Netarsudil
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2017
- First approval year
- 2017
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Netarsudil
- Molecular weight
- 453.54
- Structure (SMILES)
- Cc1ccc(C(=O)OCc2ccc([C@@H](CN)C(=O)Nc3ccc4cnccc4c3)cc2)c(C)c1
- 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
- ATC classification codes
- S01EX05
Sources for recorded values
- CAS registry numbers
- 1254032-66-0
- ChEMBL ID
- CHEMBL4594250
- InChIKey
- OURRXQUGYQRVML-AREMUKBSSA-N
- PubChem compound IDs
- 66599893
- FDA ingredient codes (UNII)
- W6I5QDT7QI
- 1992863
- 1992864
- Applicant
- ALCON LABS INC
- Approval date
- 18 Dec 2017
- Application number
- NDA208254
- 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
- First in class
- Yes
- Orphan designation
- No
- Availability
- Prescription only
- Pharmacology name
- netarsudil
- Type
- Synthetic organic
- Drug name stem
- -dil
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- topical
- 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
- 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
- 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
- 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
- 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
- NCT03248037
- NCT03971357
- NCT04752020
- NCT04051463
- NCT04234932
- NCT04498169
- Dose
- One drop
- Route
- Ocular
- How often
- Once daily
Conditions of use
- Administer at least 5 minutes apart from other topical ophthalmic drugs
- 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
- Recorded assays
- 117
- Active assays
- 61
- 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
- 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 Phase 3
- Open-angle glaucoma Early phase 1