Nepafenac

After topical ocular dosing, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a NSAID. Nepafenac and amfenac are thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production.

• ILEVRO ® 0.3% is indicated for the treatment of pain and inflammation associated with cataract surgery. ILEVRO ® 0.3% is a nonsteroidal, anti-inflammatory prodrug indicated for the treatment of pain and inflammation associated with cataract surgery ( 1 ).

• ILEVRO ® 0.3% is contraindicated in patients with previously demonstrated hypersensitivity to any of the ingredients in the formula or to other nonsteroidal anti-inflammatory drugs (NSAIDs). Hypersensitivity to any of the ingredients in the formula or to other non-steroidal anti-inflammatory drugs (NSAIDS).contraindicated

One drop of ILEVRO ® 0.3% should be applied to the affected eye one-time-daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period. An additional drop should be administered 30 to 120 minutes prior to surgery. ( 2 ) 2.1 Recommended Dosing One drop of ILEVRO ® 0.3% should be applied to the affected eye one time daily beginning 1 day prior to cataract surgery, continued on the day of surgery and through the first 2 weeks of the postoperative period. An additional drop should be administered 30 to 120 minutes prior to surgery. 2.2 Use with Other Topical Ophthalmic Medications ILEVRO ® 0.3% may be administered in conjunction with other topical ophthalmic medications such as beta-blockers, carbonic anhydrase inhibitors, alpha-agonists, cycloplegics, and mydriatics. If more than one topical ophthalmic medication is being used, the medicines must be administered at least 5 minutes apart.

Increased bleeding time due to interference with thrombocyte aggregation ( 5.1 ) Delayed healing ( 5.2 ) Corneal effects including keratitis ( 5.3 ) 5.1 Increased Bleeding Time With some NSAIDs including ILEVRO ® 0.3%, there exists the potential for increased bleeding time due to interference with thrombocyte aggregation. There have been reports that ocularly applied nonsteroidal anti-inflammatory drugs may cause increased bleeding of ocular tissues (including hyphema) in conjunction with ocular surgery. It is recommended that ILEVRO ® 0.3% be used with caution in patients with known bleeding tendencies or who are receiving other medications which may prolong bleeding time. 5.2 Delayed Healing Topical NSAIDs including ILEVRO ® 0.3%, may slow or delay healing. Topical corticosteroids are also known to slow or delay healing. Concomitant use of topical NSAIDs and topical steroids may increase the potential for healing problems. 5.3 Corneal Effects Use of topical NSAIDs may result in keratitis. In some susceptible patients, continued use of topical NSAIDs may result in epithelial breakdown, corneal thinning, corneal erosion, corneal ulceration, or corneal perforation. These events may be sight threatening. Patients with evidence of corneal epithelial breakdown should immediately discontinue use of topical NSAIDs including ILEVRO ® 0.3% and should be closely monitored for corneal health.

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 the rates in the clinical studies of another drug and may not reflect the rates observed in practice. Most common adverse reactions (5% to 10%) are capsular opacity, decreased visual acuity, foreign body sensation, increased intraocular pressure, and sticky sensation. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Harrow Eye, LLC at 1-833-4HARROW or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Serious and Otherwise Important Adverse Reactions The following adverse reactions are discussed in greater detail in other sections of labeling. Increased Bleeding Time [see Warnings and Precautions (5.1) ] Delayed Healing [see Warnings and Precautions (5.2) ] Corneal Effects [see Warnings and Precautions (5.3) ] 6.2 Ocular Adverse Reactions The most frequently reported ocular adverse reactions following cataract surgery were capsular opacity, decreased visual acuity, foreign body sensation, increased intraocular pressure (IOP), and sticky sensation. These reactions occurred in approximately 5% to 10% of patients. Other ocular adverse reactions occurring at an incidence of approximately 1% to 5% included conjunctival edema, corneal edema, dry eye, lid margin crusting, ocular discomfort, ocular hyperemia, ocular pain, ocular pruritus, photophobia, tearing, and vitreous detachment. Some of these reactions may be the consequence of the cataract surgical procedure.

8.1 Pregnancy Teratogenic Effects. Pregnancy Category C: Reproduction studies performed with nepafenac in rabbits and rats at oral doses up to 10 mg/kg/day have revealed no evidence of teratogenicity due to nepafenac, despite the induction of maternal toxicity. At this dose, the animal plasma exposure to nepafenac and amfenac was approximately 70 and 630 times human plasma exposure at the recommended human topical ophthalmic dose for rats and 20 and 180 times human plasma exposure for rabbits, respectively. In rats, maternally toxic doses greater than or equal to 10 mg/kg were associated with dystocia, increased postimplantation loss, reduced fetal weights and growth, and reduced fetal survival. Nepafenac has been shown to cross the placental barrier in rats. There are no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, ILEVRO ® 0.3% should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Non-teratogenic Effects Because of the known effects of prostaglandin biosynthesis inhibiting drugs on the fetal cardiovascular system (closure of the ductus arteriosus), the use of ILEVRO ® 0.3% during late pregnancy should be avoided. 8.3 Nursing Mothers Nepafenac is excreted in the milk of lactating rats.

