Inhibitors | E2G (1 μM) | Gimatecan (1 μM) | BNP1350 (0.2 μM) | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
BA | AB | Ratio BA/AB | BA | AB | Ratio BA/AB | BA | AB | Ratio BA/AB | |||||||
% | % | % | % | % | % | ||||||||||
15.1 ± 0.7 | 6.2 ± 0.7 | 2.4 | 28.2 ± 4.1 | 10.7 ± 0.8 | 2.6 | 28.5 ± 1.9 | 8.4 ± 3.6 | 3.4 | |||||||
Rifampicin (10 μM) | 5.7* ± 0.6 | 5.4 ± 0.6 | 1.1 | 17.4* ± 0.2 | 16.6 ± 1.1 | 1.1 | 12.4* ± 1.9 | 12.5 ± 1.0 | 1.0 | ||||||
Elacridar (5 μM) | 5.5* ± 1.0 | 5.2 ± 1.0 | 1.1 | 13.5* ± 1.3 | 12.1 ± 0.8 | 1.1 | 17.2* ± 1.4 | 16.1 ± 0.6 | 1.1 | ||||||
Zosuquidar (5 μM) | 9.1* ± 1.4 | 6.3 ± 1.1 | 1.4 | 18.2* ± 0.4 | 16.3 ± 0.04 | 1.1 | 14.4* ± 0.8 | 11.1 ± 0.7 | 1.3 | ||||||
Verapamil (10 μM) | 7.9* ± 0.1 | 4.3 ± 0.5 | 1.8 | 22.3* ± 3.6 | 14.2 ± 1.7 | 1.6 | 29.9 ± 1.9 | 9.3 ± 2.5 | 3.2 | ||||||
Valspodar (5 μM) | 8.5* ± 1.4 | 8.3 ± 0.4 | 1.0 | 15.0* ± 0.4 | 16.2 ± 2.1 | 0.9 | 11.7* ± 1.8 | 9.7 ± 2.3 | 1.2 | ||||||
Pantoprazole (500 μM) | 4.6* ± 0.5 | 4.1 ± 0.3 | 1.1 | 15.6* ± 1.3 | 17.0 ± 1.0 | 0.9 | 11.1* ± 1.7 | 12.4 ± 1.5 | 0.9 |
BA, transport from the basal to apical compartments; AB, transport from the apical to basal compartments; % total transport after 4 h. The respective modulators were present 2 h before the start and throughout the experiments.
↵* P < 0.05 compared with OATP1B1-mediated transport of E2G, gimatecan, and BNP1350 without inhibitor.