Evaluation of the Endothelin Receptor Antagonists Ambrisentan, Bosentan, Macitentan, and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes
Figure 4
Dose-dependent intracellular accumulation of test ERAs in sandwich-cultured human hepatocytes.
Ambrisentan displayed the lowest intracellular accumulation followed by bosentan, sitaxsentan, and macitentan. Data are presented as mean (±SD) micromolar (µM) concentration; n = 3 donors; *P<0.05 vs. corresponding intracellular accumulation value for ambrisentan at the same test concentration.