TABLE 1

Physicochemical properties, unbound fraction in variety of matrices, intrinsic metabolic clearance in rat hepatocytes of the selected 12 compounds

	Physicochemical properties				Unbound fraction in matrices				Intrinsic metabolic CL
	M.W.	Log D_7.4^{^a}	pKa^{^a}	P_app	f_{u, liver tissue}	f_{u, KHB w 4%BSA}	f_{u, p}	f_{u, hep}	Rat hepatocyte CL_int,met
				10⁻⁶ cm/s					µl/min per 10⁶ cells
Rosuvastatin	481.5	−2.7	4.3	1.8	0.15	0.21	0.059	0.77	19.8
Pravastatin	424.5	−0.8	4.3	0.62	0.29	0.69	0.63	0.85	NA
Valsartan	435.5	−0.6	3.7, 4.2	0.14	0.048^{^b}	0.006^{^c}	0.0029	0.79	20.4
Pitavastatin	421.5	0.4	4.2, 5.2	13	0.019	0.057	0.0065	0.56	46.2
Fluvastatin	411.5	0.5	4.3	19	0.015	0.037	0.015	0.51	38.8
Cerivastatin	459.6	0.6	4.2, 5.6	28	0.019	0.04	0.029	0.59	47.9
Nateglinide	317.4	0.6	3.6	6.2	0.037	0.063	0.015	0.73	43.5
Atorvastatin	558.6	1.3	4.3	5.5	0.018	0.066	0.036	0.63	90.8
Bosentan	551.6	1.5	4.0	16	0.025	0.057	0.0089	0.66	39.4
Glyburide	494.0	1.9	5.2	22	0.011	0.014	0.002	0.60	54.5
Asunaprevir	748.3	2.3	3.9, 5.6	1.7	0.00073	0.059	0.013	0.31	36.2
Telmisartan	514.6	4.0	3.5, 3.9, 5.0	29	0.0038	0.031	0.0061	0.45	23.3