator-activated receptor (PPAR), arylamine N-acetyltransferase (NAT), and DNA topoisomerase I and II. The modulation of gene expression may induce cell cycle arrest and apoptosis, and inhibit cancer cell proliferation. In addition, berberine modulates lipid and glucose metabolism.
  • berubicin hydrochloride The hydrochloride salt of the anthracycline derivative berubicin with potential antineoplastic activity. Berubicin intercalates into DNA and interrupts topoisomerase II activity, resulting in the inhibition of DNA replication and repair, and RNA and protein synthesis. Unlike other anthracycline derivatives, this agent crosses the blood-brain barrier (BBB).
  • Berubigen Brand name for cyanocobalamin
  • Besponsa Brand name for inotuzumab ozogamicin
  • BET bromodomain inhibitor ZEN-3694 An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor ZEN-3694 binds to the acetylated lysine recognition motifs in the bromodomains of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.
  • BET bromodomains 2/3/4 inhibitor MK-8628 A synthetic, small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins 2, 3 and 4 with potential antineoplastic activity. Upon administration, the BET bromodomains 2, 3 and 4 inhibitor MK-8628 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes, including c-Myc-dependent target genes, may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, the BET proteins BRD2, BRD3, BRD4 are transcriptional regulators that play an important role in cellular growth.
  • BET inhibitor ABBV-744 An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor ABBV-744 preferentially binds to the second bromodomain (BD2) of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that contain two homologous bromodomains, the BD1 and BD2 domains. They play an important role during development and cellular growth.
  • BET inhibitor BAY1238097 An inhibitor of the Bromodomain (BRD) and Extra-Terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BAY1238097 binds to the acetylated lysine recognition motifs on the BRD of BET proteins, thereby preventing the interaction between BET proteins and histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes. This leads to an inhibition of tumor cell growth. BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that bind to acetylated lysines on the tails of histones H3 and H4, and regulate chromatin structure and function; they play an important role in the modulation of gene expression during development and cellular growth.
  • BET inhibitor BMS-986158 An inhibitor of the bromodomain (BRD) and extra-terminal domain (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor BMS-986158 binds to the acetyl-lysine binding site in the BRD of BET proteins, thereby preventing the interaction between BET proteins and acetylated histones. This disrupts chromatin remodeling and prevents the expression of certain growth-promoting genes, resulting in an inhibition of tumor cell growth. BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that bind to acetylated lysines on the tails of histones H3 and H4, and regulate chromatin structure and function; they play an important role in the modulation of gene expression during development and cellular growth.
  • BET inhibitor CC-90010 An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor CC-90010 preferentially binds to the second bromodomain (BD2) of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that contain two homologous bromodomains, the BD1 and BD2 domains. They play an important role during development and cellular growth.
  • BET inhibitor CPI-0610 A small molecule inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor CPI-0610 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histone peptides. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of two bromodomains at the N-terminus, the BET proteins (BRD2, BRD3, BRD4 and BRDT) are transcriptional regulators that play an important role during development and cellular growth.
  • BET inhibitor FT-1101 An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon administration, the BET inhibitor FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.
  • BET inhibitor GS-5829 An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor GS-5829 binds to the acetylated lysine recognition motifs in the bromodomains of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.
  • BET inhibitor GSK2820151 An orally bioavailable inhibitor of the bromodomain and extra-terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor GSK2820151 binds to the acetylated lysine recognition motifs in the bromodomains of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.
  • BET inhibitor INCB054329 An inhibitor of the bromodomain and extra-terminal (BET) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor INCB054329 binds to the acetylated lysine recognition motifs on the bromodomain of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomain at the N-terminus, BET proteins, BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during cellular growth.
  • BET inhibitor RO6870810 A small molecule inhibitor of the BET (Bromodomain and Extra-Terminal) family of bromodomain-containing proteins with potential antineoplastic activity. Upon administration, the BET inhibitor RO6870810 binds to the acetylated lysine recognition motifs found in the bromodomain of BET proteins, which prevents the interaction between BET proteins and acetylated histones. This interaction disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of tumor cell growth. Characterized by a tandem repeat of bromodomains at the N-terminus, BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during cellular development and growth.
  • beta carotene A naturally-occurring retinol (vitamin A) precursor obtained from certain fruits and vegetables with potential antineoplastic and chemopreventive activities. As an anti-oxidant, beta carotene inhibits free-radical damage to DNA. This agent also induces cell differentiation and apoptosis of some tumor cell types, particularly in early stages of tumorigenesis, and enhances immune system activity by stimulating the release of natural killer cells, lymphocytes, and monocytes.
  • Betadine Brand name for povidone-iodine solution
  • Betadine Solution Brand name for povidone-iodine solution
  • beta-elemene One of the isomers of elemene, a lipid soluble sesquiterpene and the active component isolated from the Chinese medicinal herb Rhizoma zedoariae with potential antineoplastic and chemopreventive activities. Although the exact mechanism of action through which beta-elemene exerts its effect has yet to be fully elucidated, this agent appears to induce apoptosis through different mechanisms of action and induces cell cycle arrest at different stages based on the tumor cell type involved. Beta-elemene may sensitize cancer cells to other chemotherapeutic agents.
  • beta-glucan A polysaccharide isolated from the cell walls of bacteria, plants, and fungi with immunostimulant and antineoplastic activities. In a solubilized form, beta-glucan binds to a lectin site within complement receptor 3 (CR3) on leukocytes, priming the receptor to trigger cytotoxic degranulation of leukocytes when leukocyte CR3 binds to complement 3 (iC3b)-coated tumors. Thus, the attachment of beta-glucan to CR3 of circulating leukocytes simulates leukocytes to kill iC3b-coated tumor cells in the same way as they kill iC3b-coated yeast.
  • beta-glucan MM-10-001 A powder formulation containing a triple helix beta-glucan, isolated from the cell walls of the shiitake mushroom (Lentinula edodes), with potential immunostimulating activity. The beta-glucan in beta-glucan MM-10-001 binds to a lectin site within the complement receptor 3 (CR3 or iC3b receptor) on leukocytes, priming the receptor to trigger cytotoxic degranulation of leukocytes when leukocyte CR3 binds to iC3b-opsonized tumor cells. iC3b is the proteolyticly inactive product of the complement cleavage fragment C3b.
  • beta-glucan/alginate/hyaluronic acid/squalene/avocado oil-containing emulsion A topical emulsion containing beta-glucan (5%), alginate, hyaluronic acid, squalene and avocado oil, with cutaneous protective activity. Upon topical application of beta-glucan/alginate/hyaluronic acid/squalene/avocado oil-containing emulsion, the naturally-occurring polysaccharide beta-glucan acts as an immunomodulator by activating the innate immune response, in particular through the activation of macrophages and migration of neutrophils. Alginate acts as a moisturizer and supports skin healing. Hyaluronic acid, squalene and avocado oil provide barrier protection, help maintain skin integrity and are natural emollients and moisturizers. This emulsion may accelerate wound healing and may prevent radiation-induced dermatitis.
  • beta-glucan/Lactobacillus casei/Bifidobacterium lactis-based supplement A synbiotic supplement containing beta-1,3-glucan, bacteria Lactobacillus casei (L. casei) and Bifidobacterium lactis (B. lactis), with potential immunomodulating activity. The naturally-occurring bacterial components in this dietary supplement may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization of the GI tract, the bacteria may form a protective intestinal barrier, thereby preventing attachment of potential pathogens. Both the probiotics and beta-glucan have been shown to stimulate the immune system. This supplement also contains several vitamins and other insoluble polysaccharides. Check for active clinical trialsusing this agent.
  • beta-hydroxy-beta-methylbutyrate supplement A nutritional supplement containing the active metabolite of the essential amino acid leucine, with potential anti-catabolic and anabolic activities. Upon oral administration of beta-hydroxy-beta-methylbutyrate (HMB), this leucine metabolite may decrease protein breakdown and increase protein synthesis thereby increasing muscle strength and mass. Although the exact mechanisms remain to be fully elucidated, multiple mechanisms have been proposed: 1) HMB is a precursor of cholesterol synthesis in skeletal muscle cells thereby increasing sarcolemmal integrity; 2) HMB may inhibit the ubiquitin-proteasome proteolytic pathway responsible for the specific degradation of intracellular proteins, thereby preventing muscular proteolysis; and/or 3) HMB may stimulate protein synthesis through a mammalian target of rapamycin (mTOR)-mediated mechanism.
