Glossary of Drug Names

Abraxane - A drug approved to treat breast cancer that has spread or that has come back within 6 months after chemotherapy.  It is also being studied in the treatment of newly diagnosed breast cancer and other types of cancer. Abraxane is a type of mitotic inhibitor. Also called ABI-007, nanoparticle paclitaxel, paclitaxel albumin-stabilized nanoparticle formulation, and albumin-bound paclitaxel.  The accumulation of albumin-bound paclitaxel in tumors has been hypothesized to be enhanced by the presence of the albumin-binding protein SPARC in the tumor interstitium.

ABT-888 - A poly(ADP-ribose) polymerase (PARP) -1 and -2 inhibitor with chemosensitizing and antitumor activities. With no antiproliferative effects as a single agent at therapeutic concentrations, ABT-888 inhibits PARPs, thereby inhibiting DNA repair and potentiating the cytotoxicity of DNA-damaging agents. PARP nuclear enzymes are activated by DNA single or double strand breaks, resulting in the poly(ADP-ribosyl)ation of other nuclear DNA binding proteins involved in DNA repair; poly(ADP-ribosyl)ation contributes to efficient DNA repair and to survival of proliferating cells exposed to mild genotoxic stresses as induced by as oxidants, alkylating agents or ionizing radiation.

Aflibercept (VEGF Trap) - A protein comprised of segments of the extracellular domains of human vascular endothelial growth factor receptors 1 (VEGFR1) and 2 (VEGFR2) fused to the constant region (Fc) of human IgG1 with potential antiangiogenic activity. Afilbercept, functioning as a soluble decoy receptor, binds to pro-angiogenic vascular endothelial growth factors (VEGFs), thereby preventing VEGFs from binding to their cell receptors. Disruption of the binding of VEGFs to their cell receptors may result in the inhibition of tumor angiogenesis, metastasis, and ultimately tumor regression.

AMG 479 - AMG 479 is a fully human monoclonal antibody that targets type 1 insulin-like growth factor receptor (IGF-1R). It is being investigated as a cancer treatment.

Aromisn – See Exemestane

AZD2281 (Olaparib) - A small molecule inhibitor of the nuclear enzyme poly(ADP-ribose) polymerase (PARP) with potential chemosensitizing, radiosensitizing, and antineoplastic activities. Olaparib selectively binds to and inhibits PARP, inhibiting PARP-mediated repair of single strand DNA breaks; PARP inhibition may enhance the cytotoxicity of DNA-damaging agents and may reverse tumor cell chemoresistance and radioresistance. PARP catalyzes post-translational ADP-ribosylation of nuclear proteins and can be activated by single-stranded DNA breaks.
Avastin – see Bevacizumab

AZD6244 – a type of protein kinase inhibitor that blocks the MEK protein needed for cell growth and may kill cancer cells. 

Bevacizumab - A drug used to treat several types of cancer, including certain types of colorectal, lung, breast, and kidney cancers and glioblastoma. It is also being studied in the treatment of other types of cancer. Avastin binds to vascular endothelial growth factor (VEGF) and may prevent the growth of new blood vessels that tumors need to grow. It is a type of antiangiogenesis agent and a type of monoclonal antibody.  Also called Avastin.

BIBW 2992 - an orally bioavailable dual receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity.   BIBW 2992 irreversibly binds to and inhibits human epidermal growth factor receptors 1 and 2 (EGFR-1; HER2), which may result in the inhibition of tumor growth. EGFR and HER2 are RTKs that belong to the EGFR superfamily; both play roles in tumor cell proliferation and are overexpressed in many cancer cell types.

Carboplatin - A drug that is used to treat advanced ovarian cancer that has never been treated or symptoms of ovarian cancer that has come back after treatment with other anticancer drugs. It is also used together with other drugs to treat advanced, metastatic, or recurrent non-small cell lung cancer and is being studied in the treatment of other types of cancer. Carboplatin is a form of the anticancer drug cisplatin and causes fewer side effects in patients. It attaches to DNA in cells and may kill cancer cells. It is a type of platinum compound. Also called Paraplatin

Catumaxomab - A trifunctional bispecific monoclonal antibody with potential antineoplastic activity. Catumaxomab has two antigen-recognition sites: one for human CD3, a T cell surface antigen; and one for human epithelial cell adhesion molecule (EpCAM), a cell surface antigen expressed by a variety of epithelial tumor cells. In addition, the modified Fc portion of this antibody binds Fc receptors on antingen presenting cells (APCs) such as macrophages and dendritic cells (DCs). Catumaxomab brings T cells, EpCAM-expressing epithelial tumor cells and APCs together into tricellular complexes, which may result in a potent cytotoxic T-lymphocyte (CTL) response against EpCAM-expressing epithelial tumor cells. Fc-mediated binding of APCs in the tricellular complex potentiates EpCAM antigen presentation to T cells and the activation of anti-tumor cytotoxic T cell functions.

Celecoxib - A non-steroidal anti-inflammatory drug that inhibits the enzyme cyclooxygenase-2 (Cox2).  It is used in the treatment of osteroarthritis, rheumatoid arthritis and acute pain.  It is also used to reduce the numbers of colon and rectum polyps in patients with familial adenomatous polyposis.  Also called Celebrex and Onsenal. 

Dasatinib - An orally bioavailable synthetic small molecule-inhibitor of SRC-family protein-tyrosine kinases.  Dasatinib binds to and inhibits the growth-promoting activities of these kinases.  Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.  SRC-family protein-tyrosine kinases interact with variety of cell-surface receptors and participate in intracellular signal transduction pathways; tumorigenic forms can occur through altered regulation or expression of the endogenous protein and by way of virally-encoded kinase genes.

