BPS 333 Final: Cancer Drugs – Flashcards
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Aflatoxins
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most potent carcinogen known; in peanut butter
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Benzopyrene
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product of combustion
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Benzene
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immunosuppressant
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Cyclophosphamide
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alkylating agents; react with DNA by splitting it, cause a mutation
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Mechlorethylamine
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alkylating agent; was used in gas during world war 1 and works by reacting with a basic portion of DNA
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Classes of carcinogens
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1) Immunosuppressors (benzenes) 2) Hormones (DES) 3) Solid state carcinogens (asbestos)
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Oncogenes
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Genes that encode for transforming proteins that can cause cancer. Oncogenes are derived from the mutation of Proto-oncogenes: genes in normal cells that encode for proteins involved in cellular regulations, including: G proteins, tyrosine-specific kinases, other protein kinases, growth factors and transcription regulators.
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Tumor suppressor genes: anti oncogenes
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These are also referred to as growth suppressor genes in normal cells these proteins suppress cell growth and division mutation leads to a loss of the ability to restrain cell growth and division the anti-oncogene product is a mutant protein that is inactive as a growth suppressor
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Childhood tumors with high cure rates
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Acute lymphocytic leukemia Burkitt's lymphoma Ewings' sarcoma - bone tumor Retinoblastoma Wilms' tumor - kidney tumor
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Adult tumors with high cure rates
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Hodgkin's disease Non-Hodgkin's lymphomas Trophoblastic choriocarcinoma Testicular and ovarian germ cell cancers
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Filgrastim (Neupogen)
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granulocyte colony stimulating factor used to increase WBC's
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Prochlorperazine (Compazine) Dronabinol (Marinol) Ondansetron (Zofran)
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Drugs used to prevent nausea
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P glycoprotein
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resides in cell membranes that pump out toxins may be responsible for resistance of cells to many anticancer drugs
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2 benefits of chemotherapy mechanisms
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1) Drugs work synergistically 2) All the drugs have different toxicities
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Alkylating agents
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Mechanism of action: transfer akyl group to DNA, inhibiting cell division Adverse effects: bone marrow suppression, nausea, and vomiting
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Platinum Coordinating Compounds
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metal complexes mechanism similar to alkylating agents highly effective, but limited by nephrotoxicity.
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Carboplatin (Paraplatin)
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platinum coordinating compounds used for ovarian cancers causes kidney toxicity
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Cisplatin
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platinum coordinating compounds used for neoplasms of testies, lymph tissue, or ovaries.
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Antimetabolites
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inhibit key metabolic steps required for DNA synthesis: act during S phase of cell cycle some also used as immunosuppressive adverse, effects: immunosuppressant, GI lesions, alopecia, bone marrow depression, skin rash all antimetabolites are immunosuppressive
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Methotrexate
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antimetabolite folic acid synthesis
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Mercaptopurine
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antimetabolite purine synthesis
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Fluorouracil
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antimetabolite pyrimidine synthesis
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Vinca alkaloids
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derived from periwinkle plant inhibit mitosis: act during M phase of cell-cycle used especially in breast cancer and choriocarcinoma adverse effects: bone marrow suppression, alopecia, GI lesions, neurotoxicity currently available: vincristine and vinblastine
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Cytotoxic antibiotics and synthetics
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bind to DNA to inhibit RNA synthesis: G2 phase of cell cycle adverse effects: visual toxicity: additional unique, drug-specific side effects Example - bleomycin (lung fibrosis)
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What are the two ways hormonal therapy medicines treat hormone receptive positive breast cancer
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1) by lowering the amount of the hormone estrogen in the body 2) by blocking the action of estrogen on breast cancer cells
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Aromatase inhibitors
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Aminoglutethimide, 4-hydroxy-androstenedione Indication: Anti-cancer agent Mechanism of Action: Inhibition of aromatase-catalyzed conversion of androgens to estrogens thus blocking estrogen biosynthesis Aromatase inhibitors DO NOT block estrogen production in the ovaries **** Femara
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Selective Estrogen Receptor Modulators (SERMs)
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Action: Both estrogenic and anti-estrogenic actions, depending on the target tissue. Ex.) Block estrogen action in breast tissue while activating the action of estrogen in bone, liver, uterine cells etc. Mechanism: Mediated by its binding to the estrogen receptor and the blocking of the proliferative actions of estrogen on mammary epithelium. SERMs can be used to treat women both before and after menopause
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Important SERMs
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Tamoxifen (Nolvadex) Evista (raloxifene)
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Tamoxifen mechanism of action
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1) to compete with 17?-estradiol (E2) at the receptor site and to block the promotional role of E2 in breast cancer 2) to bind DNA after metabolic activation and to initiate carcinogenesis
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Interference with Tamoxifen metabolism . . . .
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1) Abnormal CYP2D6 enzyme levels/function 2) Strong to moderate inhibitors of tamoxifen (produce alterations in CYP2D6): SSRIs, SNRIs, quinidine (Cardioquin), diphenhydramine (Benadryl), cimetidine (Tagamet)
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Estrogen Receptor Downregulators (SERDs)
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These agents occupy the estrogen receptor and inhibit dimerization. This causes estrogen receptor downregulation. The estrogen receptor is unable to interact with the estrogen response element in the nucleus, causing a complete failure of transcription. Indication: Post-menopausal women diagnosed metastatic hormone-receptor-positive breast cancer that has stopped responding to other hormonal therapy
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Important SERDs
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Faslodex (chemical name: fulvestrant)
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Tyrosine Kinase Receptors
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An enzyme involved in the growth of cells Transduce signals that direct Growth Division Migration Synthesis Apoptosis (cell death)
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Tumor Angiogenesis and Neovasculature
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1) Tumors less than 1 mm3 receive oxygen and nutrients by diffusion from host vasculature. 2) Larger tumors require new vessel network. Tumor secretes angiogenic factors that stimulate migration, proliferation, and neovessel formation by endothelial cells in adjacent established vessels. 3) Newly vascularized tumor no longer relies solely on diffusion from host vasculature, facilitating progressive growth
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Important Tyrosine Kinase Inhibitors
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Gleevec CML results through a chromosomal rearrangement that fuses two genes together. This produces an oncogene that encodes an enzyme, a form of tyrosine kinase known as BCR-ABL. (A hybrid Bcr-Abl enzyme that is always active). The abnormal activity of the enzyme causes the overproliferation of white blood cells that is the hallmark of CML.
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Important monoclonal antibodies
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Herceptin and Avastin
