TABLE 2

Time- and concentration-dependent transport of apixaban in human breast cancer resistance protein (BCRP)-transfected canine kidney cells (MDCKII-BCRP) and control cells (MDCKII, Mock)

Cell LineApixabanTimePcapp 
Mean ± S.D.Efflux Ratio 
Mean ± S.D.BCRP-Facilitated Transport 
Mean ± S.D.
A-BB-A(B-A/A-B)IAV
μMminnm/snm/spmolpmol/cm2 per hour
BCRP11513.9 ± 6.0148 ± 7.510.7 ± 0.42.2 ± 0.612.6 ± 3.4
1302.5 ± 0.57.1 ± 1.4
16012.9 ± 3.018.4 ± 4.3
112045.6 ± 2.132.6 ± 1.5
51514.1 ± 5.0168 ± 1212.0 ± 0.42.6 ± 3.814.8 ± 21.7
53041.5 ± 9.8118.5 ± 28.0
56071.6 ± 50.6102.2 ± 72.3
5120251 ± 12179.3 ± 8.6
251510.6 ± 3.4149 ± 1311.5 ± 0.336.1 ± 8.8206.2 ± 50.3
253073.4 ± 2.4209.7 ± 6.9
2560335 ± 182478.6 ± 260
251201568 ± 1341120 ± 95.7
1001516.1 ± 3.9130 ± 188.1 ± 0.3603 ± 283445 ± 160
10030725 ± 322071 ± 91
100601100 ± 5731571 ± 818
1001205580 ± 903985 ± 64
Control1–10049.3–74.989–1121.4–2.4NANA
  • A-B, apical-to-basolateral; B-A, basolateral-to-apical; IA, intrinsic activity; NA, not applicable; V, rate of transport.