Omidenepagisopropyl是选择性的，非前列腺素的EP2受体激动剂。Omidenepagisopropyl在角膜穿透过程中转化为活性产品Omidenepag，Omidenepag是高度选择性的EP2受体激动剂。Omidenepagisopropyl对EP1，EP2和FP受体有弱亲和力。Omidenepagisopropyl可以降低眼内压(IOP)，有潜力用于青光眼的研究。
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug[1][2].
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.
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