INS117548

INS117548 is a small molecule Rho kinase (ROCK) inhibitor developed for the treatment of glaucoma and ocular hypertension. Its mechanism of action involves inhibiting both ROCK1 and ROCK2, leading to disruption of the actin cytoskeleton in trabecular meshwork cells, which increases aqueous humor outflow and lowers intraocular pressure (IOP). Preclinical studies demonstrated potent inhibition with Ki values of 14.4 nM for ROCK1 and 5.8 nM for ROCK2, resulting in significant IOP reduction in animal models by 20–25%. The drug was evaluated in phase I clinical trials as an ophthalmic solution to assess safety, tolerability, and efficacy in patients with early-stage glaucoma or ocular hypertension[2][3][6].

Other names

INS-117548INS117548INS 117548