- 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 = OralBosentan (BOZENTAN) is a dual
endothelin receptor antagonist important in the treatment ofpulmonary artery hypertension (PAH). It is licensed in theUnited States , theEuropean Union and other countries byActelion 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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