Antimitotics

Question 1

Antimitotic general MOA

Answer 1

inhibit either the polymerization or depolymerization of tubulin, the subunit of microtubules, that are essential for separating chromosomes at mitosis.

Question 2

Agents that inhibit depolymerization

Answer 2

Paclitaxel
Docetaxel/Cabazitaxel
Ixabepilone

Question 3

Paclitaxel aka Taxol

Answer 3

Binds to BETA tubulin subunit. Solubility problems.
Impairs mitosis by interfering with microtubule disassembly
–Causes myelosuppression, hypersens, cardiovasc tox, peripheral neuropathy. See Slide #52 for SAR

Question 4

Docetaxel/Cabazitaxel

Answer 4

Prostate cancer. Give with prednisone!

–Causes myelosuppression, hyper sens, renal failure

Question 5

Ixabepilone

Answer 5

antiproliferative in cancer cells with taxane resistance! Better water solubility.

Question 6

Agents that Inhibit polymerization

Answer 6

inhibit mititoc spindle formation, affect metaphase (=cycle cycle spec)
Vinca alkaloids
Eribulin

Question 7

Vincristine and Vinblastine

Answer 7

infers with microtubule assembly
For ALL, HL and NHL, neuroblastome
cause neuromuscular dysfunction. Periph neuropathy, myelosup, inappropriate ADH secretion
See Slide #57 for SAR.
–If a tumor is MDR it is resistant to this
DO NOT give intrathecally and avoid 3A4 inh and ind

Question 8

Eribulin

Answer 8

for metastatic breast cancer. Causes neutropenia, periph neuropathy, ventricular arrhythmia

Question 9

Anti-mitotics have 2 subclasses

Answer 9

Taxanes

Vinca alkaloids

Question 10

Taxanes end with

Answer 10

-axel

Question 11

Vincas start with

Answer 11

Vin-