Bosentan 2903548 225352695 2008-07-13T06:34:29Z 77.4.37.182 /* Mechanism of Action */ {{drugbox | IUPAC_name = ''N''-[6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy) -2-pyrimidin-2-yl-pyrimidin-4-yl] -4-tert- butyl-benzenesulfonamide | image = Bosentan.svg | CAS_number = 147536-97-8 | ATC_prefix = C02 | ATC_suffix = KX01 | ATC_supplemental = | PubChem = 104865 | DrugBank = APRD00829 | smiles = COc1ccccc1Oc2c(NS(=O)(=O)c3ccc(cc3)C(C)(C)C)nc(nc2OCCO)c4ncccn4 | C = 27 | H = 29 | N = 5 | O = 6 | S = 1 | molecular_weight = 551.615 g/mol | bioavailability = 50% | protein_bound = >98% | metabolism = [[Liver|Hepatic]] | elimination_half-life = 5 hours | pregnancy_category = X | legal_status = Rx-only | routes_of_administration = Oral }} '''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. 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. ==Clinical uses== 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. ==External links== * [http://www.tracleer.com/ Tracleer official website] * [http://www.tracleer.com/pdf/PI_4pg_TR2454_032707_FINAL.pdf Tracleer prescribing information] ==See also== *[[Sitaxsentan]] *[[Ambrisentan]] {{PAH rx}} {{Antihypertensives and diuretics}} [[Category:Endothelin receptor antagonists]] [[Category:Orphan drugs]] [[de:Bosentan]] [[es:Bosentan]] [[it:Bosentan]]