Drug intelligence / Profile preview

LX7101

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

Overview

LX7101 is a small molecule inhibitor developed for the treatment of ocular hypertension and primary open-angle glaucoma. It acts as a dual inhibitor of LIM domain kinase 2 (LIMK2) and, to a lesser extent, LIMK1 and Rho-associated protein kinase 2 (ROCK2). By inhibiting these kinases, which are involved in cytoskeletal dynamics and regulation of intraocular pressure, LX7101 lowers intraocular pressure—a key therapeutic goal in glaucoma management. The drug was designed for topical ocular administration with improved aqueous stability compared to earlier LIMK inhibitors. Developed by Lexicon Pharmaceuticals, it advanced through preclinical studies into Phase I clinical trials where it demonstrated efficacy in reducing intraocular pressure in patients with glaucoma or ocular hypertension[1][3][6].

Other names
[3-[[4-(aminomethyl)-1-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carbonyl]amino]phenyl] N,N-dimethylcarbamate
02

Targets

LIMK1 (LIM domain kinase 1)LIMK2 (LIM domain kinase 2)ROCK2 (Rho-associated coiled-coil containing protein kinase 2)

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