Comparison of the inhibition potentials of icotinib and erlotinib against human UDP-glucuronosyltransferase 1A1

The inhibitory potentials of icotinib and erlotinib against UDP-glucuronosyltransferase 1A1 (UGT1A1) were investigated and compared for the first time. Icotinib exhibited relatively weak inhibition against UGT1A1 in human liver microsomes compared to erlotinib. In addition, icotinib was unlikely to cause a significant drug-drug interaction (DDI) through inhibition of UGT1A1, while erlotinib exhibited much higher DDI potentials.147