|Systematic (IUPAC) name|
|Biological half-life||5 hours|
|ATC code||C02KX01 (WHO)|
|Molar mass||551.614 g/mol[[Script error: No such module "String".]]|
|Script error: No such module "collapsible list".|
Bosentan (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. Under normal conditions, endothelin-1 binding of ET-A or ET-B receptors causes pulmonary vasoconstriction. By blocking this interaction, bosentan decreases pulmonary vascular resistance. 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.
In the United States, Tracleer is indicated for the treatment of pulmonary arterial hypertension (WHO Group I) in patients with WHO Class II-IV symptoms, to improve exercise capacity and decrease the rate of clinical worsening.
Bosentan is absolutely contraindicated in pregnancy because of its teratogenic potential.
- Tracleer Prescribing Information  available in PDF format.