Bosentan

Bosentan

drugbox
IUPAC_name = "N"- [6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy) -2-pyrimidin-2-yl-pyrimidin-4-yl] -4-tert- butyl-benzenesulfonamide



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 = 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]

ee also

*Sitaxsentan
*Ambrisentan


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Look at other dictionaries:

  • Bosentán — Saltar a navegación, búsqueda [[Imagen:|px|Bosentán chemical structure]] Bosentán Aviso médico Nombre (IUPAC) sistemático …   Wikipedia Español

  • bosentán — antagonista de los receptores de endotelina 1 utilizado en el tratamiento de la hipertensión pulmonar fórmula química [véase http://www.iqb.es/diccio/b/bi.htm#bosentan] Diccionario ilustrado de Términos Médicos.. Alvaro Galiano. 2010 …   Diccionario médico

  • Bosentan — Strukturformel Allgemeines Freiname Bosentan Andere Namen …   Deutsch Wikipedia

  • bosentan — noun A dual endothelin receptor antagonist important in the treatment of pulmonary artery hypertension …   Wiktionary

  • bosentan — n. see endothelin * * * bo·sen·tan (bo senґtən) an antagonist to endothelin 1 receptors, used in treatment of pulmonary arterial hypertension; administered orally …   Medical dictionary

  • bosentan — n.; see endothelin …   The new mediacal dictionary

  • Tracleer — Strukturformel Allgemeines Freiname Bosentan Andere Namen 4 tert Butyl …   Deutsch Wikipedia

  • CTEPH — Klassifikation nach ICD 10 I27 Sonstige pulmonale Herzkrankheiten I27.0 Primäre pulmonale Hypertonie …   Deutsch Wikipedia

  • Lungenhochdruck — Klassifikation nach ICD 10 I27 Sonstige pulmonale Herzkrankheiten I27.0 Primäre pulmonale Hypertonie …   Deutsch Wikipedia

  • Primäre pulmonale Hypertonie — Klassifikation nach ICD 10 I27 Sonstige pulmonale Herzkrankheiten I27.0 Primäre pulmonale Hypertonie …   Deutsch Wikipedia

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