Review on: Aprocitentan Unveiled: A New Horizon in Anti-Hypertensive Therapy

Aprocitentan is an oral once-daily dual endothelin-1 receptor antagonist preventing ET-1 binding quite effectively to ETA and ETB receptors.It is a derivative of macitentan somewhat oddly used in treating pulmonary arterial hypertension with orphan drug status. Aprocitentan gets eliminated slowly in urine and faeces after being highly bound to proteins. Aprocitentan is tolerable at doses up to 600 milligrams and possesses a half-life (t1/2) of 44 hours with daily dosing. Dosages as low as 25 mg show significant ET receptor antagonism, with minimal differences in plasma exposure between genders and age groups. Preclinical and clinical research suggests that Aprocitentan effectively reduces blood pressure (BP), with noticeable decreases within 14 days of use. It also enhances the effects of other anti-hypertensive medications, such as renin-angiotensin system blockers. In individuals with resistant hypertension, Aprocitentan may improve cardiovascular outcomes by further lowering BP and providing broader cardiovascular protection. The findings support its potential as a new treatment option for resistant hypertension.