The ocular hypotensive effect of an ophthalmic solution of S-1033, a new prostaglandin analogue was tested in double-masked fashion, in normal human volunteers. The single ocular instillation of a 0.3% solution of S-1033 in 6 normal volunteers showed a statistically significant intraocular pressure (IOP) reduction at 1,2, and 8 hours after application when compared to that of the contralateral eyes. The magnitude of IOP reduction was about 2 to 3 mmHg (from 14 to 11 mmHg at maximum). With a 0.4% solution, an IOP reduction similar to that induced by 0.3% was observed in the 6 normal volunteers. When 0.3% S-1033 was applied twice a day for 8 consecutive days in another 6 normal human volunteers, the IOP reduction observed on the 1st day was maintained during the observation period with an average IOP reduction of about 2 mmHg. Neither ocular nor systemic side effects attributable to S-1033 application were observed in these studies. From these results, we conclude that S-1033 merits worth further investigation as a possible antiglaucoma agent.