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Nepafenac, 0.3%

Phase 3

Cataract | Small molecule | Ophthalmology |Alcon Inc.|Last Updated: Nov 18, 2016

Target and mechanism

Molecular targetPTGS2, PTGS1
Target classInhibitor
ModalitySmall molecule

Also known as Nepafenac Ophthalmic Suspension, 0.3%, Nepafenac ophthalmic suspension, 0.1% (NEVANAC), Nepafenac, 0.1%, Nepafenac ophthalmic solution 0.1%, Nepafenac 0.1%, Nepafenac Ophthalmic Suspension, 0.1%

Success Probability

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Market & Valuation

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Trial Design

RandomizedDouble-BlindPLACEBO_CONTROLLED
Total Trials5
Total Enrollment4,138

FDA Designations

No designations recorded

Clinical trial landscape

Nepafenac, 0.3% · 9 trials · 4 indications

Phase 3 7Phase 2 2
NCT01853072Nepafenac Once Daily for Macular Edema - Study 1Non-Proliferative Diabetic Retinopathy
COMPLETED881 Analytics
NCT01872611Nepafenac Once Daily for Macular Edema - Study 2Non-Proliferative Diabetic Retinopathy
COMPLETED819 Analytics
NCT01426854Nepafenac Compared to Placebo for Ocular Pain and InflammationCataract
COMPLETED260 Analytics
NCT01109173Confirmatory Study Nepafenac 0.3%Cataract
COMPLETED2,120 Analytics
NCT00332774Nevanac 3-Month Safety Study With QID DosingCataract
COMPLETED149 Analytics
NCT00405730Nepafenac 0.1% Eye Drops, Suspension Compared to Ketorolac Trometamol 0.5% Eye Drops, Solution and PlaceboCataracts
COMPLETED227 Analytics
NCT00333255Nepafenac Opthalmic Suspension 0.1% Compared to Acular LS for Treatment of Inflammation After Cataract SurgeryCataract
COMPLETED267 Analytics
PHASE3COMPLETED
Nepafenac Once Daily for Macular Edema - Study 1
Non-Proliferative Diabetic RetinopathyUnlock trial analytics
PHASE3COMPLETED
Nepafenac Once Daily for Macular Edema - Study 2
Non-Proliferative Diabetic RetinopathyUnlock trial analytics
PHASE3COMPLETED
Nepafenac Compared to Placebo for Ocular Pain and Inflammation
CataractUnlock trial analytics
PHASE3COMPLETED
Confirmatory Study Nepafenac 0.3%
CataractUnlock trial analytics
PHASE3COMPLETED
Nevanac 3-Month Safety Study With QID Dosing
CataractUnlock trial analytics
PHASE3COMPLETED
Nepafenac 0.1% Eye Drops, Suspension Compared to Ketorolac Trometamol 0.5% Eye Drops, Solution and Placebo
CataractsUnlock trial analytics
PHASE3COMPLETED
Nepafenac Opthalmic Suspension 0.1% Compared to Acular LS for Treatment of Inflammation After Cataract Surgery
CataractUnlock trial analytics

Study Endpoints

Primary Endpoints

Percentage of Participants With Best-corrected Visual Acuity (BCVA) Improvement of ≥ 15 Letters From Preoperative Baseline to Day 14 and Maintained Through Day 90
Baseline to Day 14, and maintained through Day 90

BCVA (with spectacles or other visual corrective devices) was reported in letters read correctly, using the Early Treatment Diabetic Retinopathy Study (ETDRS) test of 70 letters. Improvement of BCVA was defined as an increase (gain) in the number of letters read, compared to the baseline assessment. One eye (study eye) contributed to the analysis.

Percentage of Participants Who Develop Macular Edema Within 90 Days Following Cataract Surgery (Day 0)
Day 0 to Day 90

Macular edema was defined as ≥ 30% Increase from pre-operative baseline in central subfield macular thickness, as measured with Spectral Domain Ocular Coherence Tomography (SD-OCT). One eye (study eye) contributed to the analysis.

Proportion of Subjects With Clinical Cure at Day 14
Day 14 postoperative

Ocular inflammation was assessed by the Investigator during slit lamp examination. Aqueous cells were scored on a 5-unit scale from 0 (none) to 4 (\>30 cells), and aqueous flare (protein escaping from dilated vessels) was scored on a 4-unit scale from 0 (no visible flare when compared with the normal eye) to 3 (severe - very dense flare). To be considered cured, the patient must have had a score of 0 for both aqueous cells and aqueous flare. The proportion of subjects with a clinical cure is reported as percentage.

Percentage of Patients Cured at Day 14
Day 14

Ocular inflammation was assessed by the investigator during slit lamp examination. Aqueous cells were scored on a 5-unit scale from 0 (none) to 4 (\> 30 cells), and aqueous flare (protein escaping from dilated vessels) was scored on a 4-unit scale from 0 (no visible flare when compared with the normal eye) to 3 (severe - very dense flare). To be considered cured, the patient must have had a score of 0 for both cells and flare.

