TABLE 4

Determination of CYP3A4/5 contribution to the metabolic clearance obtained in human hepatocytes for 12 marketed drugs

Data are means ± S.D. of three independent experiments.

CompoundsCLint (µl/min per 106 hepatocytes)Predicted In Vitro Fm,CYP3A4/5Observed In Vivo Fm,CYP3A4/5References
ControlWith Azamulin
Midazolam56 ± 4.63.4 ± 0.60.94 ± 0.010.84–0.99Galetin et al., 2006; Shou et al., 2008; Xu et al., 2011
Felodipine69 ± 5.49.9 ± 1.00.86 ± 0.010.81–0.99Galetin et al., 2006
Simvastatin153 ± 1627 ± 1.00.82 ± 0.010.83–0.99Shou et al., 2008; Xu et al., 2011
Quinidine2.9 ± 0.50.81 ± 0.30.73 ± 0.040.61–0.76Galetin et al., 2006; Shou et al., 2008
Sildenafil29 ± 2.48.3 ± 1.30.71 ± 0.020.66–0.82Shou et al., 2008; Xu et al., 2009
Nifedipine56 ± 5.510 ± 1.70.82 ± 0.020.63–0.71Galetin et al., 2006; Shou et al., 2008; Xu et al., 2011
Loperamide15 ± 0.47.6 ± 0.70.48 ± 0.060.62Tayrouz et al., 2001
Zolpidem2.7 ± 0.50.97 ± 0.30.63 ± 0.110.41Xu et al., 2011
Pimozide7.6 ± 0.72.7 ± 0.50.65 ± 0.070.40Galetin et al., 2006
Cerivastatin7.2 ± 0.75.8 ± 3.40.46 ± 0.030.37Galetin et al., 2006
Mirtazapine5.6 ± 0.24.2 ± 0.20.26 ± 0.030.33Notice FDA
Metoprolol2.1 ± 0.61.8 ± 0.40.10 ± 0.130.15Xu et al., 2009