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Bosentan
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| Systematic (IUPAC) name | |
| N-[6-(2-hydroxyethoxy)-5- (2-methoxyphenoxy) -2-pyrimidin-2-yl-pyrimidin-4-yl] -4-tert- butyl-benzenesulfonamide | |
| Identifiers | |
| CAS number | |
| ATC code | C02 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C27H29N5O6S |
| Mol. mass | 551.615 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | 50% |
| Protein binding | >98% |
| Metabolism | Hepatic |
| Half life | 5 hours |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. |
X |
| Legal status |
℞ Prescription only |
| Routes | 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.
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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 in able to lower pulmonary artery pressure. Bosentan has a slightly higher affinity for ET-A than ET-B.
Clinical uses
Bosentan is indicated for the treatment of pulmonary hypertension.
External links
See also
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Wikipedia content modification information:
- This page was last modified on 7 May 2008, at 01:37.
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