TABLE 2

Inhibition of individually expressed cOATPs and hOATPs in HEK-293 cells

IC50 (µM)a
CompoundcOATP1B1bhOATP1B1bcOATP1B3chOATP1B3ccOATP2B1dhOATP2B1d
RIF0.20 ± 0.080.55 ± 0.071.4 ± 0.50.46 ± 0.1369.1 ± 7.540.1 ± 5.1
CsA1.0 ± 0.30.87 ± 0.290.50 ± 0.110.80 ± 0.22>50>50
Ritonavir0.49 ± 0.141.3 ± 0.31.3 ± 0.64.0 ± 1.14.5 ± 1.810.7 ± 2.3
Gemfibrozil20.2 ± 5.841.4 ± 9.022.4 ± 6.650.1 ± 27.3>100>100
Verapamil13.5 ± 2.814.8 ± 3.152.7 ± 15.987.3 ± 35.8>200>200
Saquinavir2.9 ± 0.91.6 ± 0.43.6 ± 1.55.5 ± 3.012.3 ± 4.89.4 ± 3.2
  • CsA, cyclosporine A; RIF, rifampin.

  • a Values represent the mean ± S.D. (n = 3 to 4 determinations).

  • b IC50 determined at a final E17βG concentration of 1 µM.

  • c IC50 determined at a final CCK-8 concentration of 0.1 µM.

  • d IC50 determined at a final E3S concentration of 1 µM.