netarsudil 🐶 Veterinary Use | 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: 5.01
  • LIPINSKI: 1
  • HAC: 6
  • HDO: 2
  • TPSA: 94.31
  • ALOGS: -6.21
  • ROTB: 8

  • Status: ONP

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

Drug dosage:

None

ADMET properties:

PropertyValueReference
S (Water solubility) 54 mg/mL Bocci G, Oprea TI, Benet LZ
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Bocci G, Oprea TI, Benet LZ

Approvals:

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

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Corneal oedema 132.81 98.22 18 167 1475 63487362
Cornea verticillata 131.42 98.22 14 171 140 63488697
Dacryostenosis acquired 103.16 98.22 13 172 596 63488241
Conjunctival hyperaemia 100.83 98.22 15 170 2364 63486473

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Corneal oedema 230.85 140.39 32 248 2588 79741520
Dacryostenosis acquired 212.77 140.39 25 255 527 79743581
Cornea verticillata 168.14 140.39 18 262 153 79743955

FDA Adverse Event Reporting System (Pediatric)

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 | Suggest Off label Use Form| |View source of the data|

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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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 ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10532993 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10882840 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 11021456 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 8450344 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 9096569 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10532993 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10882840 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 11021456 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 8450344 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 9096569 July 11, 2026 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10174017 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10654844 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 11028081 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 11618748 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10174017 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10654844 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 11028081 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 11618748 Jan. 27, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 8394826 Nov. 10, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 8394826 Nov. 10, 2030 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 10588901 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
EQ 0.02% BASE RHOPRESSA ALCON LABS INC N208254 Dec. 18, 2017 RX SOLUTION/DROPS OPHTHALMIC 9931336 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 10588901 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS INC N208259 March 12, 2019 RX SOLUTION/DROPS OPHTHALMIC 9931336 March 14, 2034 REDUCTION OF ELEVATED INTRAOCULAR PRESSURE
0.005%;EQ 0.02% BASE ROCKLATAN ALCON LABS 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)

None

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
Rho-associated protein kinase 1 Kinase INHIBITOR IC50 7.49 IUPHAR

External reference:

IDSource
W6I5QDT7QI UNII
1422144-42-0 SECONDARY_CAS_RN
C4535718 UMLSCUI
CHEMBL4594250 ChEMBL_ID
CHEMBL3545127 ChEMBL_ID
66599893 PUBCHEM_CID
DB13931 DRUGBANK_ID
CHEMBL4594251 ChEMBL_ID
D11030 KEGG_DRUG
10160 INN_ID
9322 IUPHAR_LIGAND_ID
267237 MMSL
33352 MMSL
017452 NDDF
017453 NDDF
781253004 SNOMEDCT_US
781270007 SNOMEDCT_US
4037446 VANDF
1992863 RXNORM
C000603944 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

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