Bosentan
| File:Bosentan.svg | |
| Systematic (IUPAC) name | |
|---|---|
|
4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-(pyrimidin-2-yl)pyrimidin-4-yl]benzene-1-sulfonamide | |
| Clinical data | |
| Pregnancy category |
|
| Routes of administration | Oral |
| Legal status | |
| Legal status |
|
| Pharmacokinetic data | |
| Bioavailability | 50% |
| Protein binding | >98% |
| Metabolism | Hepatic |
| Biological half-life | 5 hours |
| Identifiers | |
| CAS Number | 147536-97-8 |
| ATC code | C02KX01 (WHO) |
| PubChem | CID 104865 |
| DrugBank | APRD00829 |
| ChemSpider | 94651 |
| Chemical data | |
| Formula | C27H29N5O6S |
| Molar mass | 551.614 g/mol[[Script error: No such module "String".]] |
| Script error: No such module "collapsible list". | |
| (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.
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 absolutely contraindicated in pregnancy because of its teratogenic potential.
See also
References
- Tracleer Prescribing Information [1] available in PDF format.
Cipla ltd also markets bosentan as bosenta & bozena in 62.5 mg and 125 mgde:Bosentan es:Bosentán it:Bosentan nl:Bosentan ja:ボセンタン
- Pages with script errors
- Pages with broken file links
- Drugs with non-standard legal status
- Infobox drug tracked parameters
- Articles without EBI source
- Articles without KEGG source
- Articles without InChI source
- Articles without UNII source
- 2Fix
- Endothelin receptor antagonists
- Orphan drugs
- Pyrimidines
- Sulfonamides
- Phenol ethers
- Alcohols
