Nepafenac

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Cat Number

INT78281728

CAS Number

78281-72-8

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Product Detail Description Advanced Innovations Customer Q&A

CAS Number

78281-72-8

EINECS

200-001-8

Synonyms

2-(2-amino-3-benzoyl-phenyl)acetamide;2-Amino-3-benzoylbenzeneacetamide

Molecular Formula

C15H14N2O2

Molecular Weight

254.28

Smiles

C1(CC(N)=O)=CC=CC(C(=O)C2=CC=CC=C2)=C1N

Melting Point

177-181℃

Boiling Point

563℃

Relative Density

1.25

General Description

Nepafenac is a prodrug ophthalmic NSAID (non-steroidal anti-inflammatory drug) designed for topical ocular administration. It is an amide derivative of amfenac (a potent cyclooxygenase inhibitor) linked to a 2-aminoethanesulfonyl group that increases its corneal penetration. Upon reaching the intraocular tissues, nepafenac is hydrolyzed by ocular hydrolases to the active metabolite amfenac, which inhibits both COX-1 and COX-2 enzymes.

Mechanism of Action

Nepafenac acts as a prodrug that penetrates the cornea more efficiently than amfenac due to its higher lipophilicity. Once inside the eye (cornea, aqueous humor, iris, ciliary body), it is hydrolyzed by ocular hydrolases (including cyclooxygenase itself) to the active amfenac, which non-selectively inhibits cyclooxygenase 1 and 2 (COX-1/COX-2). By blocking prostaglandin synthesis, it reduces inflammation, pain, and macular edema following cataract surgery.

Application

Nepafenac is indicated for the treatment of pain and inflammation associated with cataract surgery (postoperative ocular inflammation), and for the reduction in risk of macular edema associated with cataract surgery in diabetic patients.

Nepafenac is an effective NSAID for ocular inflammation after cataract surgery, but the suspension causes patient compliance issues (irritation, blurred vision). To overcome this, nepafenac eye drops were developed using hydroxypropyl-β-cyclodextrin for solubilization, sodium hyaluronate for mucoadhesion, and a preservative-free carbomer base. Eleven formulations were tested for viscosity, mucoadhesion, drug release, and corneal permeability. Two promising formulations underwent ex vivo testing on porcine eyes with RAMAN mapping. One formulation showed better bioavailability than the suspension, while another containing only 60% of the original dose was ex vivo equivalent, offering improved patient compliance.

Fig. 1 Nepafenac containing eye drops were prepared using hydroxypropyl-β-cyclodextrin. (Vincze A.; et al. 2023)

References

Vincze A, et al. Cyclodextrin-enabled nepafenac eye drops with improved absorption open a new therapeutic window. Carbohydrate Polymers, 2023, 310: 120717.

What is the recommended storage condition for Nepafenac?

It should be stored at controlled room temperature in a well-sealed container, protected from moisture and direct light, to maintain its chemical integrity throughout the shelf life.

What documentation is provided with each batch of Nepafenac?

Each batch is accompanied by a Certificate of Analysis (COA) covering identity, potency, and relevant purity tests. Safety Data Sheets (SDS) are available upon request.

What scale of supply is available for Nepafenac for pilot or commercial synthesis?

Supply is available from laboratory research scale through multi-kilogram pilot quantities. Commercial-scale supply can be discussed based on projected demand.

Can Nepafenac be provided with custom specifications for synthetic applications?

Custom specifications including adjusted particle size, solvent residue limits, or additional purity testing can be arranged for qualified customers with defined requirements.

What is the minimum order quantity (MOQ) for Nepafenac?

Flexible MOQ options are available to support both early-stage research and large-scale manufacturing needs. Our team can tailor order quantities to match your specific requirements.