Omidenepag isopropyl

Omidenepag Isopropyl (DE-117, OMDI) is the prodrug of Omidenepag, which is a potent, selective agonist human EP2 receptor; demonstrates excellent IOP-lowering activities following ocular administration in ocular normotensive monkeys, Omidenepag Isopropyl (OMDI) is a clinical candidate for the treatment of glaucoma. Other Indication Preregistration

Research Areas >> Others

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

EP2

Omidenepag isopropyl at 0.0001%, 0.001%, or 0.01%, Xalatan, or vehicle was topically administered to one eye in ocular normotensive monkeys. IOP change after drug administration was compared to the predosing baseline value established on day 1. Omidenepag isopropyl also shows significant and dose-dependent IOP-lowering effects at doses of 0.0001%, 0.001%, and 0.01% in ocular normotensive monkeys, with mean maximal IOP reductions of 2.4 ± 0.6, 7.6 ± 1.7, and 13.3 ± 1.2 mm Hg at each tested concentration, respectively. The significant decreases in IOP for 0.001% and 0.01% OMDI at time 0 of day 7. Omidenepag isopropyl is hydrolyzed in the eye to Omidenepag (OMD), an EP2 receptor agonist , with a significant ocular hypotensive effect in both ocular normotensive and hypertensive animal models[1]. In ocular hypertensive monkeys finds that Omidenepag isopropyl lowers IOP by increasing both trabecular outflow facility and uveoscleral outflow[2].

[1]. Kirihara T, et al. Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent. Invest Ophthalmol Vis Sci. 2018 Jan 1;59(1):145-153.

[2]. Fuwa M, et al. Effects of a Novel Selective EP2 Receptor Agonist, Omidenepag Isopropyl, on Aqueous Humor Dynamics in Laser-Induced Ocular Hypertensive Monkeys. J Ocul Pharmacol Ther. 2018 Sep;34(7):531-537.