Local tolerance and activity of MK-927, a novel topical carbonic anhydrase inhibitor

Arch Ophthalmol. 1988 Dec;106(12):1694-6. doi: 10.1001/archopht.1988.01060140866029.

Abstract

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%).

Publication types

  • Clinical Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Carbonic Anhydrase Inhibitors / pharmacology*
  • Clinical Trials as Topic
  • Double-Blind Method
  • Eye / blood supply
  • Eye / drug effects*
  • Humans
  • Hyperemia / chemically induced
  • Intraocular Pressure / drug effects*
  • Male
  • Ophthalmic Solutions
  • Placebos
  • Random Allocation
  • Sulfonamides / adverse effects
  • Sulfonamides / pharmacology*
  • Thiophenes / adverse effects
  • Thiophenes / pharmacology*

Substances

  • Carbonic Anhydrase Inhibitors
  • Ophthalmic Solutions
  • Placebos
  • Sulfonamides
  • Thiophenes
  • sezolamide