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netarsudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| Rho protein kinase inhibitors | 5269 | 1254032-66-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork route.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK5,CDK7,CDK9,CHEK1,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT3,GRK1,GRK2,GRK3,GSK3B,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K1,MAP3K10,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKACA,PRKCD,PRKDC,PRKG1,ROCK1,ROCK2,SGK1,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1,ULK2,ZAP70 | 83 | |||
| kinase-selectivity-class | AKT2,AKT3,AXL,BRAF,CDK9,DYRK1B,EIF2AK3,GRK2,PDK4,PRKACA,PRKCD,ROCK1 | 12 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 19, 2019 | EMA | AERIE PHARMACEUTICALS IRELAND LTD | |
| Dec. 18, 2017 | FDA | AERIE PHARMACEUTICALS INC |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Corneal oedema | 177.60 | 79.26 | 25 | 348 | 1876 | 90626198 |
| Cornea verticillata | 128.64 | 79.26 | 15 | 358 | 243 | 90627831 |
| Ocular hyperaemia | 127.14 | 79.26 | 29 | 344 | 33769 | 90594305 |
| Conjunctival hyperaemia | 98.16 | 79.26 | 16 | 357 | 3153 | 90624921 |
| Dacryostenosis acquired | 95.23 | 79.26 | 13 | 360 | 766 | 90627308 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Corneal oedema | 227.64 | 111.18 | 32 | 248 | 1516 | 42619539 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Corneal oedema | 327.46 | 94.80 | 46 | 455 | 3127 | 110585671 |
| Dacryostenosis acquired | 200.53 | 94.80 | 25 | 476 | 659 | 110588139 |
| Cornea verticillata | 152.01 | 94.80 | 18 | 483 | 302 | 110588496 |
| Conjunctival hyperaemia | 126.46 | 94.80 | 22 | 479 | 5809 | 110582989 |
| Off label use | 99.37 | 94.80 | 68 | 433 | 1500117 | 109088681 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| 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 |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
| CHEBI has role | CHEBI:35674 | antihypertensive agent |
Related Drugs by ATC class:
S01EE Prostaglandin analogues 6 drugs
S01EX Other antiglaucoma preparations 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 13.3 | acidic |
| pKa2 | 7.79 | Basic |
| pKa3 | 4.99 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 | 11020385 | 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 | 11020385 | 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:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| W6I5QDT7QI | UNII |
| 1422144-42-0 | SECONDARY_CAS_RN |
| 4037446 | VANDF |
| C4535718 | UMLSCUI |
| CHEBI:757758 | CHEBI |
| CHEMBL4594250 | ChEMBL_ID |
| 66599893 | PUBCHEM_CID |
| DB13931 | DRUGBANK_ID |
| CHEMBL4594251 | ChEMBL_ID |
| D11030 | KEGG_DRUG |
| 10160 | INN_ID |
| C000603944 | MESH_SUPPLEMENTAL_RECORD_UI |
| 9322 | IUPHAR_LIGAND_ID |
| 1371434000 | SNOMEDCT_US |
| 781253004 | SNOMEDCT_US |
| 781270007 | SNOMEDCT_US |
| 267237 | MMSL |
| 33352 | MMSL |
| 017452 | NDDF |
| 017453 | NDDF |
| 1992863 | RXNORM |
| W6I5QDT7QI | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Rhopressa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70727-497 | SOLUTION/ DROPS | 0.20 mg | OPHTHALMIC | NDA | 23 sections |
| Rocklatan | HUMAN PRESCRIPTION DRUG LABEL | 2 | 70727-529 | SOLUTION/ DROPS | 0.20 mg | OPHTHALMIC | NDA | 25 sections |