Anticancer and Immunosuppresants

Question 1

Actinomycin D

Answer 1

Intercalates into DNA and blocks RNA and DNA synthesis
Limiting toxicity: bone marrow depression
Other toxicity: radiation recall

Question 2

Anastrozole

Answer 2

Aromatase inhibitor

Toxicity: effects related to estrogen deficiency

Question 3

Asparaginase

Answer 3

Degrades asparagine in the circulation and starves tumor cells for this amino acid
Limiting toxicity: hypersensitivity reactions

Question 4

Bevacizumab

Answer 4

Antibody against VEGF, inhibits angiogenesis

Limiting toxicity: hypertension, GI perforation

Question 5

Bleomycin

Answer 5

Interacts with DNA and catalyzes free radical formation and DNA destruction
Limiting toxicity: pulmonary fibrosis
Other toxicity: skin changes, radiation recall

Question 6

Cisplatin

Answer 6

Cross-links DNA
Limiting toxicity: bone marrow depression
Other toxicity: renal tubular damage, neurotoxicity

Question 7

Cyclophosphamide

Answer 7

Alkylation and cross-linking of DNA
Limiting toxicity: bone marrow depression
Other toxicity: male sterility, amenorrhea

Question 8

Cytosine arabinoside

Answer 8

Inhibitor of DNA polymerase, misincorporation into DNA

Limiting toxicity: bone marrow depression

Question 9

Doxorubicin

Answer 9

Inhibitor of topoisomerase II-DNA complex
Limiting toxicity: bone marrow depression, cardiomyopathy
Other toxicity: radiation recall

Question 10

Etoposide

Answer 10

Inhibitor of topoisomerase II-DNA complex

Limiting toxicity: bone marrow depression

Question 11

5-Fluorouracil

Answer 11

Inhibitor of thymidylate synthase, misincorporation into RNA

Limiting toxicity: bone marrow depression

Question 12

Gefitnib

Answer 12

EGFR inhibitor

Toxicity: skin problems

Question 13

Hydroxyurea

Answer 13

Inhibitor of ribonucleotide reductase

Limiting toxicity: bone marrow depression

Question 14

Imatinib

Answer 14

Inhibitor of ABL tyrosine kinase

Toxicity: fluid retention, skin rash

Question 15

Irinotecan

Answer 15

Inhibitor of topoisomerase I-DNA complex

Limiting toxicity: bone marrow depression

Question 16

Leuprolide

Answer 16

GnRH analog that causes GnRH receptor down-regulation

Toxicity: hormone withdrawal effects

Question 17

Mechlorethamine

Answer 17

Alkylates and cross-links DNA
Limiting toxicity: bone marrow depression
Other toxicity: male sterility, amenorrhea

Question 18

Methotrexate

Answer 18

DHFR inhibitor

Limiting toxicity: bone marrow depression

Question 19

Paclitaxel

Answer 19

Binds tubulin and stabilizes microtubules
Limiting toxicity: bone marrow depression
Other toxicity: sensory neuropathy

Question 20

Tamoxifen

Answer 20

Estrogen receptor modulator

Toxicity: hot flashes, risk increase for endometrial cancer, thromboembolic events

Question 21

6-Thioguanine

Answer 21

Purine biosynthesis inhibitor

Limiting toxicity: bone marrow depression

Question 22

Trastazumab

Answer 22

Binds to Her2 on cancer cells and stimulates antibody-dependent cellular cytotoxicity
Toxicity: cardiac toxicity

Question 23

Vemurafenib

Answer 23

Active site inhibitor of V600E mutant BRAF

Toxicity: skin problems

Question 24

Vinblastine

Answer 24

Interacts with tubulin and prevents microtubule polymerization
Limiting toxicity: bone marrow depression
Other toxicity: mild peripheral neuropathy

Question 25

Vincristine

Answer 25

Interacts with tubulin and prevents microtubule polymerization Limiting toxicity: peripheral neuropathy

Question 26

Allopurinol

Answer 26

Xanthine oxidase inhibitor | Toxicity: sensitivity reactions

Question 27

Leucovorin

Answer 27

Tetrahydrofolate substitute that can rescue cells from methotrexate toxicity

Question 28

Filgrastim

Answer 28

Hematopoietic agent that stimulates neutrophil production | Toxicity: mild to moderate bone pain, skin reaction

Question 29

Glucocorticoids

Answer 29

Inhibits leukotriene and prostaglandin synthesis, inhibits leukocyte function and traffic control Toxicity: many when used chronically

Question 30

Cyclosporine

Answer 30

Binds cyclophillin and inhibits calcineurin and NFAT activation Toxicity: nephrotoxicity

Question 31

Tacrolimus

Answer 31

Binds FKBP-12 and inhibits calcineurin and NFAT activation | Toxicity: nephrotoxicity

Question 32

Sirolimus

Answer 32

Binds FKBP-12 and inhibits mTOR and T-cell proliferation | Toxicity: increases cholesterol, triglycerides, bone marrow suppression

Question 33

Mycophenolate mofetil

Answer 33

Inhibits inosine monophosphate dehydrogenase and GTP synthesis Toxicity: bone marrow suppression

Question 34

Etanercept

Answer 34

Decoy receptor for TNFalpha | Toxicity: injection site reactions