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Bosentan, sold under the brand name Tracleer among others, is a dual endothelin receptor antagonist medication used in the treatment of pulmonary artery hypertension (PAH).
Read the full article on WikipediaPulmonary arterial hypertension (PAH) Clinical criteria: Treatment Phase: Continuing treatment of combination therapy (dual or triple therapy, excluding selexipag) The treatment must form part of dual combination therapy consisting of: (i) one endothelin receptor antagonist, (ii) one phosphodiesterase-5 inhibitor; OR The treatment must form part of dual combination therapy consisting of: (i) one endothelin receptor antagonist, (ii) one prostanoid; OR The treatment must form part of triple combination therapy consisting of: (i) one endothelin receptor antagonist, (ii) one phosphodiesterase-5 inhibitor, (iii) one prostanoid. Treatment criteria: Must be treated by a physician with expertise in the management of PAH, with this authority application to be completed by the physician with expertise in PAH, AND Patient must be undergoing continuing treatment of existing PBS-subsidised combination therapy (dual/triple therapy, excluding selexipag), where this drug in the combination remains unchanged from the previous authority application.
“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 receptors causes constriction of the pulmonary blood vessels. Conversely, binding of endothelin-1 to ET-B receptors has been associated with both vasodilation and vasoconstriction of vascular smooth muscle, depending on the ET-B subtype (ET-B1 or ET-B2) and tissue. Bosentan blocks both ET-A and ET-B receptors, but is thought to exert a greater effect on ET-A receptors, causing a total decrease in pulmonary vascular resistance.”
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