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31 Cards in this Set
- Front
- Back
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topoisomerase I inhibitors?
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camptothecin analogs
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Camptothecin analogs?
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topotecan, irinotecan
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Topoisomerase II inhibitors?
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epipodophyllotoxins and anthracycline analogs
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epipodophyllotoxins?
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etoposide
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anthracycline analogs?
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doxorubicin, daunorubicin
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Topoisomerases are essential for?
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DNA replication, recombination, transcription and repair
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topoisomerase I: causes ____ -strand DNA breaks
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single strand breaks
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topoisomerase II: causes ____ -strand DNA breaks
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double strand breaks
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Mechanism of Action of Camptothecin Analogs?
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The FLAT ring systems intercalate
DNA at the site of cleavage • bind and STABILIZE DNA topoisomerase I “cleavable complex” • inhibit the religation of SINGLE stranded breaks in DNA •cause irreversible DNA breaks during DNA replication, leading to apoptosis • S-phase-specific drugs |
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Addition of a _____ ring to the quinalone moiety of camptothecins is essential for activity.
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Lactone ring
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Topotecan dosing: 1.5 mg/m2 IV infusion for 5 days, every 3 weeks
cancer types? |
lung and ovarian
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Topotecan requires?
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dose reduction for renal impairment
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Irinotecan dosing: 100-350 mg/m2 IV infusion weekly or every 2 or 3 weeks for cancer types:
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lung, colorectal, cervical, ovarian, gastric, brain
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Dose limiting toxicity of Irinotecan?
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GI (diarrhea and N/V)
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Irinotecan demonstrates linear PK and is metabolized by hepatic
carboxylesterase to _____ the active form. |
SN-38
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MOA of Epipodophyllotoxins?
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- forms a ternary complex with topoisomerase II and DNA - causes DOUBLE -stranded DNA breaks- most sensitive in cells during S and G2 phases
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Etopside dosing: 50-120 mg/m2/day infusion for 3-5 days; or 50 mg/day, for 3 weeks; repeat every 3-4 weeks. Used to treat?
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Lung, lymphoma and testicular cancers
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Which Epipodophyllotoxin is not S phase specific?
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Etopside
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Mechanism of Action of Anthracyclines?
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- flat ring system intercalates directly with DNA (GC rich) - forms a complex with topoisomerase II and DNA, causing DOUBLE stranded DNA breaks and apoptosis- produces free radicals that also cause DNA damage
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Cardiotoxicity of Anthracyclines is due to?
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Superoxide free radicals
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Primary toxicity associated with anthracyclines?
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cardio toxicity
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Cardio toxicity associated with anthracyclines can be treated with?
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dexrazoxone, a potent intracellular chelator of iron
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Doxorubicin is used to treat?
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breast, lung and prostate cancers and ALL
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Doxorubicin is also a strong _______.
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Vesicant
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Doxil, the liposomal form of Doxorubicin is used to treat?
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multiple myeloma and ovarian cancer
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In addition to myelosuppression and GI toxicity, Doxorubicin Liposomal can also cause ___________.
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hand-foot syndrome
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All Anthracyclines are strong vesicants, except?
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Mitoxantrone
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Daunorubicin and Idarubicin are used to treat?
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AML
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All anthracycline toposisomerase II inhibitors end with the -bicin suffix, exept?
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mitoxantrone
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mitoxantrone is used to treat?
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prostate cancer and AML
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The anthralcycline topo-II inhibitor that produces the least cardiotoxicity is?
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mitoxantrone
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