AntiCancer Drugs

Question 1

Cyclophosphamide

Answer 1

alkylating agent, cause cross linking DNA strands, not cell cycle specific, prodrug metabolized by CYP2B6

Side effect: hemorrhage cysts

used for” Acute and chronic lymphocytic leukemia, HL and NHL

Question 2

Cisplatin

Answer 2

platinum compound, forms intra- and inter- strand DNA crosslinks

Side Effect: Nephrotoxicity and ototoxicity

Question 3

Methotrexate

Answer 3

inhibits dihydrofolate reductase (needed to take THF to N5,10 methylene THF (one carbon donor in formation of dTMP))

Side Effects: Myelosuppression

Question 4

Leucovorin (Folinic Acid)

Answer 4

replenishes N5,10 methylene THF

RESCUES Methotrexate toxicity

ENHANCES toxicity of 5-FU

Question 5

5-Fluorouracil (5-FU)

Answer 5

prodrug that inhibits de novo thymidylate and DNA synthesis

Question 6

6-Mercaptopurine

Answer 6

prodrug that inhibits purine synthesis

Question 7

Vincristine

Answer 7

bind to Beta-Tubulin and inhibit microtubule polymerization during M Phase

Side Effect: Peripheral Neuropathy

Question 8

Vinblastine

Answer 8

bind to Beta-Tubulin and inhibit microtubule polymerization during M phase

Side Effect: Peripheral Neuropathy

Question 9

Paclitaxel

Answer 9

Binds to BetaTubulin and promotes microtbule polymerization during M Phase

Question 10

Etoposide

Answer 10

Inhibits Topoisomerase II, creating double strand DNA breaks and cell death

Used in HL, NHL, AML, ALL

Question 11

Doxorubicin

Answer 11

intercalates DNA, inhibits Topoisomerase II

Side Effect: Cardiotoxicity

Question 12

Bleomycin

Answer 12

binds to iron to generate oxygen free radicals, causing DNA strand breaks

Side Effect: Pulmonary Fibrosis

Used in HL, NHL

Question 13

Prednisone

Answer 13

induces apoptosis, inhibits cytokine production alters oncogene expression, induces cell cycle arrest

Used in ALL, AML, CLL, CML, HL

Question 14

Dexamethasone

Answer 14

induces apoptosis, inhibits cytokine production alters oncogene expression, induces cell cycle arrest

Used in Leukemia, Lymphoma, Multiple Myeloma

Question 15

Asparaginase

Answer 15

depletes extracellular asparagine to induce leukemic cell death

Used for ALL

Question 16

Imatinib

Answer 16

1st generation protein tyrosine kinase inhibitor (blocks ATP binding site)

Used for CML

Question 17

Asciminib

Answer 17

3rd generation PTK inhibitor, overcomes “gatekeeper mutation”, allosteric inhibitor that causes conformational change

Side Effects: Pancreatitis

Question 18

Ivosidenib

Answer 18

IdH1 inhibitor, blocks production of 2-hydroxygluterate, inhibiting demethylase and stopping cell differentiation

Question 19

Enasidenib

Answer 19

IdH2 inhibitor, blocks production of 2-hydroxygluterate, inhibiting demethylase and stopping cell differentiation

Question 20

Nivolumab / Pembrolizumab

Answer 20

Block action of PDL 1, reactivated CD8 T Cells to Kill Lymphoma Cells

Used for HL

Question 21

Omacetaxine

Answer 21

inhibits protein translation by targeting ribosome assembly, overcomes gatekeeper mutation

Question 22

Brentuximab Vedotin

Answer 22

Brentuximab: targets CD30, delivers MMAE
Vedotin: inhibits microtubule polymerization

Used in HL