Omidenepag

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Omidenepag
Names
Trade namesEybelis, Omlonti
Other namesUR-7276, DE-117, Omidenepag isopropyl (JAN JP)
  • Propan-2-yl 2-[[6-[[(4-pyrazol-1-ylphenyl)methyl-pyridin-3-ylsulfonylamino]methyl]pyridin-2-yl]amino]acetate
Clinical data
Drug classProstaglandin E2 (EP2) receptor activator[1]
Main usesOcular hypertension including glaucoma[1]
Side effectsSensitivity to light, blurry vision, eye redness, headache, eye pain[1]
Routes of
use
Eye drop
Legal
Legal status
Chemical and physical data
FormulaC26H28N6O4S
Molar mass520.61 g·mol−1
3D model (JSmol)
  • CC(C)OC(=O)CNC1=CC=CC(CN(CC2=CC=C(C=C2)N2C=CC=N2)S(=O)(=O)C2=CC=CN=C2)=N1
  • InChI=1S/C23H22N6O4S/c30-23(31)15-25-22-6-1-4-19(27-22)17-28(34(32,33)21-5-2-11-24-14-21)16-18-7-9-20(10-8-18)29-13-3-12-26-29/h1-14H,15-17H2,(H,25,27)(H,30,31)
  • Key:YHGSTSNEOJUIRN-UHFFFAOYSA-N

  • InChI=1S/C26H28N6O4S/c1-20(2)36-26(33)17-28-25-8-3-6-22(30-25)19-31(37(34,35)24-7-4-13-27-16-24)18-21-9-11-23(12-10-21)32-15-5-14-29-32/h3-16,20H,17-19H2,1-2H3,(H,28,30)
  • Key:VIQCWEGEHRBLAC-UHFFFAOYSA-N

Omidenepag, sold under the brand name Eybelis among others, is a medication used to treat ocular hypertension including glaucoma.[1][3] It is used as an eye drop.[1]

Common side effects include sensitivity to light, blurry vision, eye redness, headache, and eye pain.[1] Other side effects may include changes to the eyelashes and macular edema.[1] It is a relatively selective prostaglandin E2 (EP2) receptor activator.[1]

Omidenepag was approved for medical use in Japan in 2018,[3] and the United States in 2022.[1] It is not currently in the approval process in either Europe or the United Kingdom as of 2022.[4]

Medical uses

Omidenepag is indicated for the treatment of glaucoma and ocular hypertension.[1][3]

Dosage

It comes as a 0.002% (0.02 mg/mL) solution.[1] It is used as one drop once per day.[1]

Side effects

The most common side effects are conjunctival hyperemia and macular edema, including cystoid macular edema.[3]

Pharmacology

Omidenepag isopropyl is a prodrug that is converted by hydrolysis of its isopropyl ester to the active metabolite omidenepag.[5] Omidenepag is a selective prostaglandin E2 receptor agonist.[6][7]

History

Omidenepag was developed by Ube Industries and Santen Pharmaceutical.[3]

References

  1. 1.00 1.01 1.02 1.03 1.04 1.05 1.06 1.07 1.08 1.09 1.10 1.11 1.12 "Omlonti- omidenepag isopropyl solution/ drops". DailyMed. 30 September 2022. Archived from the original on 16 October 2022. Retrieved 16 October 2022.
  2. "Drug Approval Package: Omlonti". U.S. Food and Drug Administration (FDA). 20 October 2022. Archived from the original on 4 December 2022. Retrieved 4 December 2022.
  3. 3.0 3.1 3.2 3.3 3.4 3.5 Duggan S (December 2018). "Omidenepag Isopropyl Ophthalmic Solution 0.002%: First Global Approval". Drugs. 78 (18): 1925–1929. doi:10.1007/s40265-018-1016-1. PMID 30465134. S2CID 53721056.
  4. "Omidenepag isopropyl". SPS - Specialist Pharmacy Service. 30 September 2022. Archived from the original on 24 October 2022. Retrieved 16 December 2022.
  5. "Omidenepag isopropyl". DrugCentral. Division of Translational Informatics at University of New Mexico. Archived from the original on 8 January 2022. Retrieved 8 January 2022.
  6. Kirihara T, Taniguchi T, Yamamura K, Iwamura R, Yoneda K, Odani-Kawabata N, et al. (January 2018). "Pharmacologic Characterization of Omidenepag Isopropyl, a Novel Selective EP2 Receptor Agonist, as an Ocular Hypotensive Agent". Investigative Ophthalmology & Visual Science. 59 (1): 145–153. doi:10.1167/iovs.17-22745. PMID 29332128.
  7. Ida Y, Hikage F, Umetsu A, Ida H, Ohguro H (September 2020). "Omidenepag, a non-prostanoid EP2 receptor agonist, induces enlargement of the 3D organoid of 3T3-L1 cells". Scientific Reports. 10 (1): 16018. Bibcode:2020NatSR..1016018I. doi:10.1038/s41598-020-72538-x. PMC 7524797. PMID 32994409.

External links

External sites:
Identifiers: