Netarsudil

Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork. The exact mechanism is unknown.

• RHOPRESSA is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. RHOPRESSA ® is a Rho kinase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.ICD-10: H40.059, H40.9

• None. None.contraindicated

The recommended dosage is one drop in the affected eye(s) once daily in the evening. If one dose is missed, treatment should continue with the next dose in the evening. Twice a day dosing is not well tolerated and is not recommended. If RHOPRESSA is to be used concomitantly with other topical ophthalmic drug products to lower IOP, administer each drug product at least 5 minutes apart [see Patient Counseling Information ( 17 )]. One drop into the affected eye(s) once daily in the evening. ( 2 )

5.1 Epithelial Corneal Edema Epithelial corneal edema, described as honeycomb or bullous, has been reported in some patients with pre-existing corneal stromal edema or following ocular procedures that could affect corneal endothelial function. Epithelial corneal edema typically resolves upon discontinuation of RHOPRESSA. Advise patients to notify their physician if they experience eye pain or decreased vision while using RHOPRESSA [see Adverse Reactions ( 6.2 ) and Patient Counselling Information ( 17 )] . 5.2 Bacterial Keratitis There have been reports of bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface [see Patient Counseling Information ( 17 )]. 5.3 Use with Contact Lenses Contact lenses should be removed prior to instillation of RHOPRESSA and may be reinserted 15 minutes following its administration.

The most common adverse reaction is conjunctival hyperemia (53%). Other common adverse reactions, approximately 20% include: corneal verticillata, instillation site pain, and conjunctival hemorrhage. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Alcon Laboratories, Inc. at 1‑800-757-9195, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice. The most common ocular adverse reaction observed in controlled clinical studies with RHOPRESSA dosed once daily was conjunctival hyperemia which was reported in 53% of patients. Six percent of patients discontinued therapy due to conjunctival hyperemia. Other common (approximately 20%) ocular adverse reactions reported were: corneal verticillata, instillation site pain, and conjunctival hemorrhage. Instillation site erythema, corneal staining, blurred vision, increased lacrimation, erythema of eyelid, and reduced visual acuity were reported in 5-10% of patients. Corneal Verticillata Corneal verticillata occurred in approximately 20% of the patients in controlled clinical studies. The corneal verticillata seen in RHOPRESSA-treated patients were first noted at 4 weeks of daily dosing. This reaction did not result in any apparent visual functional changes in patients. Most corneal verticillata resolved upon discontinuation of treatment.

8.1 Pregnancy Risk Summary There are no available data on RHOPRESSA use in pregnant women to inform any drug associated risk; however, systemic exposure to netarsudil from ocular administration is low [see Clinical Pharmacology ( 12.3 ) ] . Intravenous administration of netarsudil to pregnant rats and rabbits during organogenesis did not produce adverse embryofetal effects at clinically relevant systemic exposures [see Data] . Data Animal Data Netarsudil administered daily by intravenous injection to rats during organogenesis caused abortions and embryofetal lethality at doses ≥0.3 mg/kg/day (126-fold the plasma exposure at the recommended human ophthalmic dose [RHOD], based on C max ). The no-observed-adverse-effect-level (NOAEL) for embryofetal development toxicity was 0.1 mg/kg/day (40-fold the plasma exposure at the RHOD, based on C max ). Netarsudil administered daily by intravenous injection to rabbits during organogenesis caused embryofetal lethality and decreased fetal weight at 5 mg/kg/day (1480-fold the plasma exposure at the RHOD, based on C max ). Malformations were observed at ≥3 mg/kg/day (1330-fold the plasma exposure at the RHOD, based on C max ), including thoracogastroschisis, umbilical hernia and absent intermediate lung lobe. The NOAEL for embryofetal development toxicity was 0.5 mg/kg/day (214-fold the plasma exposure at the RHOD, based on C max ).

Metabolism

Absorption The systemic exposures of netarsudil and its active metabolite, AR-13503, were evaluated in 18 healthy subjects after topical ocular administration of RHOPRESSA 0.02% once daily (one drop bilaterally in the morning) for 8 days. There were no quantifiable plasma concentrations of netarsudil (lower limit of quantitation (LLOQ) 0.100 ng/mL) post dose on Day 1 and Day 8.

