Topoisomerase/Microtubule Inhibitor Flashcards
Irenotecan class
topo I inhibitor
irenotecan cell cycle target
s phase
irenotecan resistance
PgP overexpression
GST overexpression
topo down regulation/mutation
what should be tested before starting irenotecan
UGT1A1 for low expression
doxorubicin class
topo II inhibitor
intercolator
free radical damage
doxorubicin cell cycle target
non specific
doxorubicin dose limiting side effects
cardiotoxicity & local tissue damage
what drug should be given with doxorubicin
dexrazoxane
doxorubicin resistance
PgP & MRP overexpression
GST over expression
Topo II downregulation/mutation
increase in DNA repair
Etoposide class
Topo II inhibitor
etoposide cell cycle target
G2 cell block
etoposide resistance
PgP & MRP overexpression
Topo II downregulation/mutation
increase in DNA repair
Bleomycin class
intercolator
free radical damage
bleomycin cell cycle target
G2 and M phase
bleomycin dose limiting side effect
pulmonary toxicity
Vincristine class
microtubule destabilizer
vincristine cell cycle target
G2 and M phase
vincristine dose limiting side effect
neurotoxicity
vincristine resistance
PgP pumping drug out
Paclitaxel class
microtubule stabilizer
Paclitaxel cell cycle target
M phase
Paclitaxel dose limiting side effects
myelosuppression/neurotoxicity
Paclitaxel resistance
PgP pumping drug out
erubulin class
microtubule destabilizer
erubulin cell cycle target
G2 and M phase
erubulin dose limiting side effects
lower neurotoxicity
ixabepilone class
microtubule stabilizer
ixabepilone cell cycle target
m phase
ixabepilone resistance
not cross resistance and poor pgp substrate