  • beta-lapachone A poorly soluble, ortho-naphthoquinone with potential antineoplastic and radiosensitizing activity. Beta-lapachone (b-lap) is bioactivated by NAD(P)H:quinone oxidoreductase-1 (NQO1), creating a futile oxidoreduction that generates high levels of superoxide. In turn, the highly reactive oxygen species (ROS) interact with DNA, thereby causing single-strand DNA breaks and calcium release from endoplasmic reticulum (ER) stores. Eventually, the extensive DNA damage causes hyperactivation of poly(ADP-ribose) polymerase-1 (PARP-1), an enzyme facilitating DNA repair, accompanied by rapid depletion of NAD+/ATP nucleotide levels. As a result, a caspase-independent and ER-stress induced mu-calpain-mediated cell death occurs in NQO1-overexpressing tumor cells. NQO1, a flavoprotein and two-electron oxidoreductase, is overexpressed in a variety of tumors.
  • beta-lapachone prodrug ARQ 761 A synthetic, soluble prodrug of beta-lapachone, a poorly soluble, ortho-naphthoquinone with potential antineoplastic and radiosensitizing activity. ARQ 761 is converted to beta-lapachone (b-lap) in vivo. When b-lap is activated by NAD(P)H:quinone oxidoreductase-1 (NQO1) this agent creates a futile oxidoreduction, generating highly reactive oxygen species (ROS) that results in DNA damage. The activation of b-lap also causes hyperactivation of poly (ADP-ribose) polymerase-1 (PARP-1), an enzyme that facilitates DNA repair, accompanied by rapid depletion of NAD+/ATP nucleotide levels. As a result, a caspase-independent and endoplasmic reticulum (ER) stress-induced mu-calpain-mediated cell death occurs in NQO1-overexpressing tumor cells. In addition, b-lap induces expression of the checkpoints activator E2F transcription factor 1 (E2F1) and thereby activates the E2F1-mediated checkpoint pathway that directly triggers apoptosis. As ARQ 761 is soluble and requires less solvent, this formulation may cause less hemolytic anemia associated with administration of the synthetic b-lap ARQ 501.
  • Betalin 12 Brand name for cyanocobalamin
  • BetaMarc Brand name for formoterol fumarate/roxithromycin
  • betamethasone A synthetic glucocorticoid with metabolic, immunosuppressive and anti-inflammatory activities. Betamethasone binds to specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. The synthesis of certain anti-inflammatory proteins is induced while the synthesis of certain inflammatory mediators is inhibited. As a result, there is an overall reduction in chronic inflammation and autoimmune reactions.
  • beta-thioguanine deoxyriboside A thiopurine nucleoside derivative with antineoplastic activity. After conversion to the triphosphate, beta-thioguanine deoxyriboside is incorporated into DNA, resulting in inhibition of DNA replication. This agent is cytotoxic against leukemia cell lines and has demonstrated some activity against leukemia cells in vivo. Beta-thioguanine deoxyriboside demonstrates antineoplastic activity against 6-thioguanine-resistant tumor cells.
  • BET-bromodomain inhibitor ODM-207 An orally bioavailable inhibitor of the Bromodomain and Extra-Terminal (BET) family of proteins, with potential antineoplastic activity. Upon oral administration, the BET inhibitor ODM-207 binds to the acetylated lysine recognition motifs in the bromodomains of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression of oncogenic drivers that are important for cell proliferation and survival. Prevention of the expression of certain growth-promoting genes may lead to an inhibition of proliferation in BET-overexpressing tumor cells. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that bind to acetylated lysine residues in histones and play an important role during development and cellular growth. In tumor cells, BET proteins play a key role in the regulation of oncogene transcription and tumor cell proliferation.
  • bethanechol chloride A synthetic quaternary ammonium base derivative, parasympathomimetic bethanechol is a slowly hydrolyzed muscarinic agonist with no nicotinic effects. Generally used to increase smooth muscle tone, bethanechol is used to treat reflux esophagitis and to initiate urination after surgery, in urinary infections, or for enlarged prostate. It may cause hypotension, cardiac rate changes, and bronchial spasms. Check for active clinical trialsusing this agent.
  • betrixaban An orally active inhibitor of coagulation factor Xa (activated factor X) with anticoagulant activity. Betrixaban is primarily excreted unchanged in the bile and has a half life of about 19 hours.
  • betulinic acid A pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) with antiinflammatory, anti-HIV and antineoplastic activities. Betulinic acid induces apoptosis through induction of changes in mitochondrial membrane potential, production of reactive oxygen species, and opening of mitochondrial permeability transition pores, resulting in the release of mitochondrial apogenic factors, activation of caspases, and DNA fragmentation. Although originally thought to exhibit specific cytotoxicity against melanoma cells, this agent has been found to be cytotoxic against non-melanoma tumor cell types including neuroectodermal.and brain tumor cells.
  • bevacizumab A recombinant humanized monoclonal antibody directed against the vascular endothelial growth factor (VEGF), a pro-angiogenic cytokine. Bevacizumab binds to VEGF and inhibits VEGF receptor binding, thereby preventing the growth and maintenance of tumor blood vessels.
  • bevacizumab-IRDye 800CW An immunoconjugate and a fluorescent tracer consisting of the recombinant humanized anti-vascular endothelial growth factor (VEGF) monoclonal antibody bevacizumab conjugated to the N-hydroxysuccinamide (NHS) ester form of the near-infrared (NIR) fluorescent dye IRDye 800CW, that may be used for VEGF-specific tumor imaging. Upon administration, the bevacizumab moiety of bevacizumab-IRDye 800CW binds to VEGF and the fluorescent signal can be visualized using NIR fluorescence imaging (700–1,000 nm).
  • Bevyxxa Brand name for betrixaban
  • bexarotene A synthetic retinoic acid agent with potential antineoplastic, chemopreventive, teratogenic and embryotoxic properties. Bexarotene selectively binds to and activates retinoid X receptors (RXRs), thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression.
  • Bextra Brand name for valdecoxib
  • Bexxar Brand name for tositumomab and iodine I 131 tositumomab
  • bezlotoxumab A human monoclonal antibody directed against Clostridium difficile Toxin B (TcdB), with anti-toxin activity. Upon intravenous infusion, the two Fab regions of bezlotoxumab bind to two distinct epitopes within the N-terminal half of the TcdB combined repetitive oligopeptide (CROP) domain, blocking the carbohydrate binding pockets of the toxin and preventing binding of the toxin to target host cells. TcdB is one of two exotoxins responsible for the symptoms of Clostridium difficile infections.
  • BF-200 gel formulation A topical nanoemulsion-based gel formulation containing 5-aminolevulinic acid (ALA), a metabolic precursor of the photosensitizer protoporphyrin IX, with a potential application for enhanced photodynamic therapy (PDT) for various precancerous and malignant skin lesions. After topical administration of a thick layer of the ALA-based BF-200 gel formulation to the affected area, ALA penetrates the skin and is intracellularly converted to protoporphyrin IX (PpIX). Exposure of PpIX to the proper excitation wavelength of light generates singlet oxygen molecules, resulting in a local cytotoxic effect.
  • BH3 mimetic ABT-737 An orally bioavailable, selective small molecule B-cell lymphoma 2 (Bcl-2) Homology 3 (BH3) mimetic, with potential pro-apoptotic and antineoplastic activities. ABT-737 binds to the hydrophobic groove of multiple members of the anti-apoptotic Bcl-2 protein family, including Bcl-2, Bcl-xl and Bcl-w. This inhibits the activity of these pro-survival proteins and restores apoptotic processes in tumor cells, via activation of Bak/Bax-mediated apoptosis. The pro-survival Bcl-2 proteins are overexpressed in many cancers and play important roles in the regulation of apoptosis. Their expression is associated with increased drug resistance and tumor cell survival. ABT-737 does not inhibit the pro-survival proteins Mcl-1, Bcl-B, Bfl-1 (A1); therefore, tumors that overexpress these Bcl-2 family proteins are resistant to ABT-737.
  • BI 2536 A small molecule compound with potential antineoplastic activities. BI 2536 binds to and inhibits Polo-like kinase 1 (Plk1), resulting in mitotic arrest, disruption of cytokinesis, and apoptosis in susceptible tumor cell populations. Plk1, a serine/threonine-protein kinase, is a key regulator of multiple processes fundamental to mitosis and cell division.
