bosentan

Bosentan is a dual endothelin receptor antagonist used primarily for the treatment of pulmonary arterial hypertension (PAH) in adults and children aged 3 years and older. It works by competitively inhibiting both endothelin A (ETA) and endothelin B (ETB) receptors, with a slightly higher affinity for ETA. By blocking these receptors, bosentan prevents the action of endothelin-1—a potent endogenous vasoconstrictor—leading to vasodilation and reduced pulmonary vascular resistance. Bosentan improves exercise capacity, delays clinical worsening in PAH patients, and is also effective in persistent pulmonary hypertension of the newborn (PPHN). The drug is administered orally as tablets or dispersible tablets. Common adverse effects include elevated liver enzymes, anemia, edema, headache, dizziness, flushing, hypotension, rhinitis; regular monitoring of liver function is required due to risk of hepatotoxicity. Bosentan was developed by Actelion Pharmaceuticals.

Brand names

Tracleer

Other names

波生坦bosentan hydratebosentan anhydrous