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]]
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