Drug intelligence / Profile preview

ripasudil

Development stage
Phase 4
Lead developer
Kowa
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Ripasudil is a small molecule drug that acts as a highly selective and potent inhibitor of Rho-associated coiled-coil containing protein kinase (ROCK), specifically targeting both ROCK-1 and ROCK-2 isoforms. It is primarily indicated for the treatment of ocular hypertension and open-angle glaucoma. Ripasudil lowers intraocular pressure (IOP) by directly acting on the trabecular meshwork and Schlemm’s canal in the eye, increasing conventional aqueous outflow. This mechanism involves cytoskeletal changes in trabecular meshwork cells, leading to reduced resistance to fluid flow. The drug was originally developed from fasudil derivatives, with modifications enhancing its potency and selectivity for ROCK inhibition. Ripasudil was first approved in Japan in 2014 under the brand name Glanatec as a 0.4% ophthalmic solution[1][3][7].

Brand names
Glanatec
Other names
ripasudil hydrochloride hydrate
02

Targets

ROCK2 (Rho-associated coiled-coil containing protein kinase 2)ROCK1 (Rho-associated coiled-coil containing protein kinase 1)

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