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December 1988

Local Tolerance and Activity of MK-927, a Novel Topical Carbonic Anhydrase Inhibitor

Author Affiliations

From the Clinical Research Department, Merck Sharp & Dohme Research Laboratories, West Point, Pa (Dr Lippa); the Department of Ophthalmology, Technical University of Munich (Drs von Denffer and Hofmann); and the Clinical Pharmacology Department, Merck Sharp & Dohme Research Laboratories, Rahway, NJ (Dr Brunner-Ferber).

Arch Ophthalmol. 1988;106(12):1694-1696. doi:10.1001/archopht.1988.01060140866029

• A three-dose, randomized, double-masked, parallel, placebo-controlled ocular tolerance study was undertaken in 12 healthy, normal volunteers with the water-soluble, topical carbonic anhydrase inhibitor MK-927. To our knowledge, this constitutes the first administration of MK-927 to humans. Ten subjects received three drops of 2% MK-927 ophthalmic solution and two subjects received three drops of placebo (vehicle) in one randomly selected eye. Local tolerance of 2% MK-927 was acceptable and supports further clinical trials in patients. Significant intraocular pressure (IOP)-lowering activity was noted when comparing IOP four hours after first dose with that 20 hours predose in the treated eye of subjects receiving MK-927 (mean percent change in IOP, −29.7%; mean change in IOP, −4.6 mm Hg) as opposed to the same comparison for the contralateral, untreated eye (−7.2% and −1.3 mm Hg, respectively). In the two subjects treated with placebo, IOP-lowering activity was not seen in either the placebo-treated eye (−0.4%) or the contralateral, untreated eye (+3.1%).

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