macitentan

Macitentan is a small molecule dual endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH). It works by blocking the action of endothelin, a potent vasoconstrictor, at both the endothelin A (ETA) and endothelin B (ETB) receptors, with approximately 50-fold selectivity for ETA over ETB. By inhibiting these receptors, macitentan reduces vasoconstriction and cell proliferation in the pulmonary arteries, leading to improved blood flow and reduced workload on the heart. Macitentan is administered orally as a once-daily tablet and was first approved by the FDA in 2013. Its active metabolite aprocitentan also contributes to its pharmacological effects[1][3][5][9].

Brand names

Opsumit

Other names

macitentánmacitentanum