• Dec 18, 2017NDANDA208254Alcon Labs Inc
• Mar 12, 2019NDANDA208259Alcon Labs Inc

1. 1Conjunctival Hyperaemia33412%
2. 2Ocular Hyperaemia2659.7%
3. 3Vision Blurred2519.2%
4. 4Eye Pain2137.8%
5. 5Eye Irritation2127.8%
6. 6Off Label Use1766.5%
7. 7Lacrimation Increased1605.9%
8. 8Product Dose Omission Issue1405.1%
9. 9Eye Pruritus1254.6%
10. 10Intraocular Pressure Increased1234.5%
11. 11Drug Ineffective1094.0%
12. 12Visual Acuity Reduced1063.9%
13. 13Corneal Oedema1033.8%
14. 14Death843.1%
15. 15Headache813.0%

The 10 most recently updated of 46 ClinicalTrials.gov registrations naming Netarsudil as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Imaging the Effects of Netarsudil (Rhopressa) on the Trabecular Meshwork in Glaucoma and Ocular Hypertension
  Recruiting · Phase 4 · Interventional · 50 enrolled · Indiana University
  NCT07588152updated 2026-06-11
• Effect of Rhopressa on Intraocular Pressure (IOP) in Patients With Primary Open-Angle Glaucoma or Ocular Hypertension Post-SLT
  Active not recruiting · Phase 4 · Interventional · 70 enrolled · East Coast Institute for Research
  NCT06865144updated 2026-06-10
• Rocklatan vs Latanoprost Post-DSLT
  Recruiting · Phase 4 · Interventional · 36 enrolled · Eye Centers of Southeast Texas
  NCT07465913updated 2026-05-22
• Retinal Ganglion Cell Neuroprotection Under Prostaglandin Analogues
  Not yet recruiting · Observational · 1,500 enrolled · Association for Innovation and Biomedical Research on Light and Image
  NCT07074782updated 2026-05-06
• 24-hour Effect of Rocklatan Compared With Latanoprost in Open Angle Glaucoma and Ocular Hypertension Patients
  Recruiting · Phase 4 · Interventional · 30 enrolled · Mayo Clinic
  NCT07325240updated 2026-05-01
• Reformulated PG324 Ophthalmic Solution for Intraocular Pressure Reduction
  Completed · Phase 3 · Interventional · 489 enrolled · Alcon Research
  NCT07082816updated 2026-04-21
• Improved Efficacy of Selective Laser Trabeculoplasty With the Addition of Rocklatan Post-treatment vs Artificial Tears Post-treatment
  Completed · Observational · 70 enrolled · Colorado Ophthalmology Associates PC
  NCT06819046updated 2026-03-18
• Efficacy and Safety Assessment of T4090 Ophthalmic Solution Versus Rhopressa® Ophthalmic Solution in Patients With Open-angle Glaucoma or Ocular Hypertension
  Completed · Phase 2 · Interventional · 161 enrolled · Laboratoires Thea
  NCT06394973updated 2026-01-02
• Evaluating Injection With the Use of Brimonidine Tartrate Ophthalmic 0.025% on Patients Using Netarsudil 0.02%/Latanoprost 0.005% to Treat Glaucoma
  Recruiting · Phase 4 · Interventional · 35 enrolled · Insight Eyecare Specialties, Inc. dba Vision Source Eyecare,
  NCT07209410updated 2025-11-18
• Next Generation Rocklatan
  Completed · Phase 2 · Interventional · 426 enrolled · Alcon Research
  NCT06441643updated 2025-11-18

Frequently asked questions

How does Netarsudil work?

Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork. The exact mechanism is unknown.

What is Netarsudil used for?

According to FDA labeling, Netarsudil carries indications including: RHOPRESSA is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. RHOPRESSA ® is a Rho kinase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Netarsudil?

Netarsudil is classified as Other antiglaucoma preparations, Rho Kinase Inhibitor, Norepinephrine Uptake Inhibitors, Rho Kinase Inhibitors, Decreased Intraocular Fluid Pressure.

What are the brand names for Netarsudil?

Netarsudil is marketed under brand names including Rhopressa, Rocklatan.

What are the contraindications for Netarsudil?

Netarsudil labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.