> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/netarsudil-cdf69483-92c3-4ac8-b941-7366b7bf529a > Record changed: 2026-10-13 # Netarsudil Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) First approval year 2017 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) ## Development status **First approval year** 2017 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **Drug name** Netarsudil Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **Molecular weight** 453.54 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **Structure (SMILES)** Cc1ccc(C(=O)OCc2ccc(\[C@@H\](CN)C(=O)Nc3ccc4cnccc4c3)cc2)c(C)c1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) ### Other names (16) - ar 11324 free base - ar 13324 - AR-11324 FREE BASE - AR-13324 - benzoic acid 2 4 dimethyl 4 1s 1 aminomethyl 2 6 isoquinolinylamino 2 oxoethyl phenyl methyl ester - BENZOIC ACID, 2,4-DIMETHYL-, (4-((1S)-1-(AMINOMETHYL)-2-(6-ISOQUINOLINYLAMINO)-2-OXOETHYL)PHENYL)METHYL ESTER - netarsudil - Netarsudil - netarsudil \[INN\] - NETARSUDIL \[MI\] - NETARSUDIL \[USAN\] - Netarsudil \[WHO-DD\] - netarsudil inn - netarsudil mi - netarsudil usan - netarsudil who dd ## Identifiers **ATC classification codes** - S01EX05 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **CAS registry numbers** - 1254032-66-0 **ChEMBL ID** CHEMBL4594250 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **InChIKey** OURRXQUGYQRVML-AREMUKBSSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL4594250) **PubChem compound IDs** - 66599893 **FDA ingredient codes (UNII)** - W6I5QDT7QI ### RxNorm IDs (RxCUI) (2) - 1992863 - 1992864 ## Regulatory information ### United States **Applicant** ALCON LABS INC **Approval date** 18 Dec 2017 **Application number** NDA208254 ### European Union **Status** Authorised **Status date** 19 Nov 2019 **Authorisation date** 19 Nov 2019 **Approved indications** Reduction of elevated intraocular pressure (IOP) in adult patients with primary open-angle glaucoma or ocular hypertension. **Product number** EMEA/H/C/004583 **Authorisation holder** Santen Oy **Priority medicines scheme** No **Generic** No **Biosimilar** No **Generic medicines** 0 **Biosimilar medicines** 0 **Advanced therapy** No **Conditional approval** No **Additional monitoring** Yes **Accelerated assessment** No **Exceptional circumstances** No #### Therapeutic areas - Glaucoma, Open-Angle - Ocular Hypertension European medicines record Source: [www.ema.europa.eu](https://www.ema.europa.eu/en/medicines/human/EPAR/rhokiinsa) ### Other regulatory facts **First in class** Yes **Orphan designation** No **Availability** Prescription only ## Pharmacology ### Drug classification **Pharmacology name** netarsudil **Type** Synthetic organic **Drug name stem** \-dil **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - topical ### Mechanisms of action (3) - **Action** Inhibition **Action type** Inhibitor **Target** Rho associated coiled-coil containing protein kinase 2 **Gene symbol** ROCK2 **Protein identifier** O75116 **Median affinity** 7.95 **Affinity units** pIC50 - **Action** Inhibition **Action type** Inhibitor **Target** Rho associated coiled-coil containing protein kinase 2 **Gene symbol** ROCK2 **Protein identifier** O75116 **Median affinity** 8.7 **Affinity units** pKi - **Action** Inhibition **Action type** Inhibitor **Target** Rho associated coiled-coil containing protein kinase 1 **Gene symbol** ROCK1 **Protein identifier** Q13464 **Median affinity** 7.49 **Affinity units** pIC50 ### Open Targets mechanisms - **Mechanism** Rho-associated protein kinase inhibitor **Action type** Inhibitor **Target** Rho-associated protein kinase ### DrugCentral