Macular thickness
Percentage of Patients with Day 14 Cure
Day 14

Cure is defined as aqueous cells score = 0 and aqueous cells score = 0 at Day 14.

Percentage of patients who are a clinical success at Day 14 postoperative visit (where a "clinical success" is defined as aqueous cells < grade 1 and aqueous flare = grade 0 at the current visit and all subsequent visits).
Percentage of Patients Cured at Day 14, Nepafenac 0.3% vs. Nepafenac Vehicle 0.3%
Day 14 postoperative

Ocular inflammation was assessed by the investigator during slit lamp examination. Aqueous cells were scored on a 5-unit scale from 0 (none) to 4 (\> 30 cells), and aqueous flare (protein escaping from dilated vessels) was scored on a 4-unit scale from 0 (no visible flare when compared with the normal eye) to 3 (severe - very dense flare). To be considered cured, the patient must have had a score of 0 for both aqueous cells and aqueous flare.

Percent of Patients Who Developed Macular Edema (ME) Within 90 Days Following Cataract Surgery
3 Months

Macular edema (thickening of the center of the back of the eye) was defined as 30% or greater increase from pre-operative baseline measurement in central subfield macular thickness as measured using Optical Coherence Tomography(OCT).

Secondary Endpoints

Percentage of Participants With BCVA Improvement of ≥ 15 Letters From Preoperative Baseline to Day 90
Baseline to Day 90
Percentage of Participants With BCVA Improvement of ≥ 15 Letters From Preoperative Baseline to Day 60
Baseline to Day 60
Percentage of Participants With a > 5-letter Loss in BCVA From Day 7 to Any Visit [Time Frame: Day 7 up to Any Visit]
Day 7 up to any visit through Day 90
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Study Design & Arms

AllocationRANDOMIZED
MaskingDOUBLE
ModelPARALLEL
PurposeTREATMENT

Treatment Arms

ArmTypeDescription
NepafenacEXPERIMENTALWith prednisolone acetate standard of care, Nepafenac Ophthalmic Suspension, 0.3%, 1 drop instilled in the operative eye 1 day prior to surgery, continuing on the day of surgery, and for 90 days following surgery. An additional 1 drop will be administered 30 to 120 minutes prior to surgery.
VehiclePLACEBO_COMPARATORWith prednisolone acetate standard of care, Nepafenac vehicle, 1 drop instilled in the operative eye 1 day prior to surgery, continuing on the day of surgery, and for 90 days following surgery. An additional 1 drop will be administered 30 to 120 minutes prior to surgery.
PlaceboPLACEBO_COMPARATORNepafenac Vehicle, 1 drop to the operative eye, 3 times a day, beginning 1 day preoperatively and continuing through the day of surgery and for 14 days postoperatively. An additional dose was administered prior to surgery.
Nepafenac 0.3%EXPERIMENTALNepafenac Ophthalmic Suspension, 0.3%, one drop in affected eye once daily for 16 days, beginning one day prior to surgery, continuing on the day of surgery, and for 14 days following surgery. An additional dose was administered between 30-120 minutes prior to surgery.
NEVANACACTIVE_COMPARATORNepafenac Ophthalmic Suspension, 0.1%, one drop in affected eye three times daily, beginning one day prior to surgery, continuing on the day of surgery, and for 14 days following surgery.
Nepafenac Vehicle 0.3%PLACEBO_COMPARATORNepafenac Ophthalmic Suspension 0.3% Vehicle, one drop in affected eye once daily for 16 days, beginning one day prior to surgery, continuing on the day of surgery, and for 14 days following surgery. An additional dose was administered between 30-120 minutes prior to surgery.
NEVANAC VehiclePLACEBO_COMPARATORNepafenac 0.1% vehicle, one drop in affected eye three times daily, beginning one day prior to surgery, continuing on the day of surgery, and for 14 days following surgery.
AcularACTIVE_COMPARATOR -
Ketorolac TrometamolACTIVE_COMPARATOROne drop in the study eye 3 times daily for 23 days
Nepafenac VehiclePLACEBO_COMPARATOROne drop in the study eye 3 times daily for 23 days
Nepafenac 0.1%ACTIVE_COMPARATORNepafenac Ophthalmic Suspension, 0.1%, one drop in affected eye once daily, for 16 days, beginning one day prior to surgery, continuing on the day of surgery, and for 14 days following surgery. An additional drop was administered between 30-120 minutes prior to surgery.

