An Expert Report on the Ophthalmic Non-Steroidal Anti-Inflammatory Drug: Nepafenac

Executive Summary

Nepafenac (DrugBank ID: DB06802) is a topical non-steroidal anti-inflammatory drug (NSAID) distinguished by its unique prodrug structure and its critical role in contemporary ophthalmic care. Primarily indicated for the prevention and treatment of pain and inflammation associated with cataract surgery, Nepafenac represents a sophisticated approach to ocular drug delivery. This report provides a comprehensive analysis of its chemical properties, pharmacological mechanisms, clinical performance, safety profile, and regulatory history.

The core of Nepafenac's therapeutic value lies in its design as a prodrug. Following topical administration, the lipophilic Nepafenac molecule rapidly penetrates the cornea and is bioactivated by intraocular hydrolases into its active metabolite, amfenac. This conversion occurs preferentially within the target tissues of the anterior and posterior segments, including the iris, ciliary body, and retina. Amfenac is a potent, non-selective inhibitor of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) enzymes, thereby blocking the synthesis of prostaglandins, which are key mediators of ocular inflammation and pain. This mechanism of targeted bio-localization not only concentrates the therapeutic effect where it is needed most but also significantly enhances its safety profile, particularly regarding the ocular surface, when compared to NSAIDs administered in their active form.