Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptor.

@article{Giersbergen2002BosentanAD,
  title={Bosentan, a dual endothelin receptor antagonist, activates the pregnane X nuclear receptor.},
  author={Paul L. M. van Giersbergen and Carmela Gnerre and Alexander Treiber and Jasper Dingemanse and Urs A. Meyer},
  journal={European journal of pharmacology},
  year={2002},
  volume={450 2},
  pages={115-21}
}
Recent clinical studies have shown that bosentan, a dual endothelin receptor antagonist, decreases the exposure to various substrates of cytochrome P450 (CYP) isoenzymes 2C9 and 3A4. The aim of the study was to investigate the effect of bosentan, its metabolites and glibenclamide on the activity of the pregnane X receptor, a nuclear receptor that regulates… CONTINUE READING