Anticancer Drugs

Question 1

Anti cancer drugs are most toxic to _____________

Answer 1

Rapidly dividing cells:
Bone marrow
GI tract
Hair follicles
Renal
Reproductive and teratogenesis

Question 2

MOA for alkylating agents

Answer 2

Alkylate DNA —> cause miscoding, breakage, crosslinking
Not cell-cycle specific
Most effect on rapidly proliferating cells

Question 3

Alkylating agent toxicity

Answer 3

POTENT VESICANTS —> cause major vesicle blisters, particularly at injection site (possible infection)

Question 4

Cyclophosphamide

Answer 4

Alkylating agent - most widely used
Can be taken orally
Must be given together with MESNA to deal with acrolein (or you’ll get hemorrhagic cystitis)

Question 5

Mechlorethamine

Answer 5

Alkylating agent for HL/NHL
Toxicity —> Renal Damage
COMBINE with allopurinol

Question 6

Carmustine

Answer 6

Great for brain tumors because cross BBB

Alkylating agent

Question 7

Cisplatin

Answer 7

Platinum analog
Cross-link DNA and “glunk” it up
Renal toxicity
ACOUSTIC NERVE DAMAGE - irreversable

Question 8

Doxorubicin

Answer 8

Antibiotic widely used against lymphomas, leukemia’s, sarcomas
Intercalated into DNA —> DNA destruction
CARDITOXIC (further increased by iron so give with an iron chelator like dexrazoxane)

Question 9

Methotrexate

Answer 9

Folate antimetabolite
Give Leucovorin AFTER methotrexate to rescue the folic acid
Major side fx: mucositis, thrombocytopenia

Question 10

6-Mercaptopurine

Answer 10

Converted by HGPRT to a ribonucleotide —> inhibits DNA synthesis
Resistance develops b/c of decreased level of HGPRT
Leucovorin given after 6-MP treatment to rescue the folic acid
DO NOT give with allopurinol —> fatal blood dyscrasias

Question 11

5-Fluorouracil

Answer 11

Inhibits thymidylate synthase (TS) —> blocks DNA synthesis
Response increased by leucovorin - given PRIOR to 5-FU administration
Biggest side fx = oral and GI ulcers

Question 12

Bleomycin Sulfate

Answer 12

Antitumor antibiotic
Specifically targets G2 and M of the cell cycle
KEY Fx:
• LITTLE MYELOSUPPRESSION
• Pulmonary fibrosis
• Hypersensitivity

Question 13

Vincristine/Vinblastine

Answer 13

Bind to tubular —> cell cycle arrest in metaphase
Neurotoxic
Vincristine - more neurotoxic, less myelosuppression
Vinblastine - less neurotoxic, more myelosuppression

Question 14

Paclitaxel

Answer 14

Binds beta-tubulin—> inhibits depolymerization

Adverse fx:
SEVERE MYELOSUPPRESSION
Anemia
Peripheral neuropathy

Question 15

Imatinib (Gleevec)

Answer 15

Only useful against CML because inhibits BCR-ABL

Side fx: Fluid retention - ankle and periorbital edema

Question 16

Cetuximab

Answer 16

Monoclonal antibody binds to EGF receptor to inhibit the tyrosine kinase activity —> growth inhibition and apoptosis

Question 17

Erlotinib

Answer 17

Blocks ATP binding to EGF receptor to inhibit the tyrosine kinase activity —> growth inhibition and apoptosis

Question 18

Epidermal growth factor inhibitors

Answer 18

Cetuximab
Erlotinib

Must test for EGFR expression and mutations

Question 19

Angiogenesis Inhibitor

Answer 19

Bevacizumab

Binds to VEGF and prevents binding to VEGF receptor

Can cause bleeding and thromboembolism