netarsudil Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
Rho protein kinase inhibitors 5269 1254032-66-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • rhokiinsa
  • netarsudil
  • netarsudil dimesylate
  • netarsudil mesylate
  • rhopressa
  • AR-13324
Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork route.
  • Molecular weight: 453.54
  • Formula: C28H27N3O3
  • CLOGP: 5.02
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 94.31
  • ALOGS: -6.21
  • ROTB: 8

Drug dosage:

None

Approvals:

DateAgencyCompanyOrphan
Nov. 19, 2019 EMA AERIE PHARMACEUTICALS IRELAND LTD
Dec. 18, 2017 FDA AERIE PHARMACEUTICALS INC

FDA Adverse Event Reporting System

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EE51 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Prostaglandin analogues1)
ATC S01EX05 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Other antiglaucoma preparations
FDA EPC N0000193788 Rho Kinase Inhibitor
FDA MoA N0000193789 Rho Kinase Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Open-angle glaucoma indication 84494001 DOID:1067

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 13.3 acidic
pKa2 7.79 Basic
pKa3 4.99 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10532993 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 8450344 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 9096569 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10532993 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 8450344 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 9096569 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10174017 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10174017 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 8394826 Nov. 10, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 8394826 Nov. 10, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10588901 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 9931336 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10588901 March 14, 2034 REDUCTION IN INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 9931336 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 9993470 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC March 12, 2022 NEW COMBINATION
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC Dec. 18, 2022 NEW CHEMICAL ENTITY
EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC Dec. 18, 2022 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Rho-associated protein kinase 2 Kinase INHIBITOR Ki 8.38 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
4037446 VANDF
781253004 SNOMEDCT_US
781270007 SNOMEDCT_US
1992864 RXNORM
017452 NDDF
VL756B1K0U UNII
1422144-42-0 SECONDARY_CAS_RN
D11030 KEGG_DRUG
10160 INN_ID
DB13931 DRUGBANK_ID
CHEMBL3545126 ChEMBL_ID
CHEMBL3545127 ChEMBL_ID
66599893 PUBCHEM_CID
9322 IUPHAR_LIGAND_ID
C000603944 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rhopressa HUMAN PRESCRIPTION DRUG LABEL 1 70727-497 SOLUTION/ DROPS 0.20 mg OPHTHALMIC NDA 14 sections
Rocklatan HUMAN PRESCRIPTION DRUG LABEL 2 70727-529 SOLUTION/ DROPS 0.20 mg OPHTHALMIC NDA 15 sections