Anti-Cancer

Question 1

Methotrexate

Answer 1

Anti-folate
MOA: inhibit DHF reductase
Effect: 👇🏽 T, A, G and 👇🏽 Ser and Met = 👇🏽protein synthesis
SE: pneumonitis, liver fibrosis, BMS, N/V/D
Toxicity tx: Leucovorin rescue to decrease SEs (mobilizes folate to WBCs)

Question 2

Leucovorin

Answer 2

Tx Methotrexate toxicity by getting folate to WBCs

Question 3

5-flurouracil and Capecitabine

Answer 3

Pyrimidine (T) analog
MOA: inhibit Thymidilate synthase (after activation to FdUMP)
SE: Hand-foot syndrome, neurotoxic, BMS, N/V/D

Question 4

Cytarabine

Answer 4

Pyrimidine (C) analog
MOA: inhibit DNA polymerase after phosphorylation and incorporation in DNA (prodrug)
SE: BMS, N/V/D, CNS toxicity

Question 5

Mercaptopurine

Answer 5

Purine (A and G) analog
MOA: activated by HGPRTase to monophosphate, inhibit PRPP anidotransferase (1st and rate-limiting step in purine synthesis)
Effect: IMP accumulation inhibits formation of AMP and GMP
Use: ALL
SE: hyperpigmentation, immunosuppression
*Azathioprine is prodrug of Mercaptopurine

Question 6

6-Thioguanine

Answer 6

Purine (G) analog
MOA: activated by HGPRTase to monophosphate, inhibit PRPP anidotransferase (1st and rate-limiting step in purine synthesis)
Effect: 👇🏽G
Use: AML

Question 7

Alkylating agents

Answer 7

Non-cell cycle specific
MOA: target N7 of guanine, intrastate linking and cross-linking of strands
SE: increased risk of leukemia/lymphoma

Question 8

Cyclophosphamide and Ifosfamide

Answer 8

Nitrogen Mustard
SE: hemorrhagic cystitis d/t a role in metabolite
Toxicity tx: MESNA

Question 9

Mechlorethamine

Answer 9

Nitrogen Mustard
Use: Hodgkin
SE: severe N/V, powerful vesicant

Question 10

Melphalan

Answer 10

Nitrogen mustard
Use: MM
SE: oral ulceration, pulmonary fibrosis

Question 11

Cisplatin

Answer 11

Platinum analog
SE: nephrotoxicity (give Amifostine), severe N/V (give Ondansetron), permanent ototoxicity, peripheral neuropathy
NO severe BM suppression

Question 12

Carboplatin

Answer 12

Platinum analog

- less toxic than Cisplatin

Question 13

Oxaliplatin (not on Pharm MT)

Answer 13

Platinum analog

- no nephrotoxicity / ototoxicity

Question 14

Procarbazine

Answer 14

Methylhydrazine
Use: Hodgkin
SE: Disulfiram-like effect, metabolite of the drug is MAOI (avoid TCAs, tyramine-containing foods and MAOIs)

Question 15

Carmustine and Lomustine

Answer 15

Nitrosureas
MOA: crosses BBB
Use: glioblastoma
SE: BMS, N/V, interstitial pneumonitis

Question 16

Busulfan

Answer 16

Use: CML
SE: BMS, pulmonary fibrosis

Question 17

Vinblastine

Answer 17

Vinca alkaloid
MOA: M-phase specific, inhibition of microtubule polymerization
Effect: arrest in metaphase
Use: HL and NHL
SE: BMS, constipation, SIADH, vesicant

Question 18

Vincristine

Answer 18

Vinca alkaloid
MOA: M-phase specific inhibition of microtubule polymerization
Effect: arrested in metaphase
Use: HL and NHL, peds tumors
SE: peripheral neuropathy, SIADH

Question 19

Paclitaxel

Answer 19

Taxane
MOA: M-phase specific inhibition of microtubule depolymerization
Effect: arrested in prophase
Use: solid tumors
SE: HS rxns (premeditate w/ steroid, diphenhydramine and H2RB), peripheral neuropathy

Question 20

Docetaxel

Answer 20

Taxane
MOA: M-phase specific, inhibit microtubule depolymerization
Effect: arrested in prophase
SE: fluid retention (pre-tx w/ steroid), HS rxns

