TABLE 3

Kinetic parameters for the initial uptake rates of pitavastatin, rosuvastatin, and pravastatin in rat hepatocytes

Values are shown as the mean ± S.D.

Drug	V_max^{^a}	K_m^{^a}	V_max/K_m	PS_dif^{^a}	K_p,uu,V0^{^b}	f_T,cell,V0^{^b}
	pmol/min/10⁶ Cells	μM	μL/min/10⁶ Cells	μL/min/10⁶ Cells
Pitavastatin	893 ± 124	5.43 ± 1.29	164 ± 45	3.00 ± 1.41	55.8 ± 29.9	0.172 ± 0.131
Rosuvastatin	250 ± 80	2.86 ± 1.82	87.4 ± 62.3	1.76 ± 1.15	50.7 ± 48.0	0.649 ± 0.688
Pravastatin	178 ± 11	20.3 ± 1.4	8.77 ± 0.81	1.16 ± 0.08	8.56 ± 0.87	0.685 ± 0.428

↵^a The initial uptake rate in rat hepatocytes was calculated from the uptake of [³H]pitavastatin, [³H]rosuvastatin, and [³H]pravastatin for 0.5–1.5 minutes. Kinetic parameters are obtained by fitting to the data at seven concentrations (0.1, 0.3, 1, 3, 10, 30, and 100 µM for all statins; Supplemental Fig. 2) using eq. 4.
↵^b The K_p,uu,V0 and f_T,cell,V0 were calculated using eqs. 5 and 6, respectively. C/M ratios at 37°C (Table 2) were used for the calculation of the f_T,cell,V0.