Table 1

Probe reactions used to characterize enzyme activities, surveyed from 194 drugs approved from US-FDA from 1992 to 1997 period

EnzymesSubstrate Reactions
CYP1A1EthoxyresorufinO-deethylation
CYP1A2PhenacetinO-deethylation, caffeine 3-demethylation, ethoxyresorufinO-deethylation
CYP2A6Coumarin 7-hydroxylation
CYP2B67-Ethoxy-4-trifluoromethyl coumarinO-dealkylation
CYP2C8/9Tolbutamide 4′-hydroxylation,S-warfarin 7′-hydroxylation, diclofenac 4′-hydroxylation
CYP2C19 S-Mephenytoin 4′-hydroxylation
CYP2D6Dextromethorphan O-Demethylation, bufuralol 1′-hydroxylation, debrisoquine 4-hydroxylation, sparteine oxidation
CYP2E1Chlorzoxazone 6-hydroxylation, debrisoquine, sparteine oxidation, p-nitrophenol
CYP3A4/5Nifedipine oxidation, testosterone 6β-hydroxylation, erythromycinN-demethylation, cyclosporine oxidation, benzodiazepine hydroxylation (midazolam, triazolam, alprazolam), terfenadine hydroxylation
CYP4ALauric acid hydroxylation