Netarsudil

Rho Kinase Inhibitor — SENSORY ORGANS

Key facts

Netarsudil is an onp drug in the Rho Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2017. Its mechanism of action is classified as Rho Kinase Inhibitors. DrugCentral lists 2 molecular targets, including ROCK2 and ROCK1. Recorded indications include Ocular hypertension and Open-angle glaucoma.

• Approval status: onp (first approved 2017 by the FDA).
• Drug class: Rho Kinase Inhibitor.
• Mechanism of action: Rho Kinase Inhibitors.
• Molecular targets: ROCK2 and ROCK1 (2 listed in DrugCentral).
• Indications: Ocular hypertension and Open-angle glaucoma.
• ATC code: S01EE51 (Prostaglandin analogues).
• Molecular formula: C28H27N3O3; molecular weight 453.54 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Ocular hypertension
• Open-angle glaucoma

Mechanism & targets

• Mechanism of action (MoA): Rho Kinase Inhibitors
• Established pharmacologic class: Rho Kinase Inhibitor

Molecular targets (2)

Target	Gene	Action	Activity
Rho-associated protein kinase 2	ROCK2	inhibitor	Ki 8.38
Rho-associated protein kinase 1	ROCK1	inhibitor	IC50 7.49

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2019-11-19	EMA	—	AERIE PHARMACEUTICALS IRELAND LTD
2017-12-18	FDA	—	AERIE PHARMACEUTICALS INC

ATC classification

ATC code	Therapeutic hierarchy
S01EE51	SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Prostaglandin analogues
S01EX05	SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Other antiglaucoma preparations

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Corneal oedema	404.5
Conjunctival hyperaemia	282.9
Cornea verticillata	246.0
Ocular hyperaemia	213.8
Dacryostenosis acquired	181.5
Visual acuity reduced	152.6
Intraocular pressure increased	107.2
Off label use	88.3
Eye irritation	84.5
Vision blurred	70.7

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Netarsudil is on its molecule page.

• Molecular formula: C₂₈H₂₇N₃O₃
• Molecular weight: 453.54 g/mol
• CAS number: 1254032-66-0
• InChIKey: OURRXQUGYQRVML-AREMUKBSSA-N
• PubChem CID: 66599893

CC1=CC=C(C(=O)OCC2=CC=C(C=C2)[C@@H](CN)C(=O)NC2=CC3=C(C=C2)C=NC=C3)C(C)=C1

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Netarsudil used for?

DrugCentral lists the following indications for Netarsudil: Ocular hypertension and Open-angle glaucoma.

How does Netarsudil work?

Netarsudil is classified as Rho Kinase Inhibitors; its molecular targets in DrugCentral include ROCK2 (inhibitor) and ROCK1 (inhibitor).

When was Netarsudil first approved?

Netarsudil was first approved by the FDA in 2017.

What drug class does Netarsudil belong to?

Netarsudil is in the Rho Kinase Inhibitor class.

What is the chemical formula of Netarsudil?

Netarsudil has the molecular formula C28H27N3O3 and a molecular weight of 453.54 g/mol.

Sources

• DrugCentral drug card 5269 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4594250 — compound record and bioactivity
• PubChem CID 66599893 — chemical identifiers
• DrugBank DB13931 — drug record
• FDA UNII W6I5QDT7QI — substance identity
• DailyMed: FDA labels for Netarsudil — current prescribing information (label search)
• UniProt O75116 (ROCK2) — target protein
• UniProt Q13464 (ROCK1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.