Microtubule Targeting Drugs

Question 1

Microtubule Structures

Answer 1

o Alpha and beta tubulin subunits

o Form protofilaments that align side by side around a central core

Question 2

Taxanes Drugs

Answer 2

Paclitaxel (taxol)

Docetaxel (taxotere)

Question 3

Taxanes Use

Answer 3

ovarian, breast, AIDS-related Kaposi’s and lung cancers

Question 4

Taxanes MOA

Answer 4

Binds to already formed microtubule and helps to stabilize the microtubules (more rigid → no M phase no division)
Encourage microtubule formation and then stop the microtubules from being broken down

Question 5

Taxol + Hypersensitivity

Answer 5

have to be given with premedications to prevent hypersensitivity

Question 6

Taxanes Specificity

Answer 6

CELL CYCLE SPECIFIC for G2 and M phase

Question 7

Taxanes Resistance

Answer 7

Structural alteration in tubulin protein and p-gp efflux

Question 8

Paclitaxel SE

Answer 8

Myelosuppression, alopecia, neuropathy, hypersensitivity

Question 9

Paclitaxel Pre-Medications

Answer 9

o Dexamethasone 20 mg PO 12 & 6 hours prior
o Pepcid or tagament
o Benedryl plus anti-emetic

Question 10

Doxcetaxel SE

Answer 10

Myelosuppression, alopecia, neuropathy, hypersensitivity

Question 11

Doxcetaxel Pre-Medications

Answer 11

o Dexamethasone 8 mg PO BID starting 1 day prior and 4 days after

Question 12

Abroxane Use and MOA

Answer 12

• Solvent free paclitaxel
• Use: metastatic breast cancer
• MOA: Drug bound to albumin, in the bound it dissociation leads to activity

Question 13

Vinca Alkaloids Drugs

Answer 13

Vincristine, vinblastine, vindesine, vinorelbine

Question 14

Vinca Alkaloids Drugs Use

Answer 14

Leukemias and testicular tumors

Question 15

Vinca alkaloids MOA

Answer 15

Bind to already grown microtubules and helps break down the microtubule/depolymerizes

Question 16

***Vinca Alkaloid Key Features

Answer 16

 VERY LONG half lives
 CELL CYCLE SPECIFIC: late G2 and M phase (no metaphase to anaphase)
ALL drugs in this class are vesicants!!

Question 17

Vinca Alkaloid Resistance

Answer 17

• MDR-P glycoprotein Efflux Pumps

Question 18

Vinblastine (velban) Use

Answer 18

Hodkin's disease
Lymphomas
Breast
Testicular tumor
Kaposi

Question 19

Vinblastine (velban) SE

Answer 19

o Leukopenia
o GI
o Cellulitis
o Neuropathy

Question 20

Vincristine (oncovin) Use

Answer 20

o Leukemias and lymphomas
o NHL
Better tolerated in children

Question 21

Vincristine (oncovin) SE

Answer 21

o Peripheral neuopathy
o Constipation
o Fatal if given intrathecally

Question 22

Vinorelbine (navelbine) USE and SE

Answer 22

• Use: Lung and breast cancer

* SE: Myelosuppression and Neuropathy