Anti-Cancer Flashcards
Methotrexate
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)
Leucovorin
Tx Methotrexate toxicity by getting folate to WBCs
5-flurouracil and Capecitabine
Pyrimidine (T) analog
MOA: inhibit Thymidilate synthase (after activation to FdUMP)
SE: Hand-foot syndrome, neurotoxic, BMS, N/V/D
Cytarabine
Pyrimidine (C) analog
MOA: inhibit DNA polymerase after phosphorylation and incorporation in DNA (prodrug)
SE: BMS, N/V/D, CNS toxicity
Mercaptopurine
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
6-Thioguanine
Purine (G) analog
MOA: activated by HGPRTase to monophosphate, inhibit PRPP anidotransferase (1st and rate-limiting step in purine synthesis)
Effect: 👇🏽G
Use: AML
Alkylating agents
Non-cell cycle specific
MOA: target N7 of guanine, intrastate linking and cross-linking of strands
SE: increased risk of leukemia/lymphoma
Cyclophosphamide and Ifosfamide
Nitrogen Mustard
SE: hemorrhagic cystitis d/t a role in metabolite
Toxicity tx: MESNA
Mechlorethamine
Nitrogen Mustard
Use: Hodgkin
SE: severe N/V, powerful vesicant
Melphalan
Nitrogen mustard
Use: MM
SE: oral ulceration, pulmonary fibrosis
Cisplatin
Platinum analog
SE: nephrotoxicity (give Amifostine), severe N/V (give Ondansetron), permanent ototoxicity, peripheral neuropathy
NO severe BM suppression
Carboplatin
Platinum analog
- less toxic than Cisplatin
Oxaliplatin (not on Pharm MT)
Platinum analog
- no nephrotoxicity / ototoxicity
Procarbazine
Methylhydrazine
Use: Hodgkin
SE: Disulfiram-like effect, metabolite of the drug is MAOI (avoid TCAs, tyramine-containing foods and MAOIs)
Carmustine and Lomustine
Nitrosureas
MOA: crosses BBB
Use: glioblastoma
SE: BMS, N/V, interstitial pneumonitis
Busulfan
Use: CML
SE: BMS, pulmonary fibrosis
Vinblastine
Vinca alkaloid MOA: M-phase specific, inhibition of microtubule polymerization Effect: arrest in metaphase Use: HL and NHL SE: BMS, constipation, SIADH, vesicant
Vincristine
Vinca alkaloid MOA: M-phase specific inhibition of microtubule polymerization Effect: arrested in metaphase Use: HL and NHL, peds tumors SE: peripheral neuropathy, SIADH
Paclitaxel
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
Docetaxel
Taxane
MOA: M-phase specific, inhibit microtubule depolymerization
Effect: arrested in prophase
SE: fluid retention (pre-tx w/ steroid), HS rxns
Irinotecan
Camptothecin analog
MOA: S-phase specific, inhibition of Topoisomerase I
PK: eliminated by bile
Use: mets colorectal ca
Topotecan
Camptothecin analog
MOA: S-phase specific, inhibition of Topoisomerase I
Use: ovarian ca, small cell lung ca
SE: BMS
Etoposide and Teniposide
Epipodophyllotoxins
MOA: S-phase specific, inhibition of Topoisomerase II
SE: HS rxn, BMS
Actinomycin D (not on Pharm MT)
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
Bleomycin
MOA: G2-phase specific, binds to iron and forms free radicals
SE: pulmonary fibrosis, skin rxn (hyperpigmentation)
Doxorubicin and Daunorubicin
MOA: intercalated in DNA and form free radicals, also block Topoisomerase II
SE: cardiomyopathy (give Dexrazoxane to reduce), desquamation, red-orange urine color
Dexrazoxane
Prevents cardiomyopathy d/t Daunorubicin and Doxorubicin by inhibiting the Fenton rxn (chelating iron)
Tamoxifen
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)
Fulvestrant
MOA: pure antagonist of ER
Effect: increases ER degradation
Use: Tamoxifen-resistant breast ca
SE: menopause sx’s
Anastrozole and Letrozole
MOA: competitive aromatase inhibitor (non-steroidal)
Use: adjuvant in ER+ breast ca
Exemestane
MOA: irreversible inhibitor of aromatase (steroidal)
Flutamide
MOA: competitive antagonist of androgen receptor
Use: prostate ca
SE: gynecomastia
Goserelin and Leuprolide
MOA: GnRH analog, initial surge in LH, FSH, and Testosterone = coadminister Flutamide
Effect: downregulation of GnRH receptor = 👇🏽FSH, LH and Testosterone
Use: prostate ca
Trastuzumab
MOA: ErbB2
SE: cardiotoxic
Imatinib
MOA: inhibits bcr-abl (CML), c-kit (GI stromal tumor)
Use: CML, GI stromal tumor, idiopathic hypereosinophilic syndrome
Sorafenib
MOA: TK inhibitor
Use: RCC
Bortezomib
MOA: proteasome inhibitor
Use: MM, mantle Cell lymphoma
Sunitinib
MOA: TK inhibitor
Use: RCC, GI stromal tumor
Asparaginase
MOA: depletion of asparagine
Use: ALL
SE: pancreatitis, 👇🏽insulin👇🏽clotting factors
Hydroxyurea
MOA: S-phase specific, inhibit ribouncleotide reductase
Effect: depletion of deoxyribonucleosides
Interferon α
MOA: stimulates NK cells to kill transformed cells, increases HLA expression on tumor cells
Use: Kaposi sarcoma, hairy cell, RCC
Gefitinib
Use: non-small cell lung ca
Erlotinib
Use: non-small cell lung ca, pancreatic carcinoma
Cetuximab
Use: colorectal ca (w/ wild KRAS), head/neck ca)
Lapatinib
MOA: Inhibit EGFR and ErbB2
Use: non-small cell lung ca, pancreatic carcinoma
