(BOZENTAN) is a dual endothelin receptor antagonist
important in the treatment of pulmonary artery hypertension
(PAH). It 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
Mechanism of Action
Bosentan is a competitive antagonist of endothelin
-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. When endothelin-1 binds to these receptors, pulmonary artery pressure is elevated. By blocking this interaction, bosentan is able to lower pulmonary artery pressure. Bosentan has a slightly higher affinity for ET-A than ET-B.
Bosentan is indicated mainly for the treatment of pulmonary hypertension. In 2007, Tracleer® (bosentan) was approved in the European Union also for reducing the number of new digital ulcers in patients with systemic sclerosis and ongoing digital ulcer disease.