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Evaluation of the Endothelin Receptor Antagonists Ambrisentan, Bosentan, Macitentan, and Sitaxsentan as Hepatobiliary Transporter Inhibitors and Substrates in Sandwich-Cultured Human Hepatocytes

Figure 3

d₈-Taurocholate (d₈-TCA) biliary efflux (A) and clearance (B) in sandwich-cultured human hepatocytes exposed to ambrisentan, bosentan, and macitentan.

The biliary excretion index (BEI) of d₈-TCA was largely unaffected by the test ERAs. Bosentan and macitentan treatment resulted in dose-dependent reductions in biliary clearance (Cl_b) 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.

doi: https://doi.org/10.1371/journal.pone.0087548.g003