Interventions

NameTypeDescription
Nepafenac Ophthalmic Suspension, 0.3%DRUGTest intervention
Nepafenac vehicleOTHERInactive ingredients used as placebo comparator
Prednisolone acetateDRUG1 drop instilled in the operative eye 4 times daily beginning post-operatively on the day of surgery for the first 2 weeks, followed by 2 times daily for the next 2 weeks
VehicleOTHERInactive ingredients used as placebo comparator
Nepafenac Ophthalmic Suspension, 0.1%DRUGTopical ocular administration
Nepafenac Vehicle Ophthalmic SolutionOTHERInactive ingredients used as placebo; topical ocular administration
Nepafenac Ophthalmic Suspension 0.3% VehicleOTHERNepafenac 0.3% vehicle, one drop in affected eye once daily, for 16 days. An additional dose was administered between 30-120 minutes prior to surgery.
NEVANAC VehicleOTHERNepafenac vehicle, one drop in affected eye three times daily, for 16 days
Nepafenac ophthalmic solution 0.1%DRUG1 drop 4 times daily for 90 days
Ketorolac Tromethamine ophthalmic solution 0.4%DRUG1 drop 4 times daily for 90 days
Nepafenac ophthalmic suspension vehicleOTHER -
Nepafenac 1mg/ml eye drops, suspensionDRUGOne drop in the study eye 3 times daily for 23 days
Ketorolac Trometamol 5 mg/ml eye drops, solutionDRUGOne drop in the study eye 3 times daily for 23 days
Nepafenac vehicle eye dropsOTHEROne drop in the study eye 3 times daily for 23 days
Nepafenac Vehicle 0.3%OTHERNepafenac Vehicle 0.3%, one drop in affected eye once daily, for 16 days. An additional drop was administered between 30-120 minutes prior to surgery.
Nepafenac ophthalmic suspension, 0.1% (NEVANAC)DRUG1 drop TID beginning the day before surgery, continuing on the day of surgery and through the first 90 days following surgery.
Prednisolone acetate ophthalmic suspension (OMNIPRED)DRUGOne drop in the study eye 4 times daily (morning, late morning, late afternoon, and bedtime)for two weeks postsurgery.
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Eligibility Criteria

Age Range18 Years to N/A
SexALL
Healthy VolunteersNo

Inclusion Criteria: * Planned cataract extraction by phacoemulsification with implantation of a posterior chamber intraocular lens; * History of Type 1 or 2 diabetes and non-proliferative diabetic retinopathy (NPDR) (mild, moderate, or severe) in the study eye; * Best corrected visual acuity (BCVA)...

Countries:ChinaUnited StatesFrance
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Frequently asked questions about Nepafenac, 0.3%

What is nepafenac, 0.3%?

Nepafenac, 0.3% is an ophthalmic suspension formulation of nepafenac, a small molecule nonsteroidal anti-inflammatory drug. It is being developed by Alcon Inc. (ticker ALC) for eye conditions including cataract surgery, macular edema, and non-proliferative diabetic retinopathy. It is a higher-concentration version of the 0.1% nepafenac ophthalmic suspension.

What is nepafenac, 0.3% used for?

Nepafenac, 0.3% is being studied for cataract, macular edema, and non-proliferative diabetic retinopathy. Clinical trials have evaluated it for ocular pain and inflammation after cataract surgery and for macular edema in patients with non-proliferative diabetic retinopathy undergoing cataract surgery. It is an investigational ophthalmic anti-inflammatory therapy.

What does nepafenac, 0.3% target?

Nepafenac, 0.3% targets PTGS2 (cyclooxygenase-2) and PTGS1 (cyclooxygenase-1). It acts as an inhibitor of these enzymes, which are involved in prostaglandin synthesis and the inflammatory response in ocular tissue. This mechanism underlies its use for pain and inflammation in the eye.

Who makes nepafenac, 0.3%?

Nepafenac, 0.3% is developed by Alcon Inc., which trades under the ticker ALC. Alcon is an ophthalmology-focused pharmaceutical and device company. The 0.1% nepafenac ophthalmic suspension is marketed under the brand name NEVANAC.

What phase is nepafenac, 0.3% in?

Nepafenac, 0.3% is in Phase 3 development. Five clinical trials have been completed, including Phase 3 studies in macular edema and cataract, and no active trials are currently listed. It is an investigational product and is not described as FDA approved in the available development record.

What clinical trials is nepafenac, 0.3% in?

Completed trials include NCT01872611 and NCT01853072, Phase 3 studies of once-daily nepafenac for macular edema in non-proliferative diabetic retinopathy and cataract, and NCT01426854, a Phase 3 study of nepafenac versus placebo for ocular pain and inflammation in cataract. NCT01318499 was a Phase 2 cataract study.

Is nepafenac, 0.3% the same as NEVANAC?

Nepafenac, 0.3% is a higher-concentration ophthalmic suspension of nepafenac, while NEVANAC is the brand name for nepafenac ophthalmic suspension, 0.1%. Both contain the same active ingredient, nepafenac, but at different strengths. Other names include nepafenac ophthalmic suspension 0.1% and nepafenac 1 mg/mL eye drops.