Metabolism

Following bilateral topical ocular once-daily dosing of ILEVRO ® 0.3%, the concentrations of nepafenac and amfenac peaked at a median time of 0.5 hour and 0.75 hour, respectively on both Day 1 and Day 4. The mean steady-state C max for nepafenac and for amfenac were 0.847 ± 0.269 ng/mL and 1.13 ± 0.491 ng/mL, respectively.

• Aug 19, 2005NDANDA021862Harrow Eye
• Oct 16, 2012NDANDA203491Harrow Eye

1. 1Eye Pain45414%
2. 2Drug Ineffective32610%
3. 3Treatment Failure2307.3%
4. 4Vision Blurred2136.7%
5. 5Off Label Use1404.4%
6. 6Cataract1294.1%
7. 7Visual Impairment1233.9%
8. 8Eye Irritation1073.4%
9. 9Fatigue1013.2%
10. 10Visual Acuity Reduced932.9%
11. 11Headache812.6%
12. 12Nausea812.6%
13. 13Chronic Kidney Disease722.3%
14. 14Ocular Hyperaemia682.1%
15. 15Ulcerative Keratitis672.1%

The 10 most recently updated of 57 ClinicalTrials.gov registrations naming Nepafenac as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• The TRIBECA Study (TRIessence/Byqlovi for Easier CAtaract Surgery)
  Not yet recruiting · Phase 4 · Interventional · 40 enrolled · Research Insight LLC
  NCT07276802updated 2026-03-31
• A Comparative Analysis of the Effectiveness of Nepafenac Combined With a Lubricant Versus a Lubricant Alone in the Treatment of Epiphora Associated With Lacrimal Punctum Stenosis
  Active not recruiting · Phase 4 · Interventional · 68 enrolled · Instituto de Oftalmología Fundación Conde de Valenciana
  NCT07372014updated 2026-01-28
• Comparing Efficacy of Bromfenac 0.09%, Nepafenac 0.3% and Diclofenac 0.1% in Patients After Cataract Surgery
  Recruiting · Interventional · 150 enrolled · Nemocnice Kolín
  NCT07178639updated 2025-09-17
• Effects of 0.1% Nepafenac on Vitreous Inflammatory Biomarkers in Rhegmatogenous Retinal Detachment and Proliferative Vitreoretinopathy
  Completed · Phase 4 · Interventional · 61 enrolled · Indonesia University
  NCT07162818updated 2025-09-09
• NSAID Phase II for Non-central Involved Diabetic Macular Edema (DME)
  Completed · Phase 2 · Interventional · 125 enrolled · Jaeb Center for Health Research
  NCT01331005updated 2025-03-10
• Effect of Topical Nepafenac in Macular Thickening Related to Pan-retinal Photocoagulation
  Terminated · Phase 2 · Interventional · 50 enrolled · Asociación para Evitar la Ceguera en México
  NCT00801905updated 2024-05-30
• Eplerenone, Aflibercept and Topical Nepafenac Serous Foveal Deta Chment in Central Serous Chorioretinopathy
  Completed · Observational · 16 enrolled · Dar El Oyoun Hospital
  NCT05847049updated 2023-05-06
• DSAEK/DMEK and Cystoid Macular Edema - the Role for Topical NSAIDs (Nepafenac) (DMEC)
  Recruiting · Phase 4 · Interventional · 300 enrolled · Oslo University Hospital
  NCT05072262updated 2022-12-01
• Cataract Surgery and Inflammation - the Role for Preoperative NSAIDs (Pre-CIN)
  Unknown · Phase 4 · Interventional · 500 enrolled · Oslo University Hospital
  NCT05331690updated 2022-12-01
• Safety/Efficacy of Nepafenac Punctal Plug Delivery System Compared to Placebo to Control Ocular Pain/Inflammation After Cataract
  Completed · Phase 2 · Interventional · 56 enrolled · Mati Therapeutics Inc.
  NCT03496467updated 2021-10-12

Frequently asked questions

How does Nepafenac work?

After topical ocular dosing, nepafenac penetrates the cornea and is converted by ocular tissue hydrolases to amfenac, a NSAID. Nepafenac and amfenac are thought to inhibit the action of prostaglandin H synthase (cyclooxygenase), an enzyme required for prostaglandin production.

What is Nepafenac used for?

According to FDA labeling, Nepafenac carries indications including: ILEVRO ® 0.3% is indicated for the treatment of pain and inflammation associated with cataract surgery. ILEVRO ® 0.3% is a nonsteroidal, anti-inflammatory prodrug indicated for the treatment of pain and inflammation associated with cataract surgery ( 1 ).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Nepafenac?

Nepafenac is classified as Antiinflammatory agents, non-steroids, Nonsteroidal Anti-inflammatory Drug, Cyclooxygenase Inhibitors, Decreased Prostaglandin Production.

What are the brand names for Nepafenac?

Nepafenac is marketed under brand names including Ilevro, Nevanac.

What are the contraindications for Nepafenac?

Nepafenac labeling lists contraindications including: ILEVRO ® 0.3% is contraindicated in patients with previously demonstrated hypersensitivity to any of the ingredients in the formula or to other nonsteroidal anti-inflammatory drugs (NSAIDs). Hypersensitivity to any of the ingredients in the formula or to other non-steroidal anti-inflammatory drugs (NSAIDS).. Always consult the full prescribing information and a clinician.