TABLE 3

Inhibition of digoxin and apixaban efflux in Caco-2 cells

Test ConditionsPcA-B, appPcB-A, app% Inhibition
of Efflux ± S.D.Efflux Ratio
nm/snm/s
Digoxin (5 μM)a23 ± 3205 ± 7NA8.9
Digoxin (5 μM) + Cyclosporin A (50 μM)86 ± 1589 ± 1798 ± 11.0
Digoxin (5 μM) + Ketoconazole (50 μM)96 ± 395 ± 6100 ± 01.0
Apixaban (3 μM)16 ± 1387 ± 54NA24.2
Apixaban (3 μM) + Cyclosporin A (50 μM)67 ± 9278 ± 2543 ± 54.1
Apixaban (3 μM) + Ketoconazole (50 μM)70 ± 8177 ± 2171 ± 52.5
Apixaban (3 μM) + Naproxen (0.2 mM)12 ± 1307 ± 1321 ± 325.6
Apixaban (3 μM) + Naproxen (1 mM)16 ± 3279 ± 2929 ± 717.4
Apixaban (3 μM) + Naproxen (6 mM)35 ± 4251 ± 2542 ± 67.2
Apixaban (30 μM)10 ± 2292 ± 13NA29.2
Apixaban (30 μM) + Cyclosporin A (50 μM)39 ± 4182 ± 1850 ± 64.7
Apixaban (30 μM) + Ketoconazole (50 μM)69 ± 9147 ± 2179 ± 142.2
Apixaban (20 μM)b6 ± 0140 ± 10NA23.3
Apixaban (20 μM) + Probenecid (200 μM)b7 ± 0.2123 ± 614 ± 517.6
Apixaban (20 μM) + Probenecid (1 mM)b9 ± 0.5137 ± 65 ± 215.2
  • NA, not applicable.

  • a As a positive substrate.

  • b These experiments were done at a different time from other experiments in the table.