TABLE 3

Inhibition of bosentan and Ro 48-5033 uptake into OATP1B1- and OATP1B3-expressing CHO cells by rifampicin, cyclosporin A, and sildenafil


Substrate

Inhibitor

IC50
OATP1B1
OATP1B3
μM
Bosentan Rifampicin 3.2 ± 1.6 1.6 ± 0.8
Cyclosporin A 0.3 ± 0.1 0.8 ± 0.2
Sildenafil 1.5 ± 0.5 0.8 ± 0.3
Ro 48-5033 Rifampicin ∼50 0.8 ± 0.4
Cyclosporin A >100 0.5 ± 0.1

Sildenafil
>100
4.0 ± 1.3