TABLE 2

Uptake kinetic parameters of seven OATP substrates estimated in rat hepatocytes by using a conventional two-step approach

Uptake kinetics was measured in freshly isolated rat hepatocytes plated for 2 h over 2 min at 10 concentrations (0.1–300 μM). Data represent mean of three experiments ± S.D., with the exception of fu_med of pravastatin (n = 1).

Drug	K_m,u^{^a}	V_max	P_diff,u^{^a}	fu_med	CL_active,u^{^a}	Maximal Proportion of Active Transport
	μM	pmol/min/10⁶ cells	μl/min/10⁶ cells		μl/min/10⁶ cells	%
Bosentan	6.39 ± 2.57	471 ± 112	3.39 ± 0.47	0.84 ± 0.13	77.8 ± 15.0	95.7 ± 1.2
Pitavastatin	21.0 ± 6.6	1380 ± 202	4.12 ± 2.00	0.86 ± 0.05	69.7 ± 21.0	93.6 ± 4.7
Pravastatin	37.0 ± 20.5	448 ± 329	0.323 ± 0.071	0.96	11.3 ± 2.8	97.2 ± 0.5
Repaglinide	18.0 ± 3.7	806 ± 308	6.62 ± 5.11	0.94 ± 0.02	44.1 ± 13.3	85.9 ± 13.1
Rosuvastatin	13.5 ± 3.9	1119 ± 218	0.345 ± 0.166	0.83 ± 0.04	84.6 ± 9.2	99.6 ± 0.2
Telmisartan	6.99 ± 3.72	548 ± 141	13.2 ± 8.4	0.77 ± 0.05	89.5 ± 31.7	86.8 ± 6.8
Valsartan	4.38 ± 1.40	128 ± 68	0.192 ± 0.035	1.0 ± 0.06	31.5 ± 16.6	99.2 ± 0.4

↵a Parameters are expressed relative to unbound media drug concentration.