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28 Cards in this Set
- Front
- Back
5-FU
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pyrimidine antimetabolite that blocks methylation of deoxyuricytic acid (blocks thymidine)
suicide inhibitor of thymidylate synthetase used with leucovorin/levamisole |
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levamisole
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modulates 5-FU activity and is an immune modulator
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capecitabine
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oral prodrug of 5-FU
carboxy-esterase in liver --> cytidine deaminase in liver/tumor --> thymidine phosphorylase in tumor |
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cytarabine
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nucleotide analog (Ara-C), prodrug that must be converted to triphosphate, inhibits DNA polyermase
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gemcitabine
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can be incorporated into DNA chains in place of cytosine and causes chain termination
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fludarabine
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nucleotide analog (Ara-A)
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nelrabine
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water-soluble prodrug of Ara-G
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pentostatin
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inhibits adenosine deaminase (increased adenosine levels inhibit RNA/DNA synth)
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cladribine
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inhibits adenosine deaminase (Cl atom makes it resistant to enzymatic attack)
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mercaptopurine/thioguanine
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prodrugs made into nucleotide precursors that block RNA/DNA synth
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methotrexate
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DHFR inhibitor
-uses leucovorin rescue |
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pemetrexed
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injectable; inhibits folypolyglutamate synthetase and DHFR
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reasons for increase cell growth
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increased ligand conc
increased # of receptors decreased receptor turnover receptor mutation |
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imitinib, sorafenib, dasatinib, sunitinib, nilotinib
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oral small molecules that inhibit multiple kinases
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imitinib vs dasatinib
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if resistant to imitinib, dasatinib may still works
-dasatinib's binding to ABL doesn't depend on P-loop (where mutaitons can occur) |
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gefitinib, erlotinib, lapatinib
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oral inhibitor of EGFR TK
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cetuximab
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IV Ab that inhibits EGFR dimerization
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panitumumab
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IV Ab that inhibits EGFR dimerization
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temsirolimus
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inhibits mTOR (immunosuppression and inhibits cancer cell/fungal growth)
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endostatin
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inhibits angiogenesis
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bevacizumab
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inhibits VEGF receptor
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rituximab
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binds CD20 on B cells and recruits Abs
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herceptin
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Ab that binds HER2 receptor (HER2 promotes breast cancer)
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bexaar, oncolym, lymphocide
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uses I-131
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zavalin
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uses yttrium-90 or indium-111
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gemtuzumab
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binds CD33, delivers calicheamicin into cells that binds DNA, forms diradical, cuts DNA and kills cell
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IL-2, IFN-alpha
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stims specific aspects of immune system
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denileukin
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NOT Ab (fusion protein)
binds IL-2 receptor on cancerous T-cells recognized by T-cells, taken up, attached diptheria toxin kills cell by inhibiting protein synthesis |