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. 2016 May 15;26(10):2475-2480.
doi: 10.1016/j.bmcl.2016.03.104. Epub 2016 Apr 1.

Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma

Jill M Sturdivant  1 , Susan M Royalty  2 , Cheng-Wen Lin  2 , Lori A Moore  2 , Jeffrey D Yingling  2 , Carmen L Laethem  2 , Bryan Sherman  2 , Geoffrey R Heintzelman  2 , Casey C Kopczynski  2 , Mitchell A deLong  2
Affiliations

Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma

Jill M Sturdivant et al. Bioorg Med Chem Lett. .

Abstract

Inhibition of Rho kinase (ROCK) to improve fluid outflow through the trabecular meshwork and lower intraocular pressure is a strategy for the development of new anti-glaucoma agents. Alpha-aryl-beta-amino isoquinoline analogs were identified as potent ROCK inhibitors. Compounds that provided a longer duration of intraocular pressure reduction in Dutch Belted rabbits also inhibited norepinephrine transporter. Ester 60 improved bioavailability of its parent ROCK inhibitor, 29 (Ki=0.2nM) and demonstrated an effective and sustained IOP reduction for 24h after dosing. From these studies, netarsudil (a.k.a. AR-13324) was discovered and is currently in clinical trials for the treatment of glaucoma and ocular hypertension.

Keywords: AR-13324; Glaucoma; Intraocular pressure (IOP); Rho kinase (ROCK); Trabecular meshwork.

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