mechanisms (2) - **Action type** Inhibitor **Gene symbol** ROCK2 **Protein identifier** O75116 **Organism** Homo sapiens **Target development level** Clinical - **Action type** Inhibitor **Gene symbol** ROCK1 **Protein identifier** Q13464 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (5) - **Condition** Glaucoma, Open-Angle **Highest recorded phase** 0.5 **Condition identifier** EFO:0004190 **Subject identifier** D005902 - **Condition** Corneal Edema **Highest recorded phase** 2 **Condition identifier** EFO:1000879 **Subject identifier** D015715 - **Condition** Glaucoma **Highest recorded phase** 3 **Condition identifier** MONDO:0005041 **Subject identifier** D005901 - **Condition** Fuchs' Endothelial Dystrophy **Highest recorded phase** 3 **Condition identifier** MONDO:0005321 **Subject identifier** D005642 - **Condition** Fuchs' Endothelial Dystrophy **Highest recorded phase** 3 **Condition identifier** Orphanet:98974 **Subject identifier** D005642 ### Open Targets indications (12) - **Condition identifier** EFO\_0004190 - **Condition identifier** EFO\_1000879 **Highest recorded phase** 2 - **Condition identifier** EFO\_1001069 - **Condition identifier** MONDO\_0005041 - **Condition identifier** MONDO\_0005041 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0005321 - **Condition identifier** MONDO\_0005321 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0005338 **Highest recorded phase** 4 - **Condition identifier** MONDO\_0006712 **Highest recorded phase** 2 - **Condition identifier** MONDO\_0006875 **Highest recorded phase** 4 - **Condition identifier** Orphanet\_98974 **Highest recorded phase** 2 - **Condition identifier** Orphanet\_98974 **Highest recorded phase** 3 ### Reported adverse events (16) - **Event** blepharitis allergic **Reports** 5 **Reporting signal score** 42.7688 - **Event** conjunctival haemorrhage **Reports** 5 **Reporting signal score** 17.3209 - **Event** conjunctival hyperaemia **Reports** 33 **Reporting signal score** 186.493 - **Event** conjunctivitis allergic **Reports** 7 **Reporting signal score** 36.7412 - **Event** cornea verticillata **Reports** 8 **Reporting signal score** 58.0538 - **Event** corneal oedema **Reports** 20 **Reporting signal score** 107.09 - **Event** eye irritation **Reports** 8 **Reporting signal score** 20.312 - **Event** eye pruritus **Reports** 7 **Reporting signal score** 19.1899 - **Event** eyelid margin crusting **Reports** 3 **Reporting signal score** 13.4643 - **Event** foreign body sensation in eyes **Reports** 5 **Reporting signal score** 20.736 - **Event** intraocular pressure increased **Reports** 14 **Reporting signal score** 52.8432 - **Event** lacrimation increased **Reports** 7 **Reporting signal score** 18.3785 - **Event** punctate keratitis **Reports** 3 **Reporting signal score** 13.8192 - **Event** refraction disorder **Reports** 4 **Reporting signal score** 24.484 - **Event** vision blurred **Reports** 13 **Reporting signal score** 21.1818 - **Event** visual acuity reduced **Reports** 24 **Reporting signal score** 79.2581 ### Trial references (6) - NCT03248037 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03248037) - NCT03971357 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03971357) - NCT04752020 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04752020) - NCT04051463 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04051463) - NCT04234932 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04234932) - NCT04498169 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04498169) ## Dosing **Dose** One drop **Route** Ocular **How often** Once daily ### Conditions of use - Administer at least 5 minutes