Question 21

Irinotecan

Answer 21

Camptothecin analog
MOA: S-phase specific, inhibition of Topoisomerase I
PK: eliminated by bile
Use: mets colorectal ca

Question 22

Topotecan

Answer 22

Camptothecin analog
MOA: S-phase specific, inhibition of Topoisomerase I
Use: ovarian ca, small cell lung ca
SE: BMS

Question 23

Etoposide and Teniposide

Answer 23

Epipodophyllotoxins
MOA: S-phase specific, inhibition of Topoisomerase II
SE: HS rxn, BMS

Question 24

Actinomycin D (not on Pharm MT)

Answer 24

MOA: inhibition of RNA polymerase, binds to dsDNA and intercalated btwn adjacent G-C bp
Effect: stops transcription
Use: choriocarcinoma
SE: 
*α-Amanatin has same MOA

Question 25

Bleomycin

Answer 25

MOA: G2-phase specific, binds to iron and forms free radicals SE: pulmonary fibrosis, skin rxn (hyperpigmentation)

Question 26

Doxorubicin and Daunorubicin

Answer 26

MOA: intercalated in DNA and form free radicals, also block Topoisomerase II SE: cardiomyopathy (give Dexrazoxane to reduce), desquamation, red-orange urine color

Question 27

Dexrazoxane

Answer 27

Prevents cardiomyopathy d/t Daunorubicin and Doxorubicin by inhibiting the Fenton rxn (chelating iron)

Question 28

Tamoxifen

Answer 28

MOA: competitive inhibitor of estradiol binding to ER in breast tissue Use: ER+ breast ca SE: menopause sx’s (endometrial hyperplasia, decreased risk of MI d/t to lowering of LDL)

Question 29

Fulvestrant

Answer 29

MOA: pure antagonist of ER Effect: increases ER degradation Use: Tamoxifen-resistant breast ca SE: menopause sx’s

Question 30

Anastrozole and Letrozole

Answer 30

MOA: competitive aromatase inhibitor (non-steroidal) Use: adjuvant in ER+ breast ca

Question 31

Exemestane

Answer 31

MOA: irreversible inhibitor of aromatase (steroidal)

Question 32

Flutamide

Answer 32

MOA: competitive antagonist of androgen receptor Use: prostate ca SE: gynecomastia

Question 33

Goserelin and Leuprolide

Answer 33

MOA: GnRH analog, initial surge in LH, FSH, and Testosterone = coadminister Flutamide Effect: downregulation of GnRH receptor = 👇🏽FSH, LH and Testosterone Use: prostate ca

Question 34

Trastuzumab

Answer 34

MOA: ErbB2 SE: cardiotoxic

Question 35

Imatinib

Answer 35

MOA: inhibits bcr-abl (CML), c-kit (GI stromal tumor) Use: CML, GI stromal tumor, idiopathic hypereosinophilic syndrome

Question 36

Sorafenib

Answer 36

MOA: TK inhibitor Use: RCC

Question 37

Bortezomib

Answer 37

MOA: proteasome inhibitor Use: MM, mantle Cell lymphoma

Question 38

Sunitinib

Answer 38

MOA: TK inhibitor Use: RCC, GI stromal tumor

Question 39

Asparaginase

Answer 39

MOA: depletion of asparagine Use: ALL SE: pancreatitis, 👇🏽insulin👇🏽clotting factors

Question 40

Hydroxyurea

Answer 40

MOA: S-phase specific, inhibit ribouncleotide reductase Effect: depletion of deoxyribonucleosides

Question 41

Interferon α

Answer 41

MOA: stimulates NK cells to kill transformed cells, increases HLA expression on tumor cells Use: Kaposi sarcoma, hairy cell, RCC

Question 42

Gefitinib

Answer 42

Use: non-small cell lung ca

Question 43

Erlotinib

Answer 43

Use: non-small cell lung ca, pancreatic carcinoma

Question 44

Cetuximab

Answer 44

Use: colorectal ca (w/ wild KRAS), head/neck ca)

Question 45

Lapatinib

Answer 45

MOA: Inhibit EGFR and ErbB2 Use: non-small cell lung ca, pancreatic carcinoma