Imarikiren

Imarikiren (also known as TAK-272) is a potent, highly selective, orally bioavailable direct renin inhibitor primarily used for treating diabetic nephropathy. In hPRA assays, TAK-272 exhibits strong inhibitory activity against human renin (IC50 = 2.1 nM) and demonstrates excellent selectivity over other aspartic proteases such as pepsin (IC50 > 10 ?M) and cathepsin D (IC50 > 10 ?M) . In rats, TAK-272 shows significantly improved pharmacokinetic properties (F = 25.2%) and, upon oral administration (3 and 10 mg/kg), exhibits a dose-dependent, potent, and sustained antihypertensive effect. Currently, TAK-272 HCl is undergoing human clinical trials.