Hydroxy bosentan is an active phase I metabolite of bosentan produced by the cytochrome P450 isoforms CYP3A4 and CYP2C9. Bosentan is an antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM). Up to 20% of the activity of bosentan may be due to the action of hydroxy bosentan because even though it has a lower affinity for endothelin receptors, its concentration is 3-fold higher in plasma.

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