  • Biaxin Brand name for clarithromycin
  • BIBX 1382 A pyrimido-pyrimidine with antitumor activity. BIBX 1382 inhibits the intracellular tyrosine kinase domain of the Epidermal Growth Factor Receptor (EGFR) thus specifically reversing the aberrant enzymatic activity from overexpressed and constitutively activated EGFR, and subsequently inhibiting cell proliferation and inducing cell differentiation.
  • bicalutamide A synthetic, nonsteroidal antiandrogen. Bicalutamide competitively binds to cytosolic androgen receptors in target tissues, thereby inhibiting the receptor binding of androgens. This agent does not bind to most mutated forms of androgen receptors.
  • Bicitra Brand name for sodium citrate
  • BiCNU Brand name for carmustine
  • Bifidobacterium animalis/Lactobacillus rhamnosus probiotic supplement An orally bioavailable, probiotic supplement containing the non-pathogenic microorganisms Bifidobacterium animalis and Lactobacillus rhamnosus subspecies lactis with potential immunomodulating, anti-diarrheal and mucosal protective activities. Upon oral ingestion, the naturally-occurring bacterial components in Bifidobacterium animalis/Lactobacillus rhamnosus subspecies lactis probiotic supplement may improve digestion and help to maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. They produce lactic acid, hydrogen peroxide and other substances during fermentation, thereby creating an acidic environment that is unfavorable for pathogens. During colonization in the GI tract, the bacteria may also form a protective intestinal barrier, which may prevent damage to the mucosal epithelium, maintains the integrity of the epithelial barrier from potential damage by toxins and certain chemicals, and reduces the potential for attachment of pathogens. This further protects against bacterial translocation and infection. In addition, this agent may reduce the secretion of pro-inflammatory cytokines and may potentiate natural and acquired immunity. Altogether, this may increase immunity, prevent GI mucosal damage, malabsorption, inflammation, and reduce diarrhea, such as diarrhea induced by inflammation and GI mucosa-damaging agents.
  • Bifidobacterium lactis/Lactobacillus acidophilus/inulin probiotic supplement A tablet probiotic supplement containing the polysaccharide inulin and the non-pathogenic microorganisms Bifidobacterium lactis and Lactobacillus acidophilus, with potential anti-inflammatory, immunomodulating and protective activities. Upon oral administration of B. lactis/L. acidophilus/inulin probiotic supplement, the bacterial components in this dietary supplement may improve digestion and promote adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization in the GI tract, the bacteria may form a protective intestinal barrier that may prevent both damage to the mucosal epithelia caused by toxins and attachment of potential pathogens, which protects against bacterial translocation and infection. In addition, this agent may both reduce the secretion of pro-inflammatory cytokines, including interleukin-10, and potentiate natural and acquired immunity. In colon cancer patients, these probiotic bacteria may favorably modulate the composition of the colon cancer-associated microbiota and may increase expression of tumor-suppressing genes. Inulin promotes growth and activity of beneficial GI bacteria, thereby altering the endogenous flora further.
  • Bifidobacterium lactis/Lactobacillus acidophilus/L. plantarum/L. salivarius probiotic supplement An orally available, probiotic supplement containing the non-pathogenic microorganisms Lactobacillus acidophilus, L. plantarum, L. salivarius and Bifidobacterium lactis, with potential anti-inflammatory, immunomodulating and protective activities. Upon oral ingestion, the naturally-occurring bacterial components in this dietary supplement may improve digestion and help maintain adequate colonization of the gastrointestinal (GI) tract by modulating the composition of the normal microflora. During colonization in the GI tract, the bacteria may form a protective intestinal barrier that may prevent both damage to the mucosal epithelia caused by toxins and attachment of potential pathogens, which protects against bacterial translocation and infections. In addition, this agent may both reduce the secretion of pro-inflammatory cytokines, including interleukin-10, and potentiate natural and acquired immunity.
  • bi-functional alkylating agent VAL-083 A bi-functional alkylating agent, with potential antineoplastic activity. Upon administration, VAL-083 crosses the blood brain barrier (BBB) and appears to be selective for tumor cells. This agent alkylates and crosslinks DNA which ultimately leads to a reduction in cancer cell proliferation. In addition, VAL-083 does not show cross-resistance to other conventional chemotherapeutic agents and has a long half-life in the brain.
  • bifunctional expression vector plasmid DNA-bi-shRNA EWS/FLI1 type 1 lipoplex A proprietary plasmid DNA expression vector encoding bi-functional short hairpin RNAs (bi-shRNAs) targeting the identical type 1 translocation junction region of the human fusion oncogene Ewing sarcoma (EWS)/Ets family transcription factor Friend leukemia virus integration 1 (FLI1) and are encapsulated in liposomal delivery vehicle (lipoplex; LPX), with potential antineoplastic activity. pbi-shRNA EWS/FLI1 type 1 contains 2 stem-loop structures encoded by a plasmid vector: one cleavage-dependent unit with perfectly matched passenger- and guide-strand, which is the small interfering RNA (siRNA)-like component, and one cleavage-independent unit composed of a strategically mismatched double strand, which is the microRNA (miRNA)-like component. Upon intratumoral administration and transcription into tumor cells, one shRNA unit with an imperfectly matched sequence causes inhibition of EWS/FLI1 messenger RNA (mRNA) translation (through mRNA sequestration and cleavage-independent degradation) while the other unit with a perfectly matched sequence promotes EWS/FLI1 mRNA degradation (through cleavage-dependent mRNA silencing). This prevents EWS/FLI1 expression in tumor cells, which results in a reduction of tumor cell proliferation. The EWS/FLI1 type 1 fusion gene product is overexpressed in type 1 Ewing’s sarcoma and correlates with increased tumor proliferation and poor prognosis.
  • bimagrumab A human monoclonal antibody directed against type II activin receptors (ActRII; ActR2), with potential muscle-sparing and anti-cachectic activities. Upon administration, bimagrumab binds to ActRII, which prevents the binding of the natural ligands, myostatin and activin, to activin receptors and blocks ActRII-mediated signaling. This increases protein synthesis, decreases protein degradation, stimulates skeletal muscle cell growth, and increases muscle function and strength. Overstimulation of the ActRII-mediated signaling pathway is associated with muscle loss and weakness.
  • bimatoprost ophthalmic solution A sterile ophthalmic solution containing 0.03% of a synthetic prostaglandin analog bimatoprost with hair-growing and anti-glaucoma activities. Applied once daily to the upper eyelid margin at the base of the eyelashes and, optionally, to the eyebrows, bimatoprost penetrates into the hair follicle and may, through a mechanism that has yet to be fully understood, stimulate the transition of hair follicles from the telogen phase into the anagen phase and may increase the duration of the time follicles spend in anagen. By increasing the numbers of hair follicles in and duration of anagen phase, bimatoprost may help increase eyebrow and eyelash growth and appearance, including their length, thickness and darkness.
  • binimetinib An orally available inhibitor of mitogen-activated protein kinase kinase 1 and 2 (MEK1/2) with potential antineoplastic activity. Binimetinib, noncompetitive with ATP, binds to and inhibits the activity of MEK1/2. Inhibition of MEK1/2 prevents the activation of MEK1/2-dependent effector proteins and transcription factors, which may result in the inhibition of growth factor-mediated cell signaling. This may eventually lead to an inhibition of tumor cell proliferation and an inhibition in production of various inflammatory cytokines including interleukin-1, -6 and tumor necrosis factor. MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the activation of the RAS/RAF/MEK/ERK pathway and are often upregulated in a variety of tumor cell types.
  • Binosto Brand name for alendronate sodium
  • Biomed 101 An agent binding to the leukotriene B4 receptor, leading to reduced interleukin-2 mediated hypoxia. Biomed 101 does not affect interleukin-2 antitumor activity.
  • Bioperine Brand name for piperine extract (standardized)
  • Biopress Brand name for candesartan cilexetil
  • BioResponse DIM Brand name for oral microencapsulated diindolylmethane
  • Biotest-HCIG Brand name for hepatitis C immune globulin intravenous
  • biricodar dicitrate The dicitrate salt of a synthetic pipecolinate derivative with potential chemosensitizing activity. Biricodar binds directly to the plasma membrane drug-efflux pumps P-glycoprotein (Pgp) and multidrug resistance protein 1 (MRP-1) and inhibits their activities, which may result in increased intracellular accumulation and retention of cytotoxic agents.
