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Cancer Agents for DA final

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zidazije's version from 2017-04-30 22:11

CML and Receptor Tyrosine Kinase Inhibitors

Question Answer
Imatinib (Gleevec)competitive inhibitor of the ATP-binding site of ABL
Nilotinibcompetitive inhibitor of the ATP-binding site of ABL
Dasatinibcompetitive inhibitor of the active form of the ATP-binding site of BCR-ABL
Bosutinibcompetitive inhibitor of the ATP-binding site of ABL
Ponatinib3rd generation receptor tyrosine kinase inhibitor of BCR-ABL, covers the T315I mutation
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EGFR and HER2 Agents

Question Answer
GefitinibEGFR RTK Inhibitor: binds to a unique cysteine in the ATP-binding site
ErlotinibEGFR RTK Inhibitor: binds to a unique cysteine in the ATP-binding site
LapatinibRTK inhibitor of both HER2 and EGFR
Cetuximabbinds the extracellular domain of EGFR, decreased cell proliferation
Panitumumabbinds the extracellular domain of EGFR, decreased cell proliferation
Trastuzumabbinds to the extracellular domain of HER2, causes receptor internalization and AB-mediated cytotoxicity
Pertuzumabbinds to the dimerization domain of HER2, prevents receptor dimerization and causes AB-mediated cytotoxicity
Trastuzumab-emtansineAntibody-drug complex of trastuzumab and DM-1: binds, gets internalized and the drug portion inhibits the micro tubular network leading to cell apoptosis
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VEGF and mTOR Agents

Question Answer
BevacizumabBinds to free VEGF-A, the ligand for the VEGF2-receptor. reduces serum VEGF-A to nearly undetectable levels
SIrolimusmTOR inhibitor: binds FKBP --> drug-protein complex acts to inhibit mTOR
TemsirolimusmTOR inhibitor: binds FKBP --> drug-protein complex acts to inhibit mTOR
EverolimusmTOR inhibitor: binds FKBP --> drug-protein complex acts to inhibit mTOR
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Natural Product Antineoplastics

Question Answer
DaunorubicinAnthracycline Topoisomerase II inhibitor
DoxorubicinAnthracycline Topoisomerase II inhibitor, increased potency vs daunorubicin
IdarubicinS&S Anthracycline Topoisomerase II inhibitor lacking the 4-hydroxy --> flattened D-ring with 5-6 fold higher potency than doxorubicin
EpirubicinS&S Anthracycline Topoisomerase II inhibitor with faster clearance due to an equatorial sugar hydroxy that leads to a much higher lifetime dose
Major Toxicity of the anthracyclinesCardiotoxicity due to the hydroxyl radical produced via the Fenton reaction and poisoning of topoisomers II Beta
CatalaseEnzyme present in low concentrations in the heart that normally detoxifies the superoxide free radicals of anthracyclines
Dexrazoxanegiven as adjuvant to anthracycline therapy to prevent cardiotoxicity
ValrubicinS&S Anthracycline. Inhibits nucleotide incorporation into DNA and RNA
MitoxantroneS&S Anthracycline. Inhibits Topoisomerase II w/out producing free radicals. resistant to NADPH/CYP450 reductase. 3 ring molecule with no sugar like the anthracyclines
DactinomycinRNA polymerase inhibitor: intercalates into DNA and inhibits RNA transcription
BleomycinStrictly causes DNA damage via free radical damage. Highly Cytotoxic! toxicities occur in the skin and lungs because both tissues lack bleomycin hydrolase
MitomycinAlkylating agent that cross-links and intercalates DNA
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