In vitro evaluation of endothelin receptor antagonists in human hepatocytes reveals significant differences in hepatic transporter inhibition, with macitentan showing the greatest effect on bile acid distribution and ambrisentan the lowest.
In vitro data suggest macitentan may carry higher hepatotoxicity risk than ambrisentan; hypothesis-generating for clinical ERA selection.
Significant differences in the inhibition of hepatic transporters were observed between the evaluated ERAs in vitro. Macitentan had the highest level of cellular accumulation and caused the greatest effects on bile acid distribution in human hepatocytes followed by sitaxsentan and bosentan. Ambrisentan showed a low potential to affect bile acids.
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Lepist et al. (2014) studied this question.
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