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31 Cards in this Set
- Front
- Back
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What is the tumor cell growth fraction
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-fraction of cells not in G0, so they are responsive to chemo
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WHat are micrometastases
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-derived from tumor cells
-ultimate cause of lethality |
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What types of general target S phase, M phase
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-antimetabolites
-machinery of cell division |
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bischloroethyl amines
-MOA |
-alkylating agent
-mechlorethamine (nitrogen mustard) -covalently bonds to DNA |
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Cyclophosphamide is a
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-prodrug that is activated in the liver
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Nitrosurea:
MOA -penetration |
-alkylating agent, but little cross resistance w/other agents
-cross BBB so useful against brain tumors |
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Procarbazine:
used in works how |
MOPP regimen for hodgkin's
-metabolized to alkylating and free radical intermediates |
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Methotrexate:
MOA phase |
-DHFR inhibitor = blocks DNA synthesis
-S phase specific |
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Purine antagonists
MOA -phase -activated -resistance |
similar to natural base and interfere w/synthesis of DNA and RNA
-conversion to NMPs, NTPs via HGPRT -down regulation of HGPRT |
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Pyrimidine antagonists
5-FU -MOA -phase |
-inhibits thymidylate synthetase
-metabolites incorporated into DNA and RNA -S-phase |
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capecitabine
-prodrug of? -why its so good |
-fluorouracil
-preferentially activated in tumor tissues |
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anthracyclines:
MOA x 2 |
-DNA intercalation
-DNA topoisomerase II binding |
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DNA intercalating agnest are cell cycle specific (T/F)
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-false - b/c they interact so tightly w/DNA they don't need to be in cell cycle
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Major good thing of bleomycin
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-no significant myelosuppression
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Vinca alkaloids
MOA |
-mitotic spindle poisons
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vinblastin:
cell-cycle MOA |
M-phase
-inhibits MT polymerization |
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Paclitaxel
MOA derived from |
-blocks MT disassembly
bark of yew tree |
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Topoisomerase inhibitors
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-camptothecins: topotecan, irinotecan
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Platinum coordination complexes:
Cisplatin, carboplatin -MOA |
inhibit DNA synthesis
-non cycle specific |
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What two types of cancer are hormone dependent
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-prostate and breast
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Tamoxifen:
MOA how does it act |
-estrogen inhibitor (selective estrogen response modulators)
-binds to estrogen receptor and acts as partial agonist |
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What is necessary for tamoxifen to work
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presence of estrogen receptors in breast cancer tissues
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Why do "inib"s work
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target EGF receptor protein tyrosine kinase which are overexpressed in certain cancers (inhibit these)
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etrozole, anastrozole MOA
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inhibit conversion of androgens to estrogen
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what drug is used in "chemical castration"
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leuprolide
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flutamide MOA
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-GnRH receptor antagonist
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Why is prednisone used in cancer treatment
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-suppresses mitosis of lymphocytes, useful for inducing remission of leukemias
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2 examples of targeted agents
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-kinase inhibitors
-antibodies |
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Mechanisms of drug resistance in ANA
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-alterations in drug uptake
-increased conc of target enzyme -decreased rate of drug activation -increased drug metabolism -increased rate of drug efflux |
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What is MDR1
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APT-driven pump that transports certain drugs out of the cell
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What can MDR1 pump
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-vinca alkaloids, etoposide, anthracyclines, actinomycin D, colchicine
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