TABLE 2

IC₅₀ values for CYP3A, CYP2C9, and CYP2D6 inhibitors from human hepatocyte suspensions in HMM and human plasma

Both HMM and plasma IC₅₀ values represent the nominal values obtained from each system. Each number represents the mean ± S.E. of estimate of triplicate determinations.

Inhibitor	IC₅₀		f_{u, p}
Inhibitor	HMM	Plasma	f_{u, p}
	μM
CYP3A inhibitors
Ketoconazole	0.28 ± 0.02	1.26 ± 0.23^{^a}	0.01
Fluconazole	27.00 ± 1.50	7.61 ± 2.67^{^a}	0.89
Voriconazole	22.40 ± 4.90	3.01 ± 0.58^{^a}	0.42
Conivaptan	1.90 ± 0.18	1.70 ± 0.56^{^a}	0.01
Nefazodone	0.49 ± 0.08	1.70 ± 0.31^{^a}	0.01
Aprepitant	Poor solubility	24.10 ± 7.30^{^a}	0.05
CYP2C9 inhibitors
Miconazole	2.12 ± 0.37	2.02 ± 0.37	0.1
Fluconazole	53.96 ± 2.95	14.34 ± 1.27	0.89
Sulfaphenazole	0.29 ± 0.06	9.49 ± 1.89	0.32
Fluvastatin	4.07 ± 1.84	6.78 ± 1.01	0.01
Ibuprofen	151.30 ± 29.25	>1200	0.01
Tolbutamide	101.08 ± 22.70	>1200	0.04
CYP2D6 inhibitors
Diphenhydramine	1.71 ± 0.19	30.54 ± 4.34	0.22
Sertraline	3.10 ± 0.34	13.97 ± 3.49	0.01
Quinidine	0.03 ± 0.01	0.02 ± 0.01	0.13
Paroxetine	0.03 ± 0.01	0.07 ± 0.02	0.05
Fluoxetine	0.04 ± 0.00	0.35 ± 0.09	0.06
Duloxetine	0.22 ± 0.04	0.67 ± 0.37	0.05

↵a Data are from Mao et al. (2011).