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7 Cards in this Set
- Front
- Back
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Topotecan and irinotecan (CPT-11)
Mechanism Clinical Use Toxicities |
Derivatives of camptothecin.
Mech: Topoisomerase I -targeted. Intercalation mechanism stabilizes complex. Irinotecan is a prodrug that must be activated. Clinical: Solid tumors including colorectal, ovarian, lung, etc. Tox: Normal, plus irinotecan causes liver toxicity in some patients and diarrhea. |
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Minor Groove DNA-Binding Drugs
Mechanism |
Mech: Topoisomerase I-targeted. Maybe stabilize complex by DNA bending?
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Actinomycin D
Mechanism Clinical Use Toxicities |
Mech: Topoisomerase I -targeted. Increases amount of covalent complex by inducing DNA bending, though maybe for RNA polymerase I instead of topo I.
Clinical: CHILDHOOD malignancies. Tox: Usual suspects. |
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Etoposide and Teniposide
Mechanism Clinical Use Toxicities |
Epipodophylotoxins.
Mech: Topoisomerase II -targeted. Non-intercalative stabilizers of topo II complex. Clinical: Many cancers. Tox: Normal + anaphylaxis. |
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Doxorubicin and Daunorubicin
Mechanism Clinical Use Toxicities |
Anthracyclines.
Mech: Intercalative, direct or indirect stabilizers of Topo II. Clinical: Doxo for solid tumors, Dauno for acute leukemias. Tox: Metabolism and toxicity occurs in the liver--free radicals produced! Also LOTS of cardiotoxicity. |
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Vincristine, Vinblastine and Vinorelbine
Mechanism Clinical Use Toxicities |
Mitotic spindle poisons. Vinca alkaloids.
Mech: Slow microtubule polymerization dynamics. Clinical: Vincristine for blood, blastine for germ cell, orelbine for lung and breast. Tox: Significant liver, significant neuro (b/c axons have microtubules). |
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Paclitaxel and docetaxel
Mechanism Clinical Use Toxicities |
Mitotic spindle poisons. Taxanes.
Mech: Bind to B tubulin and stabilize lateral tubulin contacts. Clinical: Pac for ovarian and breast, doce for breast. Tox: Normal, myelosuppression, and peripheral neuropathy (spindles!). |
