Drug intelligence / Profile preview

netarsudil-M1

Development stage
Phase 1
Lead developer
Alcon
Modality
Small Molecules
Administration
Ophthalmic
01

Overview

Netarsudil-M1 is the **active metabolite of netarsudil**, a potent inhibitor of **Rho-associated protein kinase (ROCK)**, specifically ROCK1 and ROCK2. It demonstrates approximately fivefold greater potency than netarsudil in inhibiting ROCK1 and ROCK2 kinases, resulting in significant relaxation of the trabecular meshwork (TM) and disruption of actin stress fibers and focal adhesions in TM cells. This mechanism leads to increased outflow of aqueous humor via the conventional pathway, thereby lowering intraocular pressure (IOP). Experimental studies in enucleated human eyes show that netarsudil-M1 increases aqueous outflow facility primarily by expanding the juxtacanalicular connective tissue and dilating episcleral veins. Netarsudil-M1 is under investigation primarily for its role in the treatment of **open-angle glaucoma** and **ocular hypertension** and is not approved as a standalone pharmaceutical agent[3][4].

Brand names
AR-13503 SR ImplantAR13503 SR ImplantAR 13503 SR ImplantAR-13503 SRAR13503 SRAR 13503 SR
Other names
netarsudil M1AR-13503AR13503AR 13503
02

Targets

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

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