  • birinapant A synthetic small molecule and peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity. As a SMAC mimetic and IAP antagonist, birinapant binds to and inhibits the activity of IAPs, such as X chromosome-linked IAP (XIAP) and cellular IAPs 1 and 2. Since IAPs shield cancer cells from the apoptosis process, this agent may restore and promote the induction of apoptosis through apoptotic signaling pathways in cancer cells. IAPs are overexpressed by many cancer cell types and suppress apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their baculoviral lAP repeat (BIR) domains.
  • bisacodyl A synthetic pyridinylmethylene-diacetate ester derivative stimulant laxative, Bisacodyl acts with a parasympathetic effect directly on mucosal sensory nerves, increasing peristaltic contractions. It is used for occasional constipation, in pre- and postoperative treatment, and in conditions that require facilitation of defecation.
  • bisantrene hydrochloride The hydrochloride salt of an anthracenyl bishydrazone with antineoplastic activity. Bisantrene intercalates with and disrupts the configuration of DNA, resulting in DNA single-strand breaks, DNA-protein crosslinking, and inhibition of DNA replication. This agent is similar to doxorubicin in activity, but unlike doxorubicin, does not exhibit cardiotoxicity.
  • bi-shRNA-furin/GMCSF-expressing autologous tumor cell vaccine Autologous tumor cells transfected with a plasmid expressing recombinant human granulocyte macrophage-colony stimulating factor (rhGM-CSF) and bifunctional short hairpin RNA (bi-shRNA) against furin, with potential immunostimulatory and antineoplastic activities. Upon intradermal vaccination of bi-shRNA-furin/GM-CSF-expressing autologous tumor cell vaccine, expressed GM-CSF protein, a potent stimulator of the immune system, recruits immune effectors to the site of injection and promotes antigen presentation. The furin bifunctional shRNA blocks furin protein production. Decreased levels of furin lead to a reduction in the conversion of transforming growth factor (TGF) beta into TGF beta1 and beta2 protein isoforms. In turn, as part of the negative feedback mechanism, reduced furin protein levels inhibit TGFbeta1 and TGFbeta2 gene expression, thereby further decreasing TGF levels. As TGFs are potent immunosuppressive cytokines, reducing their levels may activate the immune system locally and this may eventually cause a cytotoxic T-lymphocyte (CTL) response against the tumor cells.
  • bismuth Bi213 monoclonal antibody M195 A radioimmunoconjugate consisting of murine monoclonal antibody (M195) and bismuth 213 (Bi213). Monoclonal antibody M195 binds to CD33, a surface antigen expressed by myelogenous leukemia cells. Bi213 is an isotope that emits short-ranged high-energy alpha particles. This radioimmunoconjugate selectively delivers alpha particle-mediated cytotoxicity to leukemic cells, thereby limiting the exposure of normal tissues to ionizing radiation.
  • bismuth subsalicylate A bismuth salt of salicylic acid. Little absorbed from the gastrointestinal tract, bismuth subsalicylate exerts a local effect on the gastric mucosa, coating it and protecting it from the corrosive effects of acid and pepsin. This agent also has local antimicrobial properties.
  • bisoprolol fumarate The fumarate salt of a synthetic phenoxy-2-propanol-derived cardioselective beta-1 adrenergic receptor antagonist with antihypertensive and potential cardioprotective activities. Devoid of intrinsic sympathomimetic activity, bisoprolol selectively and competitively binds to and blocks beta-1 adrenergic receptors in the heart, decreasing cardiac contractility and rate, reducing cardiac output, and lowering blood pressure. In addition, this agent may exhibit antihypertensive activity through the inhibition of renin secretion by juxtaglomerular epithelioid (JGE) cells in the kidney, thus inhibiting activation of the renin-angiotensin system (RAS). Bisoprolol has been shown to be cardioprotective in animal models.
  • bispecific antibody 2B1 A monoclonal antibody with potential antineoplastic activity. Specific for both the immunoglobulin G (IgG) receptor CD16 and c-erbB-2, bispecific antibody 2B1 may enhance cellular immune responses against c-erbB-2-positive cells, resulting in increased tumor cell lysis.
  • bispecific antibody 4G7xH22 A bispecific antibody containing a 4G7 hybridoma secreting IgG1 antibody specific for B-lymphocytes and a monoclonal antibody targeting Fc gamma RI-expressing cells.
  • bispecific antibody MDX447 An antibody with potential antineoplastic activity. Specific for both the high-affinity immunoglobulin G (IgG) receptor CD64 and epidermal growth factor receptor (EGFR), bispecific antibody MDX447 may enhance cellular immune responses against EGFR positive cells, resulting in increased tumor cell lysis.
  • bispecific antibody MDX-H210 A humanized bivalent antibody directed against both cytotoxic effector cells expressing Fc gamma receptor type I (Fc gammaRI, or CD64) and HER2/neu-overexpressing tumor cells with potential antineoplastic activity. Bispecific antibody MDX-H210 was constructed by chemically linking Fab' fragments of the anti-HER2/neu-specific monoclonal antibody 520C9 and the Fab' fragments of the anti-Fc gammaRI-specific monoclonal antibody H22. This agent selectively binds to both HER2/neu-expressing tumor cells and Fc gammaRI-expressing cytotoxic effector cells, which may trigger antibody-dependent cell-mediated cytotoxicity (ADCC) and cell lysis of HER2/neu-expressing tumor cells. While HER2/neu is overexpressed in a variety of epithelial malignancies, expression of Fc gammaRI is primarily found in cytotoxic immune cells, including monocytes, macrophages, and cytokine-activated polymorphonuclear (PMN) cells.
  • bivalent BRD4 inhibitor AZD5153 An orally bioavailable bivalent inhibitor of bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon oral administration, the BRD4 inhibitor AZD5153 selectively binds to the acetylated lysine recognition motifs in two bromodomains in the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines on histones. This disrupts chromatin remodeling and dysregulates expression of target genes, which leads to the downregulation of the expression of certain growth-promoting genes, induces apoptosis and inhibits the proliferation of BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation.
  • bivalent HPV16/18 therapeutic cervical cancer vaccine A bivalent human papillomavirus (HPV) therapeutic vaccine containing recombinant inactivated adenylate cyclase (CyaA) from Bordetella pertussis carrying a sequence encoding the E7 antigen of both HPV16 and 18, with potential immunostimulatory and antiviral properties. Upon administration of bivalent HPV16/18 therapeutic cervical cancer vaccine, the expressed proteins may activate cell-mediated immunity and induce both cytotoxic CD8+ T cells and CD4+ helper T cells against the target antigens HPV16-E7 and HPV18-E7, which leads to HPV viral clearance. Adenylate cyclase is a virulence factor of Bordetella pertussis. Its ability to bind to CD11b-expressing dendritic cells and deliver antigens directly to the cytosol allows the activation and induction of T-cell immunity. CyaA may also induce a B cell response.
  • bizelesin A synthetic cyclopropylpyrroloindole antineoplastic antibiotic. Bizelesin binds to the minor groove of DNA and induces interstrand cross-linking of DNA, thereby inhibiting DNA replication and RNA synthesis. Bizelesin also enhances p53 and p21 induction and triggers G2/M cell-cycle arrest, resulting in cell senescence without apoptosis.
  • BL22 immunotoxin A recombinant immunotoxin consisting of the Fv portion of the anti-CD22 antibody RFB4 fused to a fragment of Pseudomonas exotoxin-A with potential antineoplastic activity. BL22 immunotoxin binds to CD22, an antigen expressed in B-cell malignancies, thereby delivering its toxin directly to tumor cells. The toxin moiety induces caspase-mediated apoptosis of tumor cells via a mechanism involving mitochondrial damage; it also blocks translational elongation via binding to elongation factor-2 in eukaryotic cells. Check for active clinical trialsusing this agent.
  • black cohosh A triterpene-containing herb isolated from the roots and rhizomes of the plant Cimicifuga racemosa (also known as Actaea racemosa). While the mechanism of action of black cohosh is not completely understood, it appears to act as a selective estrogen receptor modulator. In vitro, this preparation has been shown to induce cell cycle arrest and caspase-dependent apoptosis of estrogen-sensitive breast cancer cells.
