Nepafenac

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Cat Number

INT78281728

CAS Number

78281-72-8

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Product Detail Description Scientific Support Customer Q&A

CAS Number

78281-72-8

EINECS

682-241-7

Storage

Store at room temperature

Synonyms

2-(2-Amino-3-benzoylphenyl)acetamide; Nevanac; 2-Amino-3-benzoylbenzeneacetamide; AHR-9434; Ilevro; AL-6515

Molecular Formula

C15H14N2O2

Molecular Weight

254.28

Smiles

C1=CC=C(C=C1)C(=O)C2=CC=CC(=C2N)CC(=O)N

Appearance

Light yellow to yellow solid

General Description

Nepafenac is a topical nonsteroidal anti-inflammatory drug (NSAID) formulated as an ophthalmic suspension. It is a prodrug designed with enhanced corneal penetration to target intraocular tissues effectively. Unlike conventional topical NSAIDs, its unique structure allows for rapid bioconversion to its active amine metabolite following ocular administration.

Mechanism of Action

Following penetration through the cornea, nepafenac undergoes hydrolysis by intraocular amidases to form amfenac, a potent inhibitor of cyclooxygenase (COX-1 and COX-2) enzymes. This inhibition blocks the synthesis of prostaglandins, which are key mediators of inflammation, miosis, and increased intraocular pressure. The prodrug approach facilitates targeted delivery to the iris, ciliary body, and retina.

Application

It is approved for the treatment of pain and inflammation associated with cataract surgery, as well as for reducing the risk of postoperative macular edema in diabetic patients. It is also utilized off-label for the management of non-infectious uveitis and as a prophylactic agent for intraoperative miosis. The suspension formulation allows for once-daily or twice-daily dosing due to its sustained ocular residence time.

A pilot study directly compared bromfenac 0.07% solution with nepafenac 0.3% suspension using identical once‑daily dosing plus an extra preoperative dose in 49 cataract surgery patients. At postoperative day 15, the primary endpoint (summed ocular inflammation score = 0) was achieved in 57.1% of bromfenac‑treated patients versus 50.0% of nepafenac‑treated patients (P=0.6318). However, at days 3 and 8, significantly more bromfenac patients had resolved inflammation. Visual acuity and retinal thickness outcomes were similar, and both agents were well tolerated. The authors conclude that once‑daily bromfenac 0.07% provides overall anti‑inflammatory effects comparable to nepafenac 0.3% but may act faster under identical dosing regimens.

Fig. 1 Flow chart of patient disposition. (Silverstein SM, 2019)

References

Silverstein SM. Bromfenac Ophthalmic Solution 0.07% Versus Nepafenac Ophthalmic Suspension 0.3% for Post-Cataract Surgery Inflammation: A Pilot Study of Identical Dosing Regimens with Pre-Surgical "Pulse" Dose. Ophthalmol Ther. 2019; 8(4):577-587.

Does Nepafenac require protection from light during long-term storage?

Yes, it is highly photosensitive. Degradation upon light exposure is rapid. It must be stored in light-resistant containers and handled under subdued light.

What is the recommended storage temperature for Nepafenac?

Store at controlled room temperature, between 20°C and 25°C. Refrigeration is not required but may be used if the container is tightly sealed to prevent moisture condensation.

Is Nepafenac stable in ophthalmic suspension formulations?

The API is stable in the solid state. For formulated suspensions, we provide compatibility data and recommend pH control (typically around 7.0) to maintain stability.

How is the degradation product amfenac monitored during stability studies?

Amfenac, the active metabolite, is also the primary hydrolysis product. We use a validated HPLC method to monitor its formation and ensure levels are controlled.