Cancer Drugs

Question 1

Methotrexate

Answer 1

folic acid analog; inhibits dihydrofolate reductase; retards DNA/RNA and protein synthesis

Question 2

Mercaptopurine or 6-Thioguanine

Answer 2

prodrugs requiring activation through purine
salvage pathway; induce mutations and inhibit de novo purine synthesis; also effective as antiinflammatory
and immunosuppressive drugs

Question 3

Fluorouracil (5-FU):

Answer 3

blocks thymidylate synthase

Question 4

Vinblastine

Answer 4

Vinca alkaloids
These agents bind to tubulin and prevent mitotic spindle
formation.

Question 5

Paclitaxel/Taxol

Answer 5

Taxoids
These agents induce the polymerization/stabilization of
microtubules.

Question 6

Etoposide

Answer 6

Epipodophyllotoxins
These agents lead to DNA double-strand breaks and
cause errors in DNA replication (and eventually apoptosis).

Question 7

Cyclophosphamide

Answer 7

Alkylating agents
These agents cause irreversible changes especially in DNA, often leading to cross-linking. They have
(unwanted) mutagenic, teratogenic and carcinogenic effects.

Question 8

Doxorubicin

Answer 8

Antitumor antibiotics
These agents often intercalate into DNA and inhibit gene transcription. Many were isolated from
Streptomyces.

Question 9

Irinotecan, Topotecan.

Answer 9

Topoisomerase I inhibitors
Camptothecins:
These agents bind to DNA topoisomerase I, which leads to single-strand breaks in
the DNA and inhibits replication as well as transcription

Question 10

Cisplatin,

Carboplatin

Answer 10

Platinum compounds

Induce crosslinks in DNA, thereby blocking DNA replication and transcription

Question 11

Tamoxifen

Answer 11

(estrogen receptor antagonist) for postmenopausal breast cancer

Question 12

Enzalutamide

Answer 12

(androgen receptor antagonist) for prostate carcinoma.

Question 13

Tretinoin

Answer 13

(All-trans retinoic acid/ATRA)
Acid form of Vitamin A; treatment of Acute Promyelocytic Leukemia (APL) that harbors PML-RARα
gene fusion; induces differentiation of undifferentiated cancer cells

Question 14

Imatinib/Gleevec

Answer 14

-targets ABL (including BCR-ABL), KIT, PDGF receptor
-used for CML (chronic myeloid leukemia): Philadelphia chromosome-positive; has BCR-ABL fusion
protein; displays hyperproliferation of granulocytes
-also used for therapy of GIST (gastrointestinal stromal tumor): targets in this case KIT

Question 15

Trastuzumab

Answer 15

Herceptin: anti-HER2 antibody

Question 16

Lapatinib

Answer 16

HER2 kinase inhibitor (also effective on EGFR)

Question 17

HER2 inhibitors

Answer 17

HER2 (EGFR2) amplification in breast cancer correlates with adverse prognosis

Question 18

Erlotinib

Answer 18

EGFR kinase inhibitors

Question 19

Gefitinib

Answer 19

EGFR kinase inhibitors

Question 20

Cetuximab

Answer 20

EGFR inhibitors for squamous cell carcinoma and colon cancer–Anitbody

Question 21

Bevacizumab

Answer 21

• inhibits vascular endothelial growth factor (VEGF) and thereby angiogenesis
• FDA-approved for metastatic colorectal cancer and NSCLC

Question 22

Vemurafenib

Answer 22

Serine/Threonine Kinase Inhibitors
-targets V600E mutation of B-RAF (60% of all melanomas; FDA-approved for
late-stage melanoma)

Question 23

Bortezomib

Answer 23

Proteasome Inhibitors
-small molecule inhibitor of 26S proteasome; FDA-approved for multiple
myeloma

Question 24

Azactidine

Answer 24

DNA Demethylating Agents
-Myleodysplatic Syndrome
Direct and Irreversible inhibition of DNA methyltransferase (DNMT)
-Incorporated into DNA and RNA 
-Reactivation of tumor suppressor genes

Question 25

Vorinostat

Answer 25

Histone Deacetylase Inhibitor

• Cutaneous T-cell Lymphoma
• Reactivation of tumor suppressor genes