  • black currant juice The juice from the berries of the black currant (Ribes nigrum L.) shrub belonging to the family Grossulariaceae, with potential antioxidant and protective activities. Black currant juice contains a variety of nutrients, including vitamin C, iron, potassium, manganese, anthocyanins, including delphinidin-3-O-glucoside, delphinidin-3-O-rutinoside, cyanidin-3-O-glucoside, and cyanidin-3-O-rutinoside. The antioxidants in black currant juice scavenge free radicals, thereby protecting cells from damage.
  • black raspberry nectar A concentrated fruit juice containing black raspberries, with potential antioxidant, pro-apoptotic, anti-angiogenic and chemopreventive activities. In addition to vitamins, minerals and phytosterols, black raspberries are rich in phenolic acids, such as gallic acid, ellagic acid, anthocyanidins, and flavonoids. Upon oral administration, the phytochemicals in the black raspberry nectar inhibit the activation of several signal transduction pathways involved in carcinogenesis and the expression of downstream target genes that are upregulated in a variety of cancer cell types. In addition, the phytochemicals in black raspberry may protect the oral microbiome and may enhance the bacterial defense against pathogens. Check for active clinical trialsusing this agent.
  • black tea Black tea is an infusion of dried leaves from plants of the Theaceae family. Due to the alkaloid caffeine, its main effect is stimulation. Black teas also contain other phytochemicals such as flavonoid and flavonoid-related compounds with strong antioxidant effects. They also attenuate atherosclerotic inflammation, reduce thrombosis, promote normal endothelial function, and block expression of cellular adhesion molecules. Black tea may reduce the risk of cancer, heart diseases, infectious diseases, and degenerative diseases.
  • bleomycin sulfate A mixture of the sulfate salts of basic glycopeptide antineoplastic antibiotics isolated from Streptomyces verticillus. Bleomycin sulfate forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals which cause single- and double-stranded breaks in DNA; these reactive oxygen species also induce lipid peroxidation, carbohydrate oxidation, and alterations in prostaglandin synthesis and degradation.
  • BLI850 An oral laxative containing sodium sulfate, potassium sulfate, magnesium sulfate and sucralose. Oral sulfate-based laxative BLI850 exhibits osmotic activity, attracting water into the intestinal tract from tissues and increasing the volume and the water content of the stool; gastrointestinal motility is stimulated, resulting in defecation. Sucralose, an artificial sweetener, may contribute to the laxative effect.
  • blinatumomab A recombinant, single-chain, anti-CD19/anti-CD3 bispecific monoclonal antibody with potential immunostimulating and antineoplastic activities. Blinatumomab posesses two antigen-recognition sites, one for the CD3 complex, a group of T cell surface glycoproteins that complex with the T cell receptor (TCR), and one for CD19, a tumor-associated antigen (TAA) overexpressed on the surface of B cells. This bispecific monoclonal antibody brings CD19-expressing tumor B-cells and cytotoxic T lymphocytes (CTLs) and helper T lymphocytes (HTLs) together, which may result in the CTL- and HTL-mediated cell death of CD19-expressing B-lymphocytes.
  • Blincyto Brand name for blinatumomab
  • blue citrus-based herbal capsule An oral capsule formulation of a traditional Chinese herbal medicine with potential analgesic activity. In addition to other herbs, seeds and fruits, blue citrus-based herbal capsule contains the Chinese herb blue citrus (qing pi), which is produced from the dried immature green peel of the tangerine Citrus reticulata Blanco. Blue citrus contains large amounts of limonene, citral and synephrine, which may attribute to its analgesic activity. However, due to the complexity of its chemical components, the exact mechanism of action of this agent remains to be determined.
  • blueberry powder supplement An orally available, dietary supplement consisting of lyophilized blueberry powder, with antioxidant and potential chemopreventive and chemosensitizing activity. In addition to vitamins and minerals, blueberries are rich in phytonutrients, such as proanthocyanidins, anthocyanins (e.g. malvidin, delphinidin, pelargonidin, cyanidin, petunidin, and peonidin), hydroxycinnamic acids, hydroxybenzoic acids, pterostilbene, resveratrol, and flavonols (e.g. kaempferol, quercetin and myricetin). Although the exact mechanism of action through which blueberries may exert their anti-tumor effect has yet to be fully elucidated, the effects of blueberry powder on cancer cells may be attributable to the phytonutrient’s antioxidant and pro-apoptotic activities.
  • BMI1 inhibitor PTC596 An orally active inhibitor of the polycomb ring finger oncogene BMI1 (B-cell-specific Moloney murine leukemia virus integration site 1), with potential antineoplastic activity. Upon oral administration, BMI1 inhibitor PTC596 targets BMI1 expressed by both tumor cells and cancer stem cells (CSCs), and induces hyper-phosphorylation of BMI1, leading to its degradation. This inhibits BMI1-mediated signal transduction pathways and results in a reduction of proliferation of BMI1-expressing tumor cells. BMI1, a key protein in the polycomb repressive complex 1 (PRC1), is overexpressed in certain tumor cell types, and plays a key role in CSC survival, proliferation and resistance to chemotherapeutics; its expression is associated with increased tumor aggressiveness and a poor prognosis.
  • BMS-214662 A nonsedating benzodiazepine derivative with potential antineoplastic activity. Farnesyltransferase inhibitor BMS-214662 inhibits the enzyme farnesyltransferase and the post-translational farnesylation of number of proteins involved in signal transduction, which may result in the inhibition of Ras function and apoptosis in susceptible tumor cells. This agent may reverse the malignant phenotype of H-Ras-transformed cells and has been shown to be active against tumor cells with and without Ras mutations. Check for active clinical trialsusing this agent.
  • boanmycin hydrochloride The hydrochloride salt form of boanmycin (aka bleomycin A6), a component of the antibiotic bleomycin produced by Streptomyces species, with potential antineoplastic activity. Upon administration, boanmycin forms complexes with iron that reduce molecular oxygen to superoxide and hydroxyl radicals. This causes single- and double-stranded DNA breaks which eventually leads to cell death. Compared to bleomycin, boanmycin appears to have a more favorable toxicity profile.
  • boceprevir An orally bioavailable, synthetic tripeptide inhibitor of the nonstructural protein 3 and 4A complex (NS3/NS4A), with potential activity against hepatitis C virus (HCV) genotype 1. Upon administration, boceprevir reversibly binds to the active center of the HCV NS3/NS4A and prevents NS3/NS4A protease-mediated polyprotein maturation. This disrupts the processing of viral proteins and the formation of a viral replication complex, which inhibits viral replication in HCV genotype 1-infected host cells. NS3, a serine protease, is essential for the proteolytic cleavages within the HCV polyprotein and plays a key role during HCV viral RNA replication. NS4A is an activating factor for NS3. HCV is a small, enveloped, single-stranded RNA virus belonging to the Flaviviridae family.
  • bone metastasis targeting peptide-11 A peptide that mimics naturally occurring interleukin-11 (IL-11) with interleukin receptor binding activity. Upon administration, bone metastasis targeting peptide-11 (BMTP-11) binds to interleukin-11 receptor alpha (IL-11Ra) BMTP-11. This agent might be used to deliver therapeutic agents specifically to IL-11Ra-expressing tumor cells while sparing normal cells. IL-11Ra is a cell surface receptor that may be overexpressed by osteosarcoma cells and by prostate cancer cells in prostate cancer bone metastases.
  • Bonine Brand name for meclizine hydrochloride
  • Boniva Brand name for ibandronate sodium
  • Boost Brand name for nutritional supplement drink
  • Boost Breeze Brand name for whey protein isolate nutritional supplement
  • boron-dipyrromethene-modified olaparib fluorescent imaging agent A poly (ADP-ribose) polymerase type 1 (PARP1) fluorescence imaging agent based on the PARP1 inhibitor olaparib, in which the cyclopropane group of olaparib is replaced by the green fluorescent dye boron-dipyrromethene (BODIPY) fluorophore (FL), with potential fluorescent imaging activity. Upon administration of the fluorescent PARP1 inhibitor PARPi-FL, the olaparib binding moiety specifically targets and binds to PARP1, which is often overexpressed on cancer cells. Upon fluorescent imaging, the PARP1-expressing cancer cells can be visualized. PARP1, the nuclear enzyme that catalyzes post-translational ADP-ribosylation of nuclear proteins, is activated by single-strand (SS) DNA breaks and overexpressed in certain tumor cells; it plays a key role in DNA repair, tumor cell resistance and survival.