Docetaxel - A semi-synthetic, second-generation taxane derived from a compound found in the European yew tree Taxus baccata. Docetaxel displays potent and broad antineoplastic properties; it binds to and stabilizes tubulin, thereby inhibiting microtubule disassembly which results in cell- cycle arrest at the G2/M phase and cell death. This agent also inhibits pro-angiogenic factors such as vascular endothelial growth factor (VEGF) and displays immunomodulatory and pro-inflammatory properties by inducing various mediators of the inflammatory response. Docetaxel has been studied for use as a radiation-sensitizing agent.  Also called Taxotere.

Erlotinib - A drug used to treat certain types of non-small cell lung cancer. It is also used together with gemcitabine to treat pancreatic cancer and is being studied in the treatment of other types of cancer. Erlotinib is a type of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor. Also called CP-358,774, erlotinib hydrochloride, OSI-774, and Tarceva.

Exemestane - A drug used to treat advanced breast cancer and to prevent recurrent breast cancer in postmenopausal women who have already been treated with tamoxifen.  It is also being studied in the treatment of other types of cancer. Exemestane causes a decrease in the amount of estrogen made by the body. It is a type of aromatase inhibitor.  Also called Aromasin

GDC-0449 - An orally bioavailable small molecule with potential antineoplastic activity. Hedgehog antagonist GDC-0449 targets the Hedgehog signaling pathway, blocking the activities of the Hedgehog-ligand cell surface receptors PTCH and/or SMO and suppressing Hedgehog signaling. The Hedgehog signaling pathway plays an important role in tissue growth and repair; aberrant constitutive activation of Hedgehog pathway signaling and uncontrolled cellular proliferation may be associated with mutations in the Hedgehog-ligand cell surface receptors PTCH and SMO

Gemcitabine - An analogue of the antimetabolite nucleoside deoxycytidine with antineoplastic activity. Gemcitabine is converted intracellularly to the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA synthesis; dFdCTP is incorporated into DNA, resulting in DNA strand termination and apoptosis.

MLN8237 - A second-generation, orally bioavailable, highly selective small molecule inhibitor of the serine/threonine protein kinase Aurora A kinase with potential antineoplastic activity. Aurora kinase inhibitor MLN8237 binds to and inhibits Aurora A kinase, which may result in disruption of the assembly of the mitotic spindle apparatus, disruption of chromosome segregation, and inhibition of cell proliferation. Aurora A kinase localizes to the spindle poles and to spindle microtubules during mitosis, and is thought to regulate spindle assembly. Aberrant expression of Aurora kinases occurs in a wide variety of cancers, including colon and breast cancers.

MORab-003 (Farletuzumab) - A humanized, immunoglobulin G1 monoclonal antibody with potential antitumor activity. MORab-003 specifically targets at glycoprotein 3 (GP-3), a cell surface antigen that is overexpressed on many epithelial-derived cancer cells. Upon binding to the GP-3 antigen, MORab-003 triggers a host immune response against GP-3 expressing cells resulting in cell lysis. 

NKTR-102 - A formulation of polyethylene glycol (PEG)-encapsulated irinotecan with antineoplastic activity. The prodrug irinotecan, a semisynthetic derivative of camptothecin, is converted to the biologically active metabolite 7-ethyl-10-hydroxy-camptothecin by a carboxylesterase-converting enzyme. One thousand-fold more potent than its parent compound irinotecan, 7-ethyl-10-hydroxy-camptothecin inhibits topoisomerase I activity by stabilizing the cleavable complex of topoisomerase I and DNA, resulting in DNA breaks that inhibit DNA replication and trigger apoptosis. Pegylation provides improved drug penetration into tumors and decreases drug clearance, thereby increasing the duration of therapeutic effects while lowering the toxicity profile

Paclitaxel - A compound extracted from the Pacific yew tree Taxus brevifolia with antineoplastic activity. Paclitaxel binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. This agent also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2).

Pemetrexed - a synthetic pyrimidine-based antifolate. Pemetrexed binds to and inhibits the enzyme thymidylate synthase (TS) which catalyses the methylation of 2'-deoxyuridine-5'-monophosphate (dUMP) to 2'-deoxythymidine-5'-monophosphate (dTMP), an essential precursor in DNA synthesis.

Sorafenib  (Nexavar) – a tyrosine kinase inhibitor blocking the VEGFR-2/PDGFR-beta signaling cascade, thereby blocking tumor growth and angiogenesis.

Sunitinib (Sutent) – a tyrosine kinase inhibitor with antineoplastic activity. Sunitinib blocks the tyrosine kinase activities of vascular endothelial growth factor receptor 2 (VEGFR2), platelet-derived growth factor receptor b (PDGFRb), and c-kit, thereby inhibiting angiogenesis and cell proliferation. This agent also inhibits the phosphorylation of Fms-related tyrosine kinase 3 (FLT3), another receptor tyrosine kinase expressed by some leukemic cells.

Temsirolimus - An ester analog of rapamycin. Temsirolimus binds to and inhibits the mammalian target of rapamycin (mTOR), resulting in decreased expression of mRNAs necessary for cell cycle progression and arresting cells in the G1 phase of the cell cycle. mTOR is a serine/threonine kinase which plays a role in the PI3K/AKT pathway that is upregulated in some tumors.

VEGF Trap - see Aflibercept