SAR407899

SAR407899 is a highly selective, potent, and ATP‐competitive small molecule inhibitor of Rho-associated protein kinase (ROCK), particularly ROCK2. It demonstrates strong inhibitory activity with Ki values of 36 nM for human ROCK2 and 41 nM for rat ROCK2. The drug was developed by Sanofi (formerly sanofi-aventis) as a novel antihypertensive agent, showing superior blood pressure-lowering effects compared to other ROCK inhibitors such as fasudil and Y‐27632 in preclinical models. In addition to its antihypertensive action, SAR407899 has been investigated for potential benefits in reducing end-organ damage associated with chronic hypertension, improving heart, kidney, and endothelial function in animal studies. Clinical development reached up to phase II trials across several indications including microvascular angina (Syndrome X), diabetic nephropathies, diabetic neuropathies, erectile dysfunction, pulmonary hypertension, hypertension, and kidney disorders; however, development was discontinued for all these indications[2][3][4][5][7][8].

Other names

6-piperidin-4-yloxy-2H-isoquinolin-1-one