Evaluation of the Endothelin Receptor Antagonists Ambrisentan, Bosentan, Macitentan, and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes
Figure 2
d8-Taurocholate (d8-TCA) total (A) and cellular (B) accumulation in sandwich-cultured human hepatocytes exposed to ambrisentan, bosentan and macitentan.
Bosentan and macitentan treatment resulted in a dose-dependent reduction in total accumulation of d8-TCA. Ambrisentan, bosentan and macitentan treatment each resulted in a dose-dependent reduction in cellular accumulation of d8-TCA. Data presented as mean (±SD) expressed as percent of control treated; n = 3 donors; *P<0.05 bosentan vs. control; # P<0.05 macitentan vs. control.
