Cancer Drugs: Alkylating, Microtubule-I, et al

Question 1

What are the alkylating agents in anticancer?

Answer 1

Cyclophosphamide, ifosfamide, Nitrosureas (carmustine, lomustine), Busulfan

Question 2

What are the microtubule inhibitors?

Answer 2

Vinca alkyloids (vincristine, vinblastine), Taxols (paclitaxel)

Question 3

How does cyclophosphamide/ifosfamide work?

Answer 3

covalent crosslinking of DNA (bioactivation by liver)

Question 4

Aside from myelosuppression, what’s a major concern when taking cyclophosphamide/ifosfamide?

Answer 4

Hemorrhagic cystitis

mesna is given to reduce the chances (it binds the toxic metabolite acrolein)

Question 5

The Nitrosureas (-mustine) are generally used for what type of cancer?

Answer 5

CNS tumors (since the drug crosses BBB easily)
therefore, CNS toxicities

put NITRO in your MUSTang

Question 6

Busulfan works by _______ DNA and causes what toxicity.

Answer 6

alkylating

Pulmonary fibrosis

Question 7

Vinca alkyloids do what specifically to microtubules?

Answer 7

block polymerization of microtubules

inhibits metaphase

Question 8

The Taxol drugs do what specifically to microtubules?

Answer 8

hyperstabilize the microtubules, preventing them from breaking down, preventing the cell from going into anaphase

Question 9

Identify the toxicities in the Vinca alkyloids.

Answer 9

Vincristine: neurotoxicity
Vinblastine: BM suppression (blasts the BM)

Question 10

Platinum derivatives (cisplat) are used in tumors of the _______ system and do what to DNA?

Answer 10

used in Genitourinary cancers (bladder, ovary, testicular)

cross link the DNA (like cyclophosphamide)

Question 11

Platinum derivatives share toxicity with what other drugs?

Answer 11

nephrotoxicity, ototoxicity

Same as vancomycin, aminoglycosides, loop diuretics

Question 12

What drug, also used in Sickle Cell patients, blocks ribonucleotide reductase?

Answer 12

Hydroxyurea

Question 13

What are the big 9 toxicities of the most commonly used glucocorticoid in anticancer?

Answer 13

Prednisone
(I C CHOPPAH)
Immunosuppression
Cushing-like (moon facies, buffalo hump, fat trunk)
Cataracts, HTN, Osteoporosis, PUD, Psychosis, Acne, Hyperglycemia

Question 14

Tamoxifen and raloxifene are used in what type of cancer and how do they work?

Answer 14

SERMs: antagonize estrogen receptor in breast, agonize in the bone
Therefore, used in breast cancers and prevent osteoporosis as a nice little benefit

Question 15

Trastuzumab’s MOA

Answer 15

monoclonal ab against HER-2 (erb-B2)

this is a tyrosine kinase that’s overexpressed in some breast cancers

Question 16

Imatinib is used for what specific case?

Answer 16

used in the Philadelphia chromosome: t(9;22)

mostly seen in CML, sometimes in ALL

Question 17

Rituximab is an antibody against what?

Answer 17

Ab vs CD20

therfore, used in most B cell tumors (but not Hodgkin’s, they aren’t CD20!)