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ANTIMICROTUBULES PHL 417

Learn about the mechanism of action, therapeutic uses, and side effects of Vinca alkaloids (vinblastine, vincristine, vinorelbine) and Taxanes (paclitaxel, docetaxel), powerful antimicrotubule agents derived from natural sources.

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ANTIMICROTUBULES PHL 417

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  1. ANTIMICROTUBULES PHL 417

  2. ANTIMICROTUBULE AGENTS

  3. 1. Vinca Alkaloids • Vinblastine • Vincristine • Vinorelbine

  4. Vinca Alkaloids They are plant alkaloids extracted fromPeriwinkle plant (Vinca Rosa) 3 3

  5. VincaAlkaloidsMechanism of Action • They act by binding to  and tubulin and inhibit its polymerization into microtubules leading to preventing spindle formation in mitosing cells. • Resulting in mitotic arrest at metaphase, dissolution of the mitotic spindle, and interference with chromosome segregation. • CCS agents- M phase

  6. Vinca alkaloid Mechanism of resistance • 1- Pleiotropic drug resistances i.e. cross-resistant to a wide range of chemically dissimilar agents: vinca alkaloid, epidophyllotoxin, anthracyclines and colchicine. Due to: High level of P-glycoprotein • 2- Mutation in either  and tubulinthat prevent effective binding of vinca alkaloids

  7. Vinca alkaloidTherapeutic uses

  8. Vinca alkaloid Side effects

  9. 2. Taxanes • Paclitaxel (Taxol) • Docetaxel • Alkaloid esters derived from the bark of ash tree (Taxus brevifolia).

  10. Taxanes (cont.)Mechanism of Action • Taxanes enhance assembly of microtubules and stabilize them against depolymerization. • It binds to tubulin (at a site distinct from that used by vinca alkaloids) and promotes assembly of microtubules giving non-functional microtubule network.

  11. Taxanes (cont.)Toxicity • Paclitaxel • Neutropenia, thrombocytopenia • Peripheral neuropathy • Docetaxel • Bone marrow suppression • Neurotoxicity • Fluid retention

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