[Ocular effects of topical instillation of UF-021 ophthalmic solution in healthy volunteers]

Phase I studies, as divided into two stages, were conducted in healthy volunteers with the ophthalmic solution of UF-021, a novel prostaglandin metabolite-related compound, that was reported to exhibit potent intraocular pressure (IOP)-reducing activity in various species of animals. In the first stage, the vehicle as well as UF-021 ophthalmic solutions at concentration of 0.03%, 0.06% and 0.09% were applied topically to the eyes of 8 healthy volunteers to determine their respective effects through observations on the IOP, and local ocular and systemic side effects. In the second stage, 2 dosages of UF-021 ophthalmic solution, 0.06% and 0.12%, were applied topically to 11 healthy volunteers to investigate the IOP-reducing activities and local ocular side effects. The results revealed that ophthalmic solutions of UF-021 at concentrations ranging from 0.03% to 0.12% reduced IOP in a dose-dependent manner with neither systemic nor local ocular controversial side effects at those dosage levels. In summary, UF-021 ophthalmic solutions, when administered to healthy volunteers through single instillation, reduced IOP significantly without causing any side effects.