TABLE 6

Clearances, intracellular concentrations, and error obtained with the five-compartment model, with apical efflux out of the cell

Data from both experiments 1 and 2 were used.

Drug	Experiment	f_um	CL_iavg	CL_ae	Error	C_cell,ABpass	C_cell,BA	C_cell,ABeff	C_cell,BAeff	C_cell,AB Ratio	C_cell,BA Ratio
			μl/min			μM
Amprenavir	1	0.39	26	2600	1.1	0.8	1.8	0.013	0.027	62	68
Atorvastatin	1	0.32	5.1	100	3.8	0.51	0.72	0.042	0.055	12	13
Atorvastatin	2	0.32	4.5	17	1.7	0.51	0.59	0.15	0.19	3.3	3
Digoxin	1	0.8	2.2	80	1.1	0.95	2.1	0.055	0.062	17	34
Digoxin	2	0.8	1.7	30	0.81	1.1	1.8	0.1	0.11	10	16
Labetalol	1	0.75	1.4	34	6.8	0.94	1.3	0.061	0.066	15	19
Labetalol	2	0.75	2	14	4.4	1.3	1.5	0.23	0.25	5.6	6.1
Loperamide	1	0.25	29	2100	1.2	0.5	1.3	0.012	0.027	41	47
Loperamide	2	0.25	13	640	3.2	0.48	1	0.018	0.032	26	33
Minoxidil	1	0.93	0.74	0.36	1.8	1.8	1.9	1.3	1.4	1.4	1.4
Minoxidil	2	0.93	0.61	0.34	2.4	1.7	1.8	1.2	1.2	1.4	1.5
Pitavastatin	1	0.39	4.1	28	6.6	0.64	0.7	0.12	0.15	5.3	4.7
Pitavastatin	2	0.39	5.4	16	2.5	0.73	0.83	0.24	0.32	3	2.6
Repaglinide	1	0.74	10	530	1.4	1.6	2.5	0.04	0.061	41	41
Simvastatin	1	0.36	13	15	0.66	0.76	1.4	0.45	0.75	1.7	1.9
Verapamil	1	0.5	33	820	0.94	1	2.3	0.059	0.13	17	17

f_um, fraction of drug unbound in microsomal membrane; CL_iavg, arithmetic mean of CL_iAB and CL_iBA; CL_ae, apical efflux clearance; C_cell,ABpass, predicted intracellular concentration from A-B experiments with passive diffusion only (MDCK cells); C_cell,BApass, predicted intracellular concentration from B-A experiments with passive diffusion only (MDCK cells); C_cell,ABeff, predicted intracellular concentration from A-B experiments with passive diffusion plus apical efflux (MDR1-MDCK cells); C_cell,BAeff, predicted intracellular concentration from B-A experiments with passive diffusion plus apical efflux (MDR1-MDCK cells); C_cell,AB ratio, ratio of C_cell,ABpass to C_cell,ABeff; C_cell,BA ratio, ratio of C_cell,BApass to C_cell,BAeff.