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J GlaucomaMay 20190 citations

Phase 2, Randomized, Dose-finding Studies of Omidenepag Isopropyl, a Selective EP2 Agonist, in Patients With Primary Open-angle Glaucoma or Ocular Hypertension.

Aihara Makoto, Lu Fenghe, Kawata Hisashi, Iwata Akihiro, Liu Kathy, Odani-Kawabata Noriko, Shams Naveed K


AI Summary

Omidenepag isopropyl effectively lowered IOP in glaucoma/ocular hypertension patients, with 0.002% identified as the optimal, well-tolerated dose for further study, offering a new potential treatment option.

Abstract

Unlabelled: PRéCIS:: Three randomized, multicenter studies demonstrated the stable intraocular pressure-lowering effects and tolerability of omidenepag isopropyl in patients with primary open-angle glaucoma and ocular hypertension; 0.002% was identified as the optimal dose for further investigation.

Purpose

The purpose of this study was to assess the safety and efficacy of omidenepag isopropyl, a selective EP2 agonist, and to determine the optimal dose for further investigation.

Patients and methods: Three randomized, controlled, masked, multicenter studies were conducted in United States (study 1, NCT01868126; study 2, NCT02179008) and Japan (study 3, NCT02623738). Patients were randomized to 1 of 7 omidenepag isopropyl concentrations (0.0003%, 0.001%, 0.0012%, 0.0016%, 0.002%, 0.0025%, and 0.003%), latanoprost (0.005%), or placebo, 1 drop once daily for 28 days (studies 1 and 3) or 90 days (study 2). Primary endpoints were the observed mean diurnal intraocular pressure (IOP) and IOP at each time point on the final visit (studies 1 and 2) and change from baseline in mean diurnal IOP at week 4 (study 3).

Results

IOP-lowering effects of omidenepag isopropyl 0.0003% to 0.002% increased dose-dependently. Omidenepag isopropyl 0.002% and 0.0025% resulted in clinically relevant mean diurnal IOP reductions from baseline that were similar to those of latanoprost and superior to placebo (P<0.005). Maximum reductions had already been achieved by week 1, and stable IOP-lowering effects were observed at all postbaseline time points up to 3 months. Most adverse events (AEs) were mild. Conjunctival hyperemia was the most frequently reported AE, the incidence of which increased dose-dependently. The safety profiles of omidenepag isopropyl 0.002% and 0.0025% were similar, with a slightly lower incidence of AEs in the 0.002% group.

Conclusions

Omidenepag isopropyl demonstrated stable IOP-lowering effects and was well tolerated; 0.002% was identified as the optimal dose for phase 3 investigation.


MeSH Terms

AgedAntihypertensive AgentsCorneal PachymetryDose-Response Relationship, DrugDouble-Blind MethodFemaleGlaucoma, Open-AngleGlycineHumansIntraocular PressureMaleMiddle AgedOcular HypertensionOphthalmoscopyPyrazolesPyridinesReceptors, Prostaglandin E, EP2 SubtypeSlit Lamp MicroscopyTonometry, Ocular

Key Concepts5

Omidenepag isopropyl 0.002% and 0.0025% demonstrated clinically relevant mean diurnal intraocular pressure (IOP) reductions from baseline that were similar to those of latanoprost (0.005%) and superior to placebo (P<0.005) in patients with primary open-angle glaucoma or ocular hypertension.

TreatmentRCTRandomized Controlled Trialn=patients randomized to 1 of 7 omidene…Ch28Ch29Ch31

The IOP-lowering effects of omidenepag isopropyl at concentrations ranging from 0.0003% to 0.002% increased dose-dependently in patients with primary open-angle glaucoma or ocular hypertension.

MechanismRCTRandomized Controlled Trialn=patients randomized to 1 of 7 omidene…Ch28Ch29Ch31

Maximum reductions in intraocular pressure with omidenepag isopropyl were achieved by week 1, and stable IOP-lowering effects were observed at all postbaseline time points up to 3 months in patients with primary open-angle glaucoma or ocular hypertension.

TreatmentRCTRandomized Controlled Trialn=patients randomized to 1 of 7 omidene…Ch28Ch29Ch31

Most adverse events (AEs) associated with omidenepag isopropyl were mild, with conjunctival hyperemia being the most frequently reported AE, and its incidence increased dose-dependently in patients with primary open-angle glaucoma or ocular hypertension.

TreatmentRCTRandomized Controlled Trialn=patients randomized to 1 of 7 omidene…Ch28Ch29Ch31

The safety profiles of omidenepag isopropyl 0.002% and 0.0025% were similar, with a slightly lower incidence of adverse events in the 0.002% group, leading to the identification of 0.002% as the optimal dose for further investigation in patients with primary open-angle glaucoma or ocular hypertension.

TreatmentRCTRandomized Controlled Trialn=patients randomized to 1 of 7 omidene…Ch28Ch29Ch31

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