Drug intelligence / Profile preview

ketorolac + nepafenac

Development stage
Unknown
Lead developer
Allergan
Modality
Small Molecules
Administration
Ophthalmic, Topical
01

Overview

Ketorolac + nepafenac is a combination of two non-steroidal anti-inflammatory drugs (NSAIDs) used primarily in ophthalmology for the management of pain and inflammation, especially following cataract surgery. Ketorolac is a non-selective NSAID that inhibits both cyclooxygenase 1 (COX-1) and cyclooxygenase 2 (COX-2), reducing prostaglandin synthesis to provide analgesic and anti-inflammatory effects. Nepafenac is an ophthalmic NSAID prodrug that, after corneal penetration, is rapidly converted by intraocular hydrolases to amfenac—a potent inhibitor of COX-1 and COX-2—resulting in suppression of prostaglandin synthesis within ocular tissues. Both agents are used topically as eye drops to control post-operative ocular inflammation and pain; studies suggest similar efficacy for both drugs in controlling inflammation, with nepafenac showing better tolerability regarding conjunctival hyperemia and discomfort[1][3][4][5][6][8].

Other names
ketorolac tromethamineamfenac amide
02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)PGHS-1 (Prostaglandin G/H Synthase 1)

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