Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor ( K i =200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats.
In Vivo
When given orally, Firibastat (0.1-30 mg/kg; p.o.) crosses the gastrointestinal and blood-brain barriers, enters the brain, and generates two active molecules of EC33 which inhibit brain APA activity, blocking brain angiotensin III formation, and decrease blood pressure for several hours in hypertensive rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Normotensive and hypertensive DOCA-salt rats Dosage: 0.1-30 mg/kg Administration: P.o. Result: Resulting in a dose-dependent decrease in mean arterial blood pressure (MABP).
