TABLE 1

A summary of the P450 isoform-selective substrates and their respective metabolites quantified for CHIM

IsoformSubstrateSubstrate ConcentrationMetabolites Quantified
µM
CYP1A17-Ethoxyresorufin20Resorufin
CYP1A2Phenacetin100Acetaminophen
CYP2A6Coumarin507-HC, 7-HC-sulfate, 7-HC-glucuronide
CYP2B6Bupropion500Hydroxybupropion
CYP2C8Paclitaxel206α-Hydroxypaclitaxel
CYP2C9Diclofenac254-Hydroxydiclofenac
CYP2C19S-Mephenytoin2504-Hydroxy S-mephenytoin
CYP2D6Dextromethorphan15Dextrorphan
CYP2E1Chlorzoxazone2506-Hydroxychlorzoxazone
CYP3A4/5-1Midazolam201-Hydroxymidazolam
CYP3A4/5-2Testosterone2006β-Hydroxytestosterone
CYP2J2Astemizole50O-Demethyl astemizole
  • HC, hydroxycoumarin.