Endothelin receptor antagonist.

  Bosentan is a dual endothelin receptor antagonist. It is used in the treatment of pulmonary artery hypertension (PAH). Endothelin receptor antagonists (ERAs) act on the endothelin pathway by blocking binding of endothelin-1 to its receptors [endothelin type-A (ETA) and/or type-B (ETB)] on the surface of endothelial and smooth muscle cells. Bosentan is licensed in the United States, the European Union and other countries by Actelion Pharmaceuticals for the management of PAH under the trade name Tracleer. Bosentan, is a non-peptide and orally active. Bosentan is highly protein-bound, with approximately 98% bound to albumin. This paper reviews the pharmacological and pharmaceutical properties of Bosentan. Bosentan could be an attractive target for the generic industries.