It has previously been reported that a prototypical compound (AGN 211377), which blocks pro-inflammatory prostanoid receptors (DP, DP, EP, EP FP, TP) and leaves open IP and EP receptors so that their anti-inflammatory properties could be exerted, produced superior inhibitory effects on cytokine release from human macrophages compared to cyclooxygenase (COX) inhibitors. This favorable activity profile translated into animal studies, with AGN 211377 exceeding the level of inhibition afforded by COX inhibition. AGN 211377 was not, however, a practical drug candidate, having poor bioavailability and cost of goods concerns.
View Article and Find Full Text PDFJ Ocul Pharmacol Ther
October 2019
Purpose: (1) To determine ketorolac concentrations in selected ocular tissues following the intracameral administration of phenylephrine and ketorolac injection 1%/0.3% (OMIDRIA) delivered in irrigation solution during lens replacement surgery in beagle dogs. (2) To compare the ketorolac initial dose and resultant concentrations from the above study to those achieved in aqueous and vitreous by topical administration in patients undergoing cataract surgery or vitrectomy, respectively.
View Article and Find Full Text PDFJ Ocul Pharmacol Ther
June 2018
Introduction: We compared the prostaglandin E(2) (PGE(2)) inhibition of three topical nonsteroidal antiinflammatory drugs (NSAIDs): ketorolac 0.45%, bromfenac 0.09%, and nepafenac 0.
View Article and Find Full Text PDFObjective: To compare the peak to-aqueous penetration of three nonsteroidal anti-inflammatory drugs: ketorolac tromethamine 0.45%, bromfenac 0.09%, nepafenac 0.
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