Chemo Lecture 3-4: Antimitotic and G/M phase drugs- Fitzpatrick Flashcards
List classes of antineoplastic drugs that are antimitotic drugs
- Vinca alkaloids
- Taxanes
List the drugs that are vinca alkaloids
- Vinblastine
- Vincristine
- Vinorelbine
List drugs that are taxanes
- Taxol (paclitaxel)
- Taxotere (docetaxel)
MOA of Vinca Alkaloids
Binds to beta tubulin at forming end (+) of microtubules and inhibit tubulin polymerization –> block assembly of microtubules –> inhibit microtubule elongation: rate of depolymerization (fraying»_space; rate of polymerization (assembly)
MOA of taxanes
Binds to beta tubulin at the forming end (+) of microtubules and as the microtubule continues to form and fray, the bound taxanes reaches the fraying end (-) and inhibit fraying (disassembly) –> Enhance tubulin polymerization–> stabilize microtubules
Therapeutic use of Vinblastine
- Testicular cancer (w/ bleomycin and cisplatin)
- Lymphomas
- Neuroblastoma
Therapeutic use of Vincristine
- ALL (peds)
- lymphoma
- neuroblastoma
- Wilm’s tumor
- Ewing’s sarcoma
Therapeutic use of Vinorelbine
Advanced NSCL cancer
Therapeutic use of paclitaxel
Advanced breast and ovarian (w/ cisplatin)
Therapeutic use of Docetaxel
Advanced breast, ovarian recurrence
Taxanes in general are effective against which types of tumors, solid or liquid?
Solids tumors
Dose limiting toxicity of vinblastine and vinorelbine
Bone marrow suppresssion; visicant-blisters
Dose limiting toxicity of vincristine
Neurotoxicity; peripheral neuropathy; paralytic ileus; vesicant- blisters
Dose limiting toxicity of paclitaxel
neutropenia; thrombocytopenia; peripheral neuropathy; severe hypersensitivity during infusion
Dose limiting toxicity of docetaxel
neutropenia; peripheral neuropathy
Vinca alkaloids and taxanes drugs impair spindle integrity and works during which phase of the cell cycle?
M phase
If pt experiences severe neuropathy taking administering vincristine, what drug should be substituted?
Vinblastine
Vinca and taxanes drugs commonly leads to multi drug resistance due to increased expression of _
P-glycoprotein and its enhanced extrusion of drugs from tumor cells. This is the reason for treatment failure in over 90% of pts with advanced metastatic cancer
Monoclonal antibodies chemo drugs are NOT prone to P-glycoproteins multi drug resistance because _
these drugs’ mechanism of action involve the exterior cell surface
Class of antineoplastic drugs that which are topoisomerase inhibitors
- Epipodophyllotoxins
2. Camptothecins
Antineoplastic drugs that are epipodophyllotoxins
- Etoposide
- Teniposide
(EET)
Antineoplastic drugs that are camptothecins
- Irinotecan
- Topotecan
(CIT)