  • boronophenylalanine-fructose complex A boronated phenylalanine complexed with fructose to increase its solubility. When exposed to neutron irradiation, boronophenylalanine absorbs neutrons and self-destructs releasing short-range alpha radiation and 'recoil' lithium in tumor cells, resulting in alpha radiation-induced tumor cell death. This highly selective, localized radiotargeting of tumor cells, known as boron neutron capture therapy (BNCT), spares adjacent normal tissues.
  • bortezomib A dipeptide boronic acid analogue with antineoplastic activity. Bortezomib reversibly inhibits the 26S proteasome, a large protease complex that degrades ubiquinated proteins. By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis. Specifically, the agent inhibits nuclear factor (NF)-kappaB, a protein that is constitutively activated in some cancers, thereby interfering with NF-kappaB-mediated cell survival, tumor growth, and angiogenesis. In vivo, bortezomib delays tumor growth and enhances the cytotoxic effects of radiation and chemotherapy.
  • Bosulif Brand name for bosutinib
  • bosutinib A synthetic quinolone derivative and dual kinase inhibitor that targets both Abl and Src kinases with potential antineoplastic activity. Unlike imatinib, bosutinib inhibits the autophosphorylation of both Abl and Src kinases, resulting in inhibition of cell growth and apoptosis. Because of the dual mechanism of action, this agent may have activity in resistant CML disease, other myeloid malignancies and solid tumors. Abl kinase is upregulated in the presence of the abnormal Bcr-abl fusion protein which is commonly associated with chronic myeloid leukemia (CML). Overexpression of specific Src kinases is also associated with the imatinib-resistant CML phenotype.
  • Boswellia serrata extract A standardized extract derived from the plant Boswellia serrata of the family Burseraceae with anti-inflammatory activity. Boswellia serrata extract contains terpenoid boswellic acids, which are potent inhibitors of 5-lipoxygenase activity and, so, leukotriene synthesis.
  • botanical agent BEL-X-HG An orally available botanically-based agent with potential antineoplastic activity. Upon oral administration, the components in BEL-X-HG may exert cytotoxic effects against cancer cells.
  • botanical agent LEAC-102 A botanical-based formulation derived from the Taiwanese mushroom Antrodia cinnamomea, with potential antineoplastic activity, Upon administration, the components in LEAC-102 may exert cytotoxic effects against cancer cells.
  • botanical extract DCB-BO1301 A proprietary botanical, galactolipid-enriched extract derived from the edible plant Crassocephalum crepidioides (Zhaohe Cao), with potential anti-inflammatory and antineoplastic activities. Upon oral administration, DCB-BO1301 may inhibit the growth of certain types of tumor cells, although the exact mechanism of action has yet to be fully elucidated.
  • botanical extracts rinse IZN-6N4 An oral rinse containing 1% of botanical extracts with potential anti-inflammatory and antimucositis activity. Upon rinsing with botanical extracts rinse IZN-6N4 in the oral cavity, this agent may prevent inflammation of the mucosal membranes and may decrease chemotherapy- and/or radiation-induced oral mucositis.
  • botanical lotion CG428 A proprietary lotion containing a blend of the four botanicals Allium cepa L. (Onion), Citrus limon L. (Citrus), Theobroma cacao L. (Cocoa), Paullinia cupana (Guarana), with potential activity against chemotherapy-induced alopecia (CIA). Upon administration to the scalp, botanical lotion CG428 may normalize the apoptotic process of hair follicular cells and reduce inflammation in the scalp. This may reverse CIA, restore the natural hair cycle, improve hair regrowth, and improve the psychosocial well-being of the affected patient.
  • BOTOX Brand name for botulinum toxin type A
  • Botox cosmetic Brand name for botulinum toxin type A
  • botulinum toxin E EB-001 An injectable formulation containing the bacterial Clostridium botulinum type E neurotoxin, with neuromuscular transmission inhibitory and analgesic activities. Upon injection of botulinum toxin E EB-001 into the muscles of the affected area, the heavy chain portion of botulinum toxin type E binds to the cell membrane of the presynaptic nerve terminal and is internalized via endocytosis. Upon entry into the cytoplasm, the light chain portion of the toxin binds to and cleaves synaptosomal-associated protein 25 (SNAP-25), thereby preventing the fusion of acetylcholine (ACh)-containing synaptic vesicles with the cell membrane and, thus the release of the neurotransmitter ACh into the neuromuscular junction. This prevents the binding of ACh to the motor end-plate nicotinic acid receptors and ACh-mediated muscle contraction. This causes flaccid paralysis and may decrease musculoskeletal pain and may improve wound healing and reduce scar formation due to the absence of muscle contractions. In addition, EB-001 may inhibit the release of neuropeptides, such as substance P and glutamate, which may contribute to its analgesic activity. Compared to other botulinum toxin types, type E has the fastest onset and the shortest duration of action.
  • botulinum toxin type A An injectable formulation of a neurotoxin derived through the fermentation of the Hall strain of Clostridium botulinum type A with neuromuscular transmission inhibitory and analgesic activities. Upon injection into the affected muscle, the heavy chain portion of onabotulinumtoxinA binds to the cell membrane of the motor nerve and is internalized via endocytosis. Upon entry, the light chain portion of the toxin is activated and cleaves the protein SNAP-25, thereby preventing the fusion of acetylcholine (ACh)-containing synaptic vesicles with the cell membrane and, so, the release of ACh into the neuromuscular junction; subsequent binding of ACH to motor end-plate nicotinic acid receptors and ACh-mediated muscle contraction are thus blocked. In addition to ACh, onabotulinumtoxinA may inhibit the release of neuropeptides, such as substance P and glutamate, which may contribute to its analgesic activity.
  • bovine lactoferrin supplement A supplement containing lactoferrin derived from bovine milk with potential chemopreventive, immunostimulating, and antimicrobial activity. Upon administration, lactoferrin binds to metal in the oral cavity and may prevent metal-induced oxidation of lipids. This may reduce the metallic taste and taste disturbances induced by certain metal-containing chemotherapeutics; metal-induced lipid oxidation, and the subsequent production of aldehydes and ketones attributed to the metallic smell. Lactoferrin, a glycoprotein belonging to the transferrin family of metal-binding proteins, can be found in milk and other secretory fluids as well as in polymorphonuclear cells and leukocytes; lactoferrin plays a role in the innate defense of mucosal surfaces and its iron-binding activity is associated with the antibacterial activity.
  • Bowman-Birk inhibitor concentrate An extract of soybeans enriched in Bowman-Birk inhibitor (BBI), a soybean-derived, 71-amino acid, polypeptide and serine protease inhibitor with potential chemopreventive activity. Bowman-Birk inhibitor contains distinct inhibitory sites for trypsin and chymotrypsin. Although the exact mechanism by which BBI suppresses carcinogenesis is unknown, its antiproliferative activity appears to be linked to the chymotrypsin inhibitory region.
  • BP-Cx1-platinum complex BP-C1 A combination agent composed of the benzo-poly-carbonic-acid polymer BP-Cx1 chelated to platinum with potential antineoplastic activity. Upon intramuscular injection, the polymer moiety of BP-Cx1-Platinum Complex BP-C1 (BP-C1) alters the permeability of the cell membranes, which allows for increased penetration of platinum into tumor cells. In turn, platinum binds to nucleophilic groups such as GC-rich sites in DNA and induces intrastrand and interstrand DNA cross-links, as well as DNA-protein cross-links. These cross-links result in apoptosis and cell growth inhibition. In addition, the BP-Cx1 ligand is able to stimulate the innate immune system and upregulates a variety of cytokines including interferon, tumor necrosis factor-alpha (TNF-alpha), granulocyte macrophage-colony stimulating factor (GM-CSF), and various interleukins (ILs) such as IL-6 and IL-25. In comparison to cisplatin and other platinum–based compounds, treatment with BP-C1 allows for less platinum administration, which reduces platinum-associated systemic toxicity and side effects, and enhances the safety profile while maintaining or improving its efficacy.
