TABLE 1

Time- and concentration-dependent transport of apixaban in human P-gp-transfected porcine kidney cells (LLC-PK₁-P-gp) and control cells (LLC-PK₁, Mock)

Cell Line	Apixaban	Time	Pc_app  Mean ± S.D.		Efflux Ratio Mean ± S.D.	P-gp-Facilitated Transport
			A-B	B-A	B-A/A-B	IA	V
	μM	min	nm/s	nm/s		pmol	pmol/cm²per hour
P-gp	10	60	4.3 ± 0.2	130 ± 16	30 ± 3.3	146 ± 23	471 ± 76
	10	90	5.1 ± 0.3	160 ± 9.3	31 ± 2.3	235 ± 20	505 ± 43
	10	120	4.4 ± 0.4	170 ± 9.2	38 ± 1.5	294 ± 13	474 ± 22
Control	10	60–120	31–44.1	74–97	1.7–3.2	NA	NA
P-gp	2.5	90	9.4 ± 2.6	210 ± 9.3	23 ± 4.9	33 ± 13	71 ± 28
	5.0	90	5.5 ± 0.1	200 ± 11	36 ± 2.2	64 ± 12	139 ± 26
	10	90	6.2 ± 0.2	200 ± 11	31 ± 1.9	167 ± 58	360 ± 125
	25	90	6.1 ± 0.6	220 ± 4.2	36 ± 4.3	548 ± 99	1179 ± 213
	50	90	6.9 ± 0.6	240 ± 9.5	35 ± 4.6	1485 ± 69	3194 ± 148
	100	90	5.7 ± 0.6	210 ± 9.3	36 ± 4.9	2772 ± 109	5962 ± 234
Control	2.5–100	90	34–60.3	84–150	1.4–4.4	NA	NA

A-B, apical-to-basolateral; B-A, basolateral-to-apical; IA, intrinsic activity; NA, not applicable; P-gp, permeable glycoprotein; V, rate of transport.