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Human Disease Systems > Anti-Cancer Drugs > Flashcards

Anti-Cancer Drugs Flashcards

1
Q

purine inhibitors

A

6-mercaptopurine, azathioprine, pentostatin, cladribine

6-mercaptopurine, azathioprine
-MOA: converted to T-IMP by hypoxanthine-guanine phosphoribosyltransferase (HGPRT); T-IMP inhibits IMPDH => decreased intracellular AMP and GMP; inhibits purine synthesis
-AE: myelosuppression, hepatoxicity, uricemia, GI upset, rash

pentostatin
-MOA: inhibits adenosine deaminase and homocysteine hydrolase => increased homocysteine (toxic to lymphocytes)
-AE: myelosuppression, nephro/neurotoxicity

cladribine
-MOA: incorporates into DNA causing strand breakage; depletes pools of NAD and ATP

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2
Q

pyrimidine inhibitors

A

cytarabine, gemcitabine, 5-fluorouracil, capecitabine (prodrug)

cytarabine
-MOA: inhibits DNA polymerase by competing with CTP for binding => chain termination
-AE: myelosuppression, ulceration of GI mucosa, nausea/vomiting

gemcitabine
-MOA: competitively inhibits DNA polymerase in inhibits DNA chain elongation
-AE: nausea, vomiting, flu-like symptoms

5-fluorouracil, capecitabine
-MOA: converted to FdUMP => inhibits thymidylate synthase => thymine depletion => FdUTP incorporates into DNA
-AE: myelosuppression, cardiotoxicity, GI ulcers, alopecia, thymine depletion, CNS/visual alterations, hand-foot syndrome, Steven-Johnson syndrome (capecitabine)

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3
Q

folate analogues

A

methotrexate

MOA: inhibits thymidylate synthase and dihydrofolate reductase (DHFR), preventing DNA synthesis

AE: myelosuppression, folate deficiency*, thymine depletion, mouth ulcers, nephro/hepatotoxic, pulmonary fibrosis, teratogenic

*leucovorin (folinic acid) nonenzymatically generates THFs - protects/rescues normal cells from folate deficiency

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4
Q

taxanes

A

paclitaxel, docetazel

MOA: bind beta-tubulin, inhibiting depolymerization

AE: myelosuppression (docetaxel), neuropathy (paclitazel), mucositis, tumor lysis syndrome

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5
Q

vinca alkaloids

A

vincristine, vinblastine

MOA: bind beta-tubulin, inhibiting polymerization

AE:
neurotoxicity (vincristine), myelosuppression (vinblastine), alopecia, nausea/vomiting

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6
Q

topoisomerase inhibitors

A

topotecan, irinotecan, etoposide

topotecan, irinotecan
-MOA: inhibits topoisomerase I
-AE: myelosuppression, diarrhea

etocposide
-MOA: inhibits topoisomerase II
-AE: myelosuppression, alopecia, tumor lysis syndrome*

*rasburicase metabolizes uric acid produced by TLS

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7
Q

hydroxyurea

A

MOA: binds iron and tyrosine radical at ribonucleotide reductase so it cannot convert nucleotides to deoxynucleotides => inhibits DNA synthesis

AE: severe myelosuppression, megaloblastic anemia

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8
Q

bleomycin

A

MOA: generates free radicals due to iron/oxygen interaction, causing strand breakage

AE: pulmonary fibrosis, alopecia, stomatitis

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9
Q

cytotoxic antibiotics

A

dactinomycin (actinomycin D)

MOA: binds DNA between G-C residues and inhibits topoisomerase II and RNA polymerase binding

AE: myelosuppression

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10
Q

anthracyclines

A

doxorubicin (hydroxydaunorubicin), daunorubicin

MOA: generates free radicals; DNA binding and strand breakage; topoisomerase II inhibition

AE: myelosuppression, alopecia, cardiomyopathy*

*dexrazoxane inhibits free radical formation, decreasing cardiomyopathy

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11
Q

triazenes

A

decarbazine/ temozolomide, procabazine

MOA: DNA methylation leads to strand breakage; generation of peroxide radicals leads to cellular toxicity

AE: myelosuppression, nausea/ vomiting

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12
Q

nitrogen mustards

A

cyclophosphamide, isosfamide, carmustine, lomustine

cyclophosphamide, isosfamide
-MOA: immunosuppressive and dose-dependent cross-linking of DNA strands
-AE: hemorrhagic cystitis, infertility, embryo toxicity, myelosuppression

carmustine, lomustine
-MOA: C-G cross-linking and RNA/RNA cross-linking
-AE: CNS toxicity (dizziness, ataxia, seizures), infertility, myelosuppression

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13
Q

platinums

A

cisplatin, carboplatin, oxaplatin

MOA: platinum binds two bases causing DNA cross-linking

AE: neuropathy, Faconi syndrome (nephrotoxicity), myelosuppression, nausea

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14
Q

cyclophosphamide and isosfamide are administered with [?]

A

mesna

binds to and inactivates toxic metabolite acrolein

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15
Q

sulfonates

A

busulfan

MOA: cross-links DNA via G-A bases

AE: severe myelosuppression, pulmonary fibrosis, skin hyperpigmentation

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16
Q

monoclonal antibodies

A

bevacizumab: VEGF

cetuximab, panitumamab: EGRF

pembrolizumab, nivolumab, cemiplimab: PD-1

durvalumab, atezolizumab, avelumab: PD-L1

ipilimumab: CTLA-4

trastuzumab: HER2

alemtuzumab: CD52

rituximab: CD20

AE: these cause increased risk of autoimmunity and infections

17
Q

small molecule inhibitors

A

imatinib: tyrosine kinase inhibitor (BCR-ABL genes)

ruxolitinib: JAK1/2 inhibition

bortezomib: proteosome inhibition

alectinib: ALK tyrosine kinase inhibition

gefitinib: EGFR tyrosine kinase inhibition

Human Disease Systems (11 decks)

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