TABLE 4

The K_m,u, V_max, P_dif,u, CL_int, and percentage of active uptake values generated for pravastatin, rosuvastatin, repaglinide, and pitavastatin in OATP1B1 and OATP1B3 overexpressing cells in buffer and human plasma (n = 3)

CL_int = V_max/K_m,u.

Compound	Transporter	Incubation	K_m,u	V_max	K_m,u (Reported in the Literature)	P_dif,u	CL_int	Active uptake
			μM	pmol/min per milligram	μM	μl/min per milligram	μl/min per milligram	%
Pravastatin	OATP1B1	Buffer	84.9 ± 19.8	274 ± 29.1	85.7^{^a}, 104^{^b}, 109^{^c}	0.159 ± 0.0143	3.23 ± 0.827	95.3
		Plasma	44.5 ± 12.8	224 ± 29.7		0.614 ± 0.0419	5.03 ± 1.59	89.1
		Fold difference (Buffer/Plasma)	1.91	1.22
		Fold difference (Plasma/Buffer)				3.86	1.56
	OATP1B3	Buffer	57.5 ± 11.5	179 ± 14.5	228^{^b}	0.159 ± 0.0143	3.11 ± 0.672	95.1
		Plasma	28.5 ± 7.02	145 ± 14.2		0.614 ± 0.0419	5.09 ± 1.35	89.2
		Fold difference (Buffer/Plasma)	2.02	1.23
		Fold difference (Plasma/Buffer)				3.86	1.63
Rosuvastatin	OATP1B1	Buffer	22.2 ± 5.25	132 ± 14.5	9.31^{^d}, 13.0^{^e}, 13.1^{^f}	0.677 ± 0.0407	5.95 ± 1.55	89.8
		Plasma	3.25 ± 1.41	50.0 ± 8.47		2.64 ± 0.116	15.4 ± 7.17	85.4
		Fold difference (Buffer/Plasma)	6.83	2.64
		Fold difference (Plasma/Buffer)				3.90	2.59
	OATP1B3	Buffer	18.0 ± 1.74	156 ± 6.57	14.2^{^g}, 16.5^{^e}	0.677 ± 0.0407	8.67 ± 0.914	92.8
		Plasma	5.61 ± 1.17	37.1 ± 3.60		2.64 ± 0.116	6.61 ± 1.52	71.5
		Fold difference (Buffer/Plasma)	3.21	4.20
		Fold difference (Plasma/Buffer)				3.90	0.762
Repaglinide	OATP1B1	Buffer	1.07 ± 0.414	42.9 ± 9.50	1.36^{^d}	48.6 ± 1.78	40.1 ± 17.9	45.2
		Plasma	0.0100 ± 0.00587	1.98 ± 0.501		84.2 ± 2.70	198 ± 126	70.2
		Fold difference (Buffer/Plasma)	107	21.7
		Fold difference (Plasma/Buffer)				1.73	4.94
	OATP1B3	Buffer	N/A	N/A	N/A	48.6 ± 1.78	N/A	N/A
		Plasma	N/A	N/A		84.2 ± 2.70	N/A	N/A
		Fold difference (Buffer/Plasma)					N/A
		Fold difference (Plasma/Buffer)				1.73
Pitavastatin	OATP1B1	Buffer	5.29 ± 0.984	111 ± 10.1	1.30^{^h}, 2.48^{^d}, 3.00^ⁱ	6.33 ± 0.109	21.0 ± 4.35	76.8
		Plasma	0.00855 ± 0.00413	5.69 ± 1.29		148 ± 18.9	665 ± 355	81.8
		Fold difference (Buffer/Plasma)	619	19.5
		Fold difference (Plasma/Buffer				23.4	31.7
	OATP1B3	Buffer	8.80 ± 0.748	152 ± 7.46	2.60^{^j}, 3.25^ⁱ	6.33 ± 0.109	17.3 ± 1.70	73.2
		Plasma	0.0157 ± 0.0270	1.56 ± 1.54		148 ± 18.9	99.4 ± 192	40.2
		Fold difference (Buffer/Plasma)	561	97.4			0.174
		Fold difference (Plasma/Buffer)				23.4	5.75

↵^a Kameyama et al. (2005).
↵^b Kindla et al. (2011).
↵^c Furihata et al. (2009).
↵^d Izumi et al. (2015).
↵^e Bosgra et al. (2014).
↵^f van de Steeg et al. (2013).
↵^g Kitamura et al. (2008).
↵^h Sharma et al. (2012).
↵ⁱ Hirano et al. (2004).
↵^j Vildhede et al. (2016).
N/A, Not Applicable.