Synonyms: AR-11324 | AR11324 | ester 60 [PMID: 27072905] | Rhokiinsa® | Rhopressa®
netarsudil is an approved drug (FDA (2017), EMA (2019))
Compound class:
Synthetic organic
Comment: Netarsudil (AR-11324) is a combination Rho-associated protein kinase (Rho or ROCK) and norepinephrine transporter (NET) inhibitor [2,5]. Netarsudil is the S-enantiomeric, 2,4-dimethyl benzoate ester of compound 29 (Ki 0.2nM) described in [5]. Esterification improves bioavailability and corneal penetrating ability of the compound. It is an ocular hypotensive medication.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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No information available. |
Summary of Clinical Use |
An ophthalmic solution containing netarsudil was approved by the FDA in December 2017 for the treatment of glaucoma or ocular hypertension, following successful Phase 3 clinical trial [4]. Click here to link to the Phase 3 netarsudil (research code AR-13324) trials registered with ClinicalTrials.gov. A fixed-dose combination of netarsudil + latanoprost (Roclanda®) has EMA authorisation as a treatment for open-angle glaucoma and ocular hypertension (approved in January 2021). |
Mechanism Of Action and Pharmacodynamic Effects |
Inhibition of Rho kinase improves fluid outflow through the trabecular meshwork to lower intraocular pressure. The full action of netarsudil involves multiple mechanisms, including changes to outflow hydrodynamics and ocular morphology [3]. |