Chemo- Anti-Mitotic Drugs/Topoisomerase Inhibitors Flashcards
(21 cards)
What is the MOA of Vinca alkaloids?
Bind to B tubulin and inhibit polymerization
What is the MOA of Taxanes?
Enhance tubule polymerization and stabilize microtubules
What cell-cycle phase do Vinca alkaloids and Taxanes act on?
M phase (impair spindle integrity)
What are the taxanes and what cancers are they used for?
Paclitaxel and Docetaxel- Used for solid tumors- especially advanced breast and ovarian cancer
What is the therapeutic use of Vincristine?
WALEN: Wilm’s tumor, ALL, lymphoma, Ewings sarcoma, Neuroblastoma
What is Vinblastine used for?
Testicular cancer (wi/bleomycin and cisplatin), lymphomas, neuroblastoma
What is Vinorelbine used for?
Advanced non-small cell lung cancer
What are the side effects of Vincristine?
Neurotoxicity and peripheral neuropathy!!
Also blisters and paralytic ileus
What are the side effects of Vinblastine and Vinorelbine?
Bone marrow suppression and blisters (vesicant)
What are the side effects of Paclitaxel?
Severe hypersensitivity during infusion!
Also neutropenia, thrombocytopenia, peripheral neuropathy
What can cause treatment failure for the Vinca allaloids and taxanes?
P-glycoprotein expression by tumor cells–> pumps drug out of cells and can cause relapse of cancer
What are the Epipodophyllotoxins and what is their MOA?
Etoposide and Teniposide
Inhibit Topoisomerase 2–> cause dsDNA breaks
What are the Camptothecins and what is their MOA?
Irinotecan and Topotecan
Inhibit Topoisomerase 1–> cause ssDNA breaks
What is Etoposide used for?
Oat cell carcinoma of the lung and testicular cancer; (wi/cisplatin and bleomycin)
What is Teniposide used for?
Glioma and Neuroblastoma
What is Irinotecan used for?
Metastatic colon cancer
What is Topotecan used for?
Second-line treatment for various cancers that failed prior 1st line treatment
What is the Dose limiting toxicity of Irinotecan?
Severe diarrhea! And myelosupression
What is the dose limiting toxicity of Etoposide?
Leukopenia, and secondary cancer (leukemia)
What is the MOA of topoisomerase inhibitors?
Bind to DNA-enzyme complex and create a persistently cleavable complex
What are the differences in the cell cycle activity of topoisomerase 1 and 2 inhibitors?
Topoisomerase 1 inhibitors- S phase
Topoisomerase 2 inhibitors- CCNS
