firibastat

Firibastat is a first-in-class, orally active prodrug developed for the treatment of hypertension. It acts centrally by inhibiting aminopeptidase A (APA), a membrane-bound zinc metalloprotease in the brain that converts angiotensin II to angiotensin III. Angiotensin III increases blood pressure through several central mechanisms, including stimulation of vasopressin release and increased sympathetic tone. Firibastat crosses the blood-brain barrier and is cleaved into two active EC33 molecules, which inhibit APA activity, thereby reducing angiotensin III formation and lowering blood pressure. Unlike traditional antihypertensive drugs that act peripherally, firibastat targets the brain renin–angiotensin system[1][2][4][6]. Clinical trials have shown efficacy in some hypertensive populations but not in resistant hypertension[5][7].

Other names

EC33 (active metabolite)