netarsudil Indications/Contra | FAERs-F | FAERs-M | Orange Bk | 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

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

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

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC S01EE51 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Prostaglandin analogues
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)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.005%;EQ 0.02% BASE ROCKLATAN AERIE PHARMS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC March 12, 2022 NEW COMBINULLTION
EQ 0.02% BASE RHOPRESSA AERIE PHARMS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC Dec. 18, 2022 NEW CHEMICAL ENTITY
0.005%;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
1422144-42-0 SECONDARY_CAS_RN
4037446 VANDF
C4079000 UMLSCUI
CHEMBL4594250 ChEMBL_ID
CHEMBL4594251 ChEMBL_ID
CHEMBL3545127 ChEMBL_ID
D11030 KEGG_DRUG
66599893 PUBCHEM_CID
DB13931 DRUGBANK_ID
C000603944 MESH_SUPPLEMENTAL_RECORD_UI
9322 IUPHAR_LIGAND_ID
10160 INN_ID
W6I5QDT7QI UNII
1992863 RXNORM
267237 MMSL
33352 MMSL
017452 NDDF
017453 NDDF
781253004 SNOMEDCT_US
781270007 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Rhopressa HUMAN PRESCRIPTION DRUG LABEL 1 70727-497 SOLUTION/ DROPS 0.20 mg OPHTHALMIC NDA 22 sections
Rocklatan HUMAN PRESCRIPTION DRUG LABEL 2 70727-529 SOLUTION/ DROPS 0.20 mg OPHTHALMIC NDA 23 sections