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The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions

Clinical Pharmacology & Therapeutics · 2001 · Vol. 69(4) · pp. 223–231

Karin Fattinger✉(University of Bern)

Abstract

These results indicate that bosentan-induced liver injury is mediated, at least in part, by inhibition of Bsep/BSEP-causing intracellular accumulation of cytotoxic bile salts and bile salt induced liver cell damage. The data further emphasize the pathophysiologic importance of drug-Bsep interactions in acquired forms of cholestatic liver injury.

Drug Transport and Resistance Mechanisms Liver Disease and Transplantation Pharmacological Effects and Toxicity StudiesBosentanBile Salt Export PumpPharmacologyLiver injuryInternal medicineCholestasisEndothelin receptor antagonistEndothelin receptorMedicineEndocrinology

MeSH terms

ATP Binding Cassette Transporter, Subfamily B, Member 11BosentanAnimalsAntihypertensive AgentsBile Acids and SaltsBile CanaliculiCholestasis, IntrahepaticClinical Trials as TopicDose-Response Relationship, DrugDrug CombinationsGlyburideHumansHypertensionLiverMale

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503

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6.72

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