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Bosentan
Systematic (IUPAC) name
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide
Identifiers
CAS number 147536-97-8
ATC code C02KX01
PubChem 104865
DrugBank APRD00829
ChemSpider 94651
Chemical data
Formula C27H29N5O6S 
Mol. mass 551.614 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability 50%
Protein binding >98%
Metabolism Hepatic
Half life 5 hours
Therapeutic considerations
Pregnancy cat. X
Legal status Prescription only
Routes Oral
 Yes check.svgY(what is this?)  (verify)

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.

Contents

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.

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.

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.[1]

External links

Bosentan is obsolutely contraindicated in pregnancy because of its tetrogenic potential.

See also

References

  1. ^ http://www.tracleer.com/pdf/09%20276%2001%2000%200809_Tra%20PI_4%20Pg_081409pdf.pdf
  • Tracleer Prescribing Information [1] available in PDF format.

Cipla ltd also markets bosentan as bosenta & bozena in 62.5 mg and 125 mg








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