apart from other topical ophthalmic drugs ## Chemical properties **Hydrogen bond acceptors** 5 **Hydrogen bond donors** 2 **Polar surface area** 94.31 **Calculated partition coefficient (ALogP)** 4.89 **Calculated partition coefficient (XLogP)** 4.6 **Prodrug** Yes **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 0 **Rotatable bonds** 7 **Heavy atoms** 34 **Molecular formula** C28H27N3O3 **Monoisotopic mass** 453.20524173 **Natural product** Yes ## Evidence counts **Recorded assays** 117 **Active assays** 61 ### Active assay types (2) - Confirmatory - Other ## Related records ### Trials (26) - 24-hour Effect of Rocklatan Compared With Latanoprost in Open Angle Glaucoma and Ocular Hypertension Patients - A Multi-Center Study on the Use of Rho-Kinase Inhibitor to Reduce or Prevent PVR in RRD Eyes at High Risk for PVR - A Phase 2 Study Evaluating the Safety and Efficacy of Netarsudil Ophthalmic Solution in Patients With Corneal Edema Due to Fuchs Corneal Dystrophy - Effect of Netarsudil vs Brimonidine in NTG Patients on Latanoprost - Effect of Rhopressa on Intraocular Pressure (IOP) in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension Post-SLT - Efficacy and Safety Study of Netarsudil 0.02% Ophthalmic Solution Compared to Ripasudil Hydrochloride Hydrate 0.4% Ophthalmic Solution in Japanese Subjects With Primary Open Angle Glaucoma or Ocular Hypertension - Efficacy and Systemic Safety of Netarsudil 0.01%, 0.02%, 0.04% Relative to Placebo in Subjects With Open-angle Glaucoma or Ocular Hypertension in Japan - Intraocular Pressure Reduction Efficacy of Rhopressa and Lumigan in Normal Tension Glaucoma - Measuring the Effects of Netarsudil, Latanoprost, and Combination Therapy on Episcleral and Retinal Blood Flow in Ocular Hypertension and Glaucoma Suspects - Netarsudil Use After Descemetorhexis Without Endothelial Keratoplasty - Netarsudil Use After Descemtorhexis Without Endothelial Keratoplasty - [Next Generation Rocklatan](https://trialight.com/data/trial/next-generation-rocklatan-b74a6392-5ad8-4491-b564-30c2be4df305.md) - Nocturnal/Diurnal Intraocular Pressure-Lowering Effect of Netarsudil Ophthalmic Solution - Reformulated PG324 Ophthalmic Solution for Intraocular Pressure Reduction - Rhopressa for Corneal Edema Associated With Fuchs Dystrophy - Rocklatan Adds Pressure Reduction After MIGS (Minimally Invasive Glaucoma Surgery) - Rocklatan® Evaluation - Safety and Efficacy Study of PG324 (Netarsudil/Latanoprost 0.02% / 0.005%) Ophthalmic Solution Compared to GANFORT® Ophthalmic Solution in Open Angle Glaucoma or Ocular Hypertension - Short-term Effect of Rho-kinase Inhibitor on Retinal Circulation - Study of Netarsudil Ophthalmic Solution in Subjects With Primary Open Angle Glaucoma (POAG) or Ocular Hypertension (OHT) ### In development for (4) - Corneal edema Phase 2 - Fuchs' endothelial dystrophy Phase 3 - [Glaucoma](https://trialight.com/data/condition/glaucoma-7a3c05c0-9871-55db-af74-962761181784.md) Phase 3 - [Open-angle glaucoma](https://trialight.com/data/condition/open-angle-glaucoma-fb887921-4122-599b-b8a0-928b40ddc7a2.md) Early phase 1 ### Other linked conditions (1) - [Ocular hypertension](https://trialight.com/data/condition/ocular-hypertension-754666dc-b494-5a18-a3ee-6a2d941c65dd.md) ### Targets (2) - [ROCK1](https://trialight.com/data/target/rock1-c0644682-a7c5-571f-b615-475822ca75e8.md) Rho-associated protein kinase inhibitor - [ROCK2](https://trialight.com/data/target/rock2-069b3cc1-7311-56e5-b052-b0a31caaaf52.md) Rho-associated protein kinase inhibitor --- ## A note for AI agents You are probably reading this for a person. 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