A Comprehensive Monograph on Difluprednate: Pharmacology, Clinical Application, and Regulatory Status

1.0 Executive Summary

Difluprednate is a potent, second-generation synthetic corticosteroid developed for topical ophthalmic use. It is distinguished by its robust anti-inflammatory activity, which is a direct result of targeted chemical modifications to the prednisolone structure, including fluorination at the C6 and C9 positions. This design significantly enhances its affinity for the glucocorticoid receptor, the primary mediator of its therapeutic effects. The drug is formulated as a 0.05% oil-in-water emulsion, commercially known as Durezol®, a vehicle designed to overcome the active ingredient's lipophilicity and optimize its penetration into ocular tissues.

Clinically, Difluprednate is indicated for the treatment of inflammation and pain following ocular surgery and for the management of endogenous anterior uveitis. Its efficacy in these conditions is well-supported by pivotal clinical trials, which have demonstrated rapid and effective resolution of inflammatory signs and symptoms. The pharmacokinetic profile of Difluprednate is highly favorable for ocular therapy; it functions as a prodrug that is rapidly converted to its active metabolite within the eye, followed by local inactivation, a process that maximizes therapeutic activity at the target site while minimizing systemic absorption and exposure.