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31 Cards in this Set

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