Ripasudil hydrochloride dihydrate

Ripasudil (K-115) is a potent inhibitor of Rho kinase (ROCK), with IC₅₀ values of 19 and 51 nM for ROCK-2 and ROCK-1, respectively. Ripasudil (10 μM) induces cytoskeletal changes, including retraction, cell rounding and reduced actin bundles of cultured trabecular meshwork (TM) cells. It significantly reduces transendothelial electrical resistance (TEER) and increases FITC-dextran permeability in Schlemm’s canal endothelial (SCE) cell monolayers at a concentration of 5 μM. A 0.4% ophthalmic solution significantly lowers intraocular pressure (IOP) in rabbits and monkeys. It was the first ophthalmic solution developed for the treatment of glaucoma and ocular hypertension in Japan.