ANG 4201 - ROCK2 Inhibitor

The Rho kinase family members, consisting of Rho-associated kinase1 (ROCK1) and ROCK2, are serine–threonine kinases that are activated by Rho GTPases. We have recently found that renal ROCK2 and not ROCK1 is significantly upregulated in UUO, a mouse model of chronic kidney disease. This upregulation of ROCK2 is associated with increase in renal collagen, hydroxyproline and alpha-SMA, which are the markers of renal fibrosis. We are employing state of the art core-hopping method and structure-based drug design to develop orally bioavailable and highly selective ROCK2 inhibitor for the treatment of renal fibrosis. We have identified ANG4201 as our lead candidate which is a selective for ROCK2 and shown promising antifibrotic effects in preclinical animal models of kidney disease. We believe that ROCK2 inhibitor will not only prove efficacious in mitigating fibrosis but will also carry a lower risk of any side effects associated with chronic dosing.