  • brachyury-expressing modified vaccinia Ankara-TRICOM vaccine A cancer vaccine composed of a replication-deficient, attenuated derivative of the vaccinia virus strain Ankara expressing both a CD8+ T-cell epitope from the brachyury protein and a triad of T-cell co-stimulatory molecules (MVA Brachyury-TRICOM), with potential immunomodulating and antineoplastic activities. Upon subcutaneous administration of the brachyury-expressing modified vaccinia Ankara (MVA)-TRICOM vaccine, the expressed brachyury protein induces specific CD8+ and CD4+ T-cell responses against brachyury-expressing tumor cells. This causes both tumor cell lysis and a decrease in the growth of brachyury-expressing tumor cells. Brachyury, a member of the T-box family of transcription factors that is overexpressed in numerous cancer cell types, is correlated with increased epithelial-mesenchymal transition (EMT), cancer resistance and cancer progression. TRICOM, a triad of three human T-cell co-stimulatory molecules, B7.1, ICAM-1 and LFA-3, enhances antigen-specific T-cell activation.
  • brachyury-expressing yeast vaccine GI-6301 A cancer vaccine composed of a heat-killed, recombinant form of the yeast Saccharomyces cerevisiae that is genetically modified to express the transcription factor brachyury protein, with potential antineoplastic activity. Upon subcutaneous administration, the brachyury-expressing yeast vaccine GI-6301 is recognized by dendritic cells, processed, and presented by Class I and II MHC molecules on the dendritic cell surface. This elicits a targeted CD4+ and CD8+ T-lymphocyte-mediated immune response. This process kills brachyury-expressing tumor cells. Brachyury is overexpressed in a variety of tumor types and plays an important role in cancer progression and metastasis.
  • BRAF inhibitor ARQ 736 An orally bioavailable, highly soluble phosphate prodrug of B-raf (BRAF) protein kinase with potential antineoplastic activity. BRAF inhibitor ARQ 736 is converted into its active form ARQ 680 in the presence of phosphatases. In turn, ARQ 680 selectively binds to and inhibits the activity of oncogenic B-raf, which may inhibit the proliferation of tumor cells expressing mutated B-raf gene. B-raf belongs to the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. The valine to glutamic acid substitution at residue 600 (V600E) accounts for about 90% of BRAF gene mutations.
  • BRAF inhibitor LUT014 A topically bioavailable small molecule inhibitor of serine/threonine-protein kinase B-raf (BRAF) protein with potential chemoprotective activity. Upon topical administration, BRAF inhibitor LUT014 targets and binds BRAF and, through the paradoxical effect of BRAF inhibition, induces mitogen-activated protein kinase (MAPK) signaling, which leads to the proliferation and migration of healthy human keratinocytes. This decreases dermal toxicities associated with epidermal growth factor (EGFR) inhibitor therapy. BRAF, a member of the raf family of serine/threonine protein kinases, plays a role in the regulation of MAPK/extracellular signal-regulated kinase (ERK) signaling pathways.
  • BRAF inhibitor PLX8394 An orally bioavailable inhibitor of serine/threonine-protein kinase B-raf (BRAF) protein with potential antineoplastic activity. BRAF inhibitor PLX8394 appears to selectively bind to and inhibit the activity of both wild-type and mutated forms of BRAF, which may subsequently inhibit the proliferation of tumor cells which express mutated forms of BRAF. This inhibitor appears to be effective against tumors that express multiple mutated forms of the kinase and may be an effective therapeutic agent for tumors that are resistant to other BRAF inhibitor therapies that are specific for the BRAF V600E mutant. BRAF, a member of the raf family of serine/threonine protein kinases, plays a role in the regulation of MAP kinase/ERK signaling pathways, which may be constitutively activated due to BRAF gene mutations. Mutated forms of BRAF are associated with a number of neoplastic diseases.
  • BRAF V600E kinase inhibitor RO5212054 An orally available small-molecule inhibitor of mutant (V600E) v-raf murine sarcoma viral oncogene homolog B1 (BRAF) with potential antineoplastic activity. BRAF(V600E) kinase inhibitor RO5212054 selectively binds to the ATP-binding site of BRAF(V600E) kinase and inhibits its activity, which may result in an inhibition of an over-activated MAPK signaling pathway downstream in BRAF(V600E) kinase-expressing tumor cells and a reduction in tumor cell proliferation. The valine to glutamic acid substitution at residue 600 accounts for about 90% of BRAF gene mutations; the oncogenic product, BRAF(V600E) kinase, exhibits a markedly elevated activity that over-activates the MAPK signaling pathway. The BRAF(V600E) mutation has been found to occur in approximately 60% of melanomas, and in about 8% of all solid tumors.
  • BRAF(V600E) inhibitor CEP-32496 An orally available v-raf murine sarcoma viral oncogene homolog B1 (B-raf) serine/threonine protein kinase inhibitor with potential antineoplastic activity. CEP-32496 specifically and selectively inhibits the activity of the mutated form (V600E) of B-raf kinase. This inhibits the activation of the RAF/mitogen-activated protein kinase kinase (MEK)/extracellular signal-related kinase (ERK) signaling pathway and may result in a decrease in the proliferation of tumor cells expressing the mutated B-raf gene. The Raf mutation BRAF V600E, in which valine is substituted for glutamic acid at residue 600, is frequently found in a variety of human tumors and results in the constitutive activation of the RAF/MEK/ERK signaling pathway that regulates cellular proliferation and survival.
  • BRAF/EGFR inhibitor BGB-283 An inhibitor of the serine/threonine protein kinase B-raf (BRAF) and epidermal growth factor receptor (EGFR), with potential antineoplastic activity. BRAF/EGFR inhibitor BGB-283 selectively binds to and inhibits the activity of BRAF and certain BRAF mutant forms, and EGFR. This prevents BRAF- and EGFR-mediated signaling and inhibits the proliferation of tumor cells that either contain a mutated BRAF gene or express over-activated EGFR. In addition, BGB-283 inhibits mutant forms of the Ras proteins K-RAS and N-RAS. BRAF and EGFR are mutated or upregulated in many tumor cell types.
  • B-Raf/VEGFR-2 inhibitor RAF265 An orally bioavailable small molecule with potential antineoplastic activity. B-Raf/VEGFR-2 inhibitor RAF265 binds and inhibits Raf kinases, which may result in a reduction of tumor cell growth and proliferation, and tumor cell death. In addition, this agent inhibits vascular endothelial growth factor receptor type 2 (VEGFR-2), thereby disrupting tumor angiogenesis. Raf kinases are critical enzymes in the Ras/Raf/MEK/ERK signaling pathway and are frequently upregulated in neoplasms.
  • Braftovi Brand name for encorafenib
  • BRAFV600/PI3K inhibitor ASN003 A selective inhibitor of mutated forms of B-RAF kinase at amino acid position 600 (BRAFV600), including BRAFV600E, the alpha, delta and, to a lesser extent, beta isoforms of phosphatidylinositide 3-kinase (PI3K), including mutated forms of PI3KCA, which encodes the p110-alpha catalytic subunit of the class I PI3K, and the phosphatase and tensin homologs (PTEN) with loss-of-function mutation, with potential antineoplastic activity. Upon administration of ASN003, this agent selectively targets, binds to and inhibits the activity of BRAFV600 mutants as well as mutated isoforms of PI3K. This inhibits signaling through B-RAF- and PI3K/mechanistic target of rapamycin (mTOR)-mediated pathways and inhibits cellular proliferation in tumor cells with BRAFV600 mutations, those expressing PI3K and/or those driven by PTEN. Dysregulation of the B-RAF- and PI3K-mediated pathways is frequently seen in a variety of tumors and results in increased tumor cell growth and survival. Dual targeting of both pathways may increase efficacy and anti-tumor potential compared to the targeting of just one pathway by a selective B-RAF inhibitor or selective PI3K pathway inhibitor alone.
  • brain tumor initiating cell vaccine A cell-based cancer vaccine comprised of brain tumor initiating cells (BTICs), with potential immunostimulating and antineoplastic activity. BITCs are from the glioblastoma multiforme (GBM) cell line GBM-6 and contain glioma stem-like cell-associated antigens. Upon administration, the BITC vaccine may stimulate a specific anti-tumoral cytotoxic T –lymphocyte (CTL) response against brain tumor cancer cells and brain tumor stem like cells, resulting in tumor cell lysis. BITC have unique antigenicity and have the ability to self-renew; vaccination against BITC antigens may kill these cells and may prevent tumor recurrences. Check for active clinical trialsusing this agent.
