title: Bosentan: a dual endothelin receptor antagonist.
abstract: The peptide endothelin plays a significant role in a wide array of pathological conditions, including primary pulmonary hypertension and pulmonary arterial hypertension associated with collagen vascular disease. These are life-threatening conditions that can severely compromise the function of the lungs and heart. Inhibiting the actions of endothelin by blockade of its receptors provides a new and effective approach to therapy for patients with these conditions. Bosentan (Tracleer ) is the first orally-active dual endothelin receptor antagonist and has recently been approved in the US, Canada, Switzerland and the EU for the treatment of pulmonary arterial hypertension. Bosentan significantly improves exercise capacity, symptoms and functional status in patients with this disease and also slows clinical deterioration, which may be indicative of a delay of disease progression. Results from large-scale studies of bosentan in patients with pulmonary arterial hypertension and chronic heart failure have established its long-term safety and tolerability profiles. The introduction of the dual endothelin receptor antagonist bosentan has provided an essential treatment for pulmonary arterial hypertension and ongoing trials are evaluating its potential role in the management of other endothelin-mediated disease states.
authors.affiliation: Division of Pulmonary & Critical Care Medicine, Department of Medicine, University of California at San Diego, School of Medicine, 9300 Campus Point Drive, 7372, La Jolla, CA 92037, USA. ljrubin@ucsd.edu
authors.forename: Lewis J
authors.initials: LJ
authors.lastname: Rubin
authors.forename: Sébastien
authors.initials: S
authors.lastname: Roux
mesh_terms: D000818:Animals; D000959:Antihypertensive Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D000077300:Bosentan; D002986:Clinical Trials as Topic; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000037:antagonists & inhibitors / Q000096:biosynthesis; D006333:Heart Failure / Q000188:drug therapy; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy; D023421:Models, Animal; D013449:Sulfonamides / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000959:Antihypertensive Agents; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D013449:Sulfonamides; D000077300:Bosentan