netarsudil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
Rho protein kinase inhibitors	5269	1254032-66-0

Description:

Molecule	Description
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

Molecule

Description

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:

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

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	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 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	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:

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

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	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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Rho-associated protein kinase 2	Kinase	O75116	ROCK2_HUMAN	INHIBITOR	Ki	8.38		SCIENTIFIC LITERATURE	DRUG LABEL
Rho-associated protein kinase 1	Kinase	Q13464	ROCK1_HUMAN	INHIBITOR	IC50	7.49		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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