  • Brakiva Brand name for liposomal topotecan hydrochloride
  • branched chain amino acid supplement A nutritional supplement containing essential branched-chain amino acids (BCAAs), including leucine, isoleucine and valine, with potential anti-cachectic, antiangiogenic, hepatocellular carcinoma (HCC)-inhibiting and hepatoprotective activities. Upon oral administration, BCAAs inhibit the expression of both hypoxia-inducible factor 1-alpha subunit (HIF-1a) and vascular endothelial growth factor (VEGF), which prevents VEGF-mediated angiogenesis in HCC cells. In addition, BCAAs inhibit proliferation and induce apoptosis of HCC cells by both suppressing the expression of insulin-like growth factor (IGF), and inhibiting the phosphatidylinositol 3-kinase (PI3K)/Akt/mammalian target of rapamycin (mTOR) pathway. BCAAs also correct the plasma amino acid imbalance and promote protein metabolism, including the synthesis of albumin and glycogen. They reduce oxidative stress by inducing the activation of genes involved in antioxidant defenses, which prevent the production of reactive oxygen species (ROS). BCAAs also strengthen the immune system by increasing hepatic lymphocytes and stimulating natural killer (NK) cell activity. This supplement is able to improve insulin resistance and promote ammonia detoxification through increased glutamine (Gln) production.
  • Brassica vegetable A vegetable belonging to the Brassica genus of plants in the mustard family with potential chemopreventive activity. Brassica vegetables, including broccoli, cabbage, kale, Brussel sprouts, turnip and cauliflower, contain a significant amount of glucosinolates. Glucosinolate metabolites, such as sulforaphane and indole-3-carbinol, act as antioxidants and may stimulate endogenous phase II detoxifying enzymes, including glutathione S-transferase and quinone reductase. These biotransformation enzymes play major roles in the detoxification of carcinogenic agents.
  • BRD4 inhibitor PLX2853 An orally bioavailable inhibitor of the bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon oral administration, the BRD4 inhibitor PLX2853 binds to the acetylated lysine recognition motifs in the bromodomains of the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines on histones. This disrupts chromatin remodeling and dyregulates gene expression. This may lead to the downregulation of the expression of certain growth-promoting genes, which may induce apoptosis and inhibit the proliferation of BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation.
  • BRD4 inhibitor PLX51107 An inhibitor of the bromodomain-containing protein 4 (BRD4), with potential antineoplastic activity. Upon administration, the BRD4 inhibitor PLX51107 binds to the acetylated lysine recognition motifs in the bromodomains of the BRD4 protein, thereby preventing the binding of BRD4 to acetylated lysines on histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to an induction of apoptosis and an inhibition of proliferation in BRD4-overexpressing tumor cells. BRD4, a member of the human bromodomain and extra-terminal (BET) family of proteins, is a transcriptional regulator that is overexpressed in certain tumor cells and plays an important role in cellular proliferation.
  • 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.
  • 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.
  • Brevicon Brand name for ethinyl estradiol/norethindrone
  • Bria-IMT Brand 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.
  • Bridion Brand 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.
  • 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.
  • 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.
  • brimonidine tartrate nanoemulsion OCU-300 An ophthalmic nanoemulsion consisting of the tartrate salt form of brimonidine, an imidazole derivative and selective alpha-adrenergic receptor agonist, with potential anti-inflammatory and vasoconstrictive activities. Upon ophthalmic instillation, brimonidine tartrate nanoemulsion OCU-300 reduces intraocular pressure by promoting the outflow and decreasing the production of aqueous humor and may reduce ocular erythema through direct vasoconstriction. Additionally, brimonidine may disrupt leukocyte extravasation into the ocular tissue, inhibit nociception and reduce inflammation associated with ocular graft-versus-host disease (oGvHD). The nanoemulsion formulation may enhance distribution of brimonidine to target tissues, thereby allowing more of the active drug to reach underlying ocular tissue.
  • 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.
  • Brintellix Brand 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.
  • 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.
  • Briviact Brand 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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).
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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.
  • 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 trialsusing this agent.
  • 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.
  • BTK inhibitor ICP-022 A small molecule inhibitor of Bruton’s tyrosine kinase (BTK; Bruton agammaglobulinemia tyrosine kinase) with potential antineoplastic activity. Upon administration, BTK inhibitor ICP-022 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, inhibiting 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.
  • BTK inhibitor LOXO-305 An orally available, selective, non-covalent Bruton’s tyrosine kinase (BTK) inhibitor with potential antineoplastic activity. Upon oral administration, BTK inhibitor LOXO-305 selectively and reversibly binds to BTK. This prevents both the activation of the B-cell antigen receptor (BCR) signaling pathway and BTK-mediated activation of downstream survival pathways, thereby inhibiting the growth of malignant B cells that overexpress BTK. Reversible binding of LOXO-305 may preserve antitumor activity in the presence of certain acquired resistance mutations, including C481 mutated BTK, and limit toxicity associated with inhibition of other non-BTK kinases. 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.
  • 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.
  • 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.
  • 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.
  • Bulkamid Brand 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.
  • Bumex Brand 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.
  • Buphenyl Brand 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.
  • 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.
  • 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.
  • 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.
  • 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, improving sexual desire, and improving cancer-related fatigue. Bupropion is a weak blocker of the neuronal uptake of serotonin, dopamine and norepinephrine and is a central nicotinic acetylcholine receptor antagonist. Bupropion may also reduce circulating levels of tumor necrosis factor (TNF) and normalize hypothalamic-pituitary-adrenal (HPA) axis functioning, which is dysregulated in certain cases of cancer-related fatigue. The controlled-release formulation results in a higher concentration of the drug in the body over an extended period, 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.
  • burosumab An orally bioavailable recombinant human immunoglobulin G1 monoclonal antibody directed against human fibroblast growth factor 23 (FGF23), that can be used to increase serum phosphate levels. Upon subcutaneous administration, burosumab binds to and inhibits FGF23, thereby interfering with FGF23 signaling. This increases tubular phosphate reabsorption, decreases excretion of phosphate, and increases serum phosphate levels, resulting in enhanced bone mineralization. FGF23, a member of the fibroblast growth factor (FGF) family produced by osteocytes, plays a key role in hypophosphatemic rickets/osteomalacia, such as X-linked hypophosphatemia (XLH) and tumor-induced rickets/osteomalacia. Increased FGF23 levels lead to decreased expression of the sodium-phosphate co-transporters in the proximal tubules, reduced renal phosphate reabsorption, increased excretion by the kidneys, and low serum phosphate concentration.
  • 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.
  • Bushen Culuan decoction A traditional Chinese medicine (TCM) decoction containing a mixture of ten Chinese herbs including Tusizi, Yinyanghuo, Xianmao, Xuduan, Gouqizi, Nvzhenzi, Zelan, Shengpuhuang, Xiangfu and Chuanshanlong, with potential to induce ovulation. Upon oral administration, Bushen Culuan decoction may, through a not yet fully elucidated mechanism, depress follicle-stimulating hormone (FSH) levels, elevate anti-Mullerian hormone (AMH) levels, and increase the number of antral follicle counts (AFCs), thereby promoting ovulation.
  • Bushen-Jianpi decoction A traditional Chinese medicine (TCM) that is used for Yin deficiency of the liver, kidney and spleen, with potential immunomodulating and antineoplastic activities. Bushen-Jianpi decoction (BSJPD; BJD) consists of various herbs, including, but not limited to, Radix Codonopsis (Dang Shen), Fructus Lycii (the fruit of Chinese wolfberry), Rhizoma Atractylodis Macrocephalae (Baishu; Bai Zhu), Fructus Ligustri Lucidi, Cuscuta chinensis (Chinese dodder) seed, and Psoralea corylifolia Linn. As a TCM, Bushen-Jianpi is used as an antineoplastic agent as it is thought to invigorate the spleen and tonify the kidney, which presumably prevents or treats a variety of cancers. Upon administration of Bushen-Jianpi decoction, the ingredients in the decoction may affect signaling pathways involved in carcinogenesis and enhance the immune system by increasing the levels of numerous cytokines and a variety of immune cells, such as cytotoxic T lymphocytes (CTLs), natural killer cells (NKs) and macrophages. It may also reduce the expression of various proteins involved in tumorigenesis.
  • Buspar Brand 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 trialsusing this agent.
  • 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.
  • busulfan-melphalan regimen A chemotherapeutic regimen composed of busulfan and melphalan used as a conditioning regimen for stem cell transplantation (SCT).
  • Busulfex Brand 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.
  • 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.
  • 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.
  • Byetta Brand name for exenatide
 

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