Table 2

In vitro clearance at low substrate concentrations of substrate by CYP3A4, CYP3A5, and CYP3A7

ml/min/nmol P450
1′-OH Midazolam3.343.310.02
4-OH Midazolam0.990.150.04
1′-OH Alprazolam0.050.030.003
4-OH Alprazolam1.100.340.02
1′-OH Triazolam0.540.140.004
4-OH Triazolam0.300.050.061
N-Desmethyl diltiazem0.690.200.18
6β-OH Testosterone2.340.060.02
N-Desmethyl clarithromycin51.24.305.06
14-OH Clarithromycin7.030.230.53
2-OH Estradiol0.440.010.005
4-OH Estradiol0.100.0060.0002
Oxidized nifedipine5.00.240.08
7-Hydroxy-4-trifluoro methylcoumarin0.02.00040.0006
N-Desmethyl tamoxifen0.280.130.045

Clearance calculated from the slope of the velocity versus substrate concentration relationship at the lowest linear portion, which was the lowest 2 to 6 concentrations of substrate (1–6.25 μM MDZ; 1–12.5 μM APZ; 1–6.25 μM TZ; 3.12–12.5 μM DTZ; 1.56–12.5 μM TEST; 1–5 μM CLAR; 5–10 μM TAM; 1.56–6.25 μM E2; 0.62–5 μM NIF and 0.78–6.25 μM BFC).