Drug intelligence / Profile preview

rki983a

Development stage
Phase 2
Lead developer
Novartis
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

RKI983A is a small molecule Rho kinase (ROCK) inhibitor developed for ophthalmic use, specifically as an eye drop formulation to lower intraocular pressure in patients with primary open-angle glaucoma (POAG) or ocular hypertension. Its mechanism of action involves inhibition of the Rho-associated coiled-coil containing protein kinases ROCK1 and ROCK2, which play key roles in regulating cytoskeletal dynamics and smooth muscle contraction within the trabecular meshwork, thereby facilitating increased aqueous humor outflow and reducing intraocular pressure. Clinical trials demonstrated that while RKI983A produced a dose-dependent reduction in intraocular pressure, its efficacy was less than that of latanoprost. Adverse effects were primarily ocular, including conjunctival hyperemia. No further development has been reported since 2009[3][5][7].

Other names
RKI983RKI-983RKI 983
02

Targets

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

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