aprocitentan

Aprocitentan is an orally active, dual endothelin receptor antagonist used in combination with other antihypertensive agents to treat resistant hypertension in adults whose blood pressure is not adequately controlled on other medications. It works by inhibiting the binding of endothelin-1 (ET-1), a potent vasoconstrictor, to both endothelin A (ETA) and endothelin B (ETB) receptors. This blockade mitigates the hypertensive effects of ET-1 overexpression, including endothelial dysfunction, vascular hypertrophy and remodeling, sympathetic activation, and increased aldosterone synthesis. Aprocitentan is the active metabolite of macitentan and represents a novel therapeutic option for patients with treatment-resistant hypertension[1][2][5][6].

Brand names

TryvioJeraygo

Other names

aprocitentanACT-132577ACT132577ACT 132577