Table 3

Effect of substrate on the IC50 of various compounds for CYP3A4 in HLM

CompoundIC50
DextromethorphanMidazolamTestosterone
μM
Ketoconazole0.280.070.03
32.165.434.54
41.002.292.70
50.936.786.16
101.134.916.76
12>30.00>30.00>30.00
153.368.5815.90
180.541.860.69
2211.4031.613.80
230.681.872.05
251.033.765.40
260.999.981.89
2831.940.426.30
392.4710.66.49
440.811.340.85
4516.9035.004.68
5237.5066.4011.20