Anti-Cancer Agents

Question 1

S-phase specific agents

Answer 1

Methotrexate, 5-FU, cytarabine, azathioprine, and 6-MP

Question 2

MOA of MTX

Answer 2

Inhibits dihydrofolate reductase which decreases dTMP synthesis

Question 3

Non-neoplastic uses of MTX

Answer 3

Abortion, ectopic pregnancy, rheumatoid arthritis, and psorisasis

Question 4

SE of MTX

Answer 4

Myelosuppression which is reversible with leucovorin, macrovesicular fatty change, teratogenic

Question 5

MOA of 5-FU

Answer 5

Inhibits thymidylate synthase which decreases dTMP synthesis

Question 6

SE of 5-FU

Answer 6

Myelosuppression which is not reversible with leucovorin, overdose rescue with thymidine

Question 7

MOA of cytarabine

Answer 7

Pyrimidine analog

Question 8

MOA of azathioprine and 6-MP

Answer 8

Purine analogs

Question 9

Antitumor antibiotics

Answer 9

Dactinomycin, doxorubicin, and bleomycin

Question 10

MOA of dactinomycin

Answer 10

Intercalates in DNA

Question 11

Indications for dactinomycin

Answer 11

Wilm’s tumor, Ewing’s sarcoma, rhabdomyosarcoma (childhood tumors)

Question 12

MOA fo doxorubicin

Answer 12

Generates free radicals that noncovalently intercalate in DNA which cause breaks in DNA

Question 13

SE of doxorubicin

Answer 13

Cardiotoxicity (dilated cardiomyopathy), myelosuppresion, alopecia

Dexrazoxane to prevent cardiotoxicity

Question 14

MOA of bleomycin

Answer 14

Induces free radical damage which causes breaks in DNA strands

Question 15

Major side effect of bleomycin

Answer 15

Pulmonary fibrosis

Question 16

MOA of cyclophosphamide and ifosfamide

Answer 16

Covalently X-link (interstrand) DNA at guanine N-7

Question 17

Toxicity of cyclophoshamide

Answer 17

Myelosuppression, hemorrhagic cystitis (partially prevented with mesna)

Question 18

MOA of nitrosoureas (carmustine, lomustine, semustine, streptozococin)

Answer 18

Requires bioactivation, crosses BBB

Question 19

MOA of busulfan

Answer 19

Alkylates DNA

Question 20

Indication of busulfan

Answer 20

CML

Question 21

MOA of vincristine and vinblastine

Answer 21

Alkaloids that bind to tubulin in M phase and block polymerization of microtubules so that mitotic spindle cannot form

Question 22

SE of vincristine

Answer 22

Neurotoxicity (areflexia, peripheral neuropathy, paralytic ileus)

Question 23

SE of vinblastine

Answer 23

Bone marrow suppression

Question 24

MOA of paclitaxel and other taxols

Answer 24

Hyperstabilize polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)

Question 25

SE of paclitaxel and other taxols

Answer 25

Myelosuppresion and hypersensitivity

Question 26

MOA of cisplatin and carboplatin

Answer 26

Cross-link DNA

Question 27

SE of cisplatin

Answer 27

Nephrotoxicity and acoustic nerve damage (prevent nephrotoxicity with amifostine, which is a free radical scavenger)

Question 28

MOA of etoposide and teniposide

Answer 28

Inhibits topoisomerase II which increases DNA degradation

Question 29

Two specific tumors treated with etoposide

Answer 29

Testicular and small cell lung cancers

Question 30

SE of etoposide

Answer 30

Myelosuppresion, GI irritation and alopecia

Question 31

MOA of hydroxyurea

Answer 31

Inhibits ribonucleotide reducatase wich decreased DNA synthesis (S phase specific)

Question 32

Indications of hydroxyurea

Answer 32

Melanoma, CML, sickle cell

Question 33

MOA of prednisone, prednisolone

Answer 33

May trigger apoptosis

Question 34

SE of prednisone

Answer 34

Cushing-like syndromes, immunosuppresion, cataracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis

Question 35

MOA of tamoxifen and raloxifene

Answer 35

SERMs- receptor antagonists in breast and agonists in bone; block the binding of estrogen in estrogen receptor-positive cells

Question 36

Major side effect of tamoxifen

Answer 36

Increased risk of endometrial cancer

Question 37

MOA of trastruzumab (Herceptin)

Answer 37

Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase

Question 38

MOA of imatinib (Gleevev)

Answer 38

Philadelphia chromosome bcr-able tyrosine kinase inhibitor

Question 39

MOA of rituximab

Answer 39

Monoclonal antibody against CD20 which is found on most B-cell neoplasms

Question 40

MOA of vemurafenib

Answer 40

Small molecular inhibitor of forms of the B-raf kinase with the 600E mutation (metastatic melanoma)

Question 41

MOA of bevacizumab

Answer 41

Monoclonal antibody against VEFG which inhibits angiogenesis

Question 42

Indication of bevacizumab

Answer 42

Solid tumors, first line Tx of metastatic colorectal cancer