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1 General aspects (0)   1.1 Epidemiology (6)   1.2 Population genetics (0)   1.3 Pathogenesis (1)   1.4 Quality of life (11)   1.5 Glaucomas as cause of blindness (4)   1.6 Prevention and screening (4) 2 Anatomical structures in glaucoma (0)   2.1 Conjunctiva (3)   2.2 Cornea (10)   2.3 Sclera (4)   2.4 Anterior chamber angle (6)   2.5 Meshwork (0)     2.5.1 Trabecular meshwork (7)     2.5.2 Schlemms canal (2)     2.5.3 Scleral outlet channels (1)   2.6 Aqueous humor dynamics (0)     2.6.1 Production (0)     2.6.2 Outflow (0)       2.6.2.1 Trabecular meshwork (0)       2.6.2.2 Uveoscleral (0)     2.6.3 Compostion (6)   2.7 Episcleral veins and venous pressure (0)   2.8 Iris (6)   2.9 Ciliary body (1)   2.10 Lens (0)   2.11 Vitreous body (0)   2.12 Choroid, peripapillary choroid, peripapillary atrophy (9)   2.13 Retina and retinal nerve fibre layer (29)   2.14 Optic disc (21)   2.15 Optic nerve (0)   2.16 Chiasma and retrochiasmal central nervous system (3)   2.17 Stem cells (0)   2.20 Other (0) 3 Laboratory methods (0)   3.1 Microscopy (3)   3.2 Electron microscopy (1)   3.3 Immunohistochemistry (4)   3.4 Molecular genetics (0)     3.4.1 Linkage studies (0)     3.4.2 Gene studies (13)   3.5 Molecular biology incl. 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Without tube implant (15)     12.8.2 With tube implant or other drainage devices (19)     12.8.3 Non-perforating (3)     12.8.4 Using laser (0)     12.8.5 Other (0)     12.8.10 Woundhealing antifibrosis (10)     12.8.11 Complications, endophthalmitis (8)   12.9 Trabeculotomy, goniotomy (8)   12.10 Cyclodestruction (2)   12.11 Cyclodialysis (1)   12.12 Cataract extraction (0)     12.12.1 Intracapsular (0)     12.12.2 Extracapsular (0)     12.12.3 Phacoemulsification (5)   12.14 Combined cataract extraction and glaucoma surgery (0)     12.14.1 Intracapsular (0)     12.14.2 Extracapsular (0)     12.14.3 Phacoemulsification (3)   12.15 Capsulotomy (0)   12.16 Vitrectomy (3)   12.17 Anesthesia (0)   12.20 Other (1) 13 Therapeutic prognosis and outcome (0)   13.1 Prognostic factors (0)   13.2 Outcome (0)     13.2.1 IOP (0)     13.2.2 Visual field (0)       13.2.2.1 Progression (0)       13.2.2.2 Improvement (0)     13.2.3 Other (0) 14 Costing studies; pharmacoeconomics (4) 15 Miscellaneous (23)

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Abstract #78100 Published in IGR 19-4

Identification of a Selective, Non-Prostanoid EP2 Receptor Agonist for the Treatment of Glaucoma: Omidenepag and its Prodrug Omidenepag Isopropyl

Iwamura R; Iwamura R; Tanaka M; Okanari E; Kirihara T; Odani-Kawabata N; Shams N; Yoneda K
Journal of Medicinal Chemistry 2018; 61: 6869-6891

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EP2 receptor agonists are expected to be effective ocular hypotensive agents; however, it has been suggested that agonism to other EP receptor subtypes may lead to undesirable effects. Through medicinal chemistry efforts, we identified a scaffold bearing a (pyridin-2-ylamino)acetic acid moiety as a promising EP2-selective receptor agonist. (6-((4-(Pyrazol-1-yl)benzyl)(pyridin-3-ylsulfonyl)aminomethyl)pyridin-2-ylamino)acetic acid 13ax (omidenepag, OMD) exerted potent and selective activity toward the human EP2 receptor (h-EP2). Low doses of omidenepag isopropyl (OMDI), a prodrug of 13ax, lowered intraocular pressure (IOP) in ocular normotensive monkeys. OMDI was selected as a clinical candidate for the treatment of glaucoma.

Pharmaceuticals Research Laboratory , UBE Industries, Ltd. , 1978-5 Kogushi , Ube , Yamaguchi 755-8633 , Japan.

Full article

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Classification:

11.4 Prostaglandins (Part of: 11 Medical treatment)
11.14 Investigational drugs; pharmacological experiments (Part of: 11 Medical treatment)
5.2 Primates (Part of: 5 Experimental glaucoma; animal models)
3.8 Pharmacology (Part of: 3 Laboratory methods)

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