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28 Cards in this Set

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