TABLE 2

Ketoconazole IC50 values for metabolism of CYP3A substrates in monkey intestinal and liver microsomes

Seven CYP3A substrates (200 nM, final concentration) were incubated at 37°C for 15 min with pooled intestinal and liver microsomes from cynomolgus monkeys (MIM and MLM) in the absence or presence of various concentrations of ketoconazole, respectively. Each value presents the mean of duplicate measurements.

CompoundsIC50
MIMMLM
μM
Buspirone0.0080.045
Felodipine0.0070.100
Midazolam0.0100.016
Nicardipine0.0150.036
Nifedipine0.0180.086
Saquinavir0.0560.087
Verapamil0.0430.233