CYP2C9, SLCO1B1, SLCO1B3, and ABCB11 polymorphisms in patients with bosentan-induced liver toxicity

Clin Pharmacol Ther. 2014 Jun;95(6):583-5. doi: 10.1038/clpt.2014.42.


Bosentan is an endothelin receptor antagonist used as a first-line treatment in pulmonary arterial hypertension (PAH). Its main adverse effect is a dose-dependent liver toxicity. CYP2C9*2 has recently been shown to be associated with hepatotoxicity in PAH patients. We conducted a nested case-control study to further explore the relationship between functional polymorphisms of gene products involved in bosentan pharmacokinetics (OATP1B1, OATP1B3, and CYP2C9) or hepatobiliary transporters affected by bosentan (ABCB11) and bosentan-induced liver toxicity.

Publication types

  • Research Support, Non-U.S. Gov't
  • Comment

MeSH terms

  • Aryl Hydrocarbon Hydroxylases / genetics*
  • Chemical and Drug Induced Liver Injury / etiology*
  • Endothelin Receptor Antagonists*
  • Female
  • Humans
  • Hypertension, Pulmonary / drug therapy*
  • Male
  • Sulfonamides / adverse effects*


  • Endothelin Receptor Antagonists
  • Sulfonamides
  • Aryl Hydrocarbon Hydroxylases