Omarigliptin

Chemical compound
  • None
Legal statusLegal status
  • Developing
Identifiers
  • (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine
CAS Number
  • 1226781-44-7
PubChem CID
  • 46209133
ChemSpider
  • 28424182
UNII
  • CVP59Q4JE1
KEGG
  • D10317
ChEMBL
  • ChEMBL2105762
CompTox Dashboard (EPA)
  • DTXSID70153678 Edit this at Wikidata
ECHA InfoCard100.207.924 Edit this at WikidataChemical and physical dataFormulaC17H20F2N4O3SMolar mass398.43 g·mol−13D model (JSmol)
  • Interactive image
  • CS(=O)(=O)n1cc2c(n1)CN(C2)[C@@H]3C[C@@H]([C@H](OC3)c4cc(ccc4F)F)N
InChI
  • InChI=1S/C17H20F2N4O3S/c1-27(24,25)23-7-10-6-22(8-16(10)21-23)12-5-15(20)17(26-9-12)13-4-11(18)2-3-14(13)19/h2-4,7,12,15,17H,5-6,8-9,20H2,1H3/t12-,15+,17-/m1/s1
  • Key:MKMPWKUAHLTIBJ-ISTRZQFTSA-N

Omarigliptin (MK-3102) is a potent, long-acting oral antidiabetic drug of the DPP-4 inhibitor class used for once-weekly treatment of type 2 diabetes and currently under development by Merck & Co.[1] It inhibits DPP-4 to increase incretin levels (GLP-1 and GIP),[2][3][4] which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying and decreases blood glucose levels.

History

Marizev (omarigliptin) 25 mg and 12.5 mg tablets were approved by Japan's Pharmaceuticals and Medical Devices Agency (PMDA) on 28th Sept 2015. Japan was the first country to have approved omarigliptin.[5] However Merck has announced that the company will not submit marketing application in the US and Europe.[6]

References

  1. ^ Tatosian DA, Glasgow S, Caceres M, Grenier J, DeGroot B, Ward T, Johnson-Levonas A, George L, Lasseter KC, Marbury TC, Kauh E (March 2014). "Pharmacokinetics of omarigliptin (MK‐3102), a once weekly dipeptidyl peptidase‐IV (DPP‐4) inhibitor, in patients with renal impairment" (PDF). Clin Pharmacol Ther. 95 (S1). Merck & Co., Inc.: S90. Retrieved 20 September 2015.
  2. ^ McIntosh CH, Demuth HU, Pospisilik JA, Pederson R (June 2005). "Dipeptidyl peptidase IV inhibitors: how do they work as new antidiabetic agents?". Regulatory Peptides. 128 (2): 159–65. doi:10.1016/j.regpep.2004.06.001. PMID 15780435. S2CID 9151210.
  3. ^ Behme MT, Dupré J, McDonald TJ (April 2003). "Glucagon-like peptide 1 improved glycemic control in type 1 diabetes". BMC Endocrine Disorders. 3 (1): 3. doi:10.1186/1472-6823-3-3. PMC 154101. PMID 12697069.
  4. ^ Dupre J, Behme MT, Hramiak IM, McFarlane P, Williamson MP, Zabel P, McDonald TJ (June 1995). "Glucagon-like peptide I reduces postprandial glycemic excursions in IDDM". Diabetes. 44 (6): 626–30. doi:10.2337/diabetes.44.6.626. PMID 7789625.
  5. ^ "Merck MARIZEV Once-Weekly DPP-4 Inhibitor For Type2 Diabetes Approved In Japan". NASDAQ. 28 September 2015. Retrieved 29 September 2015.
  6. ^ "Merck Provides Update on Filing Plans for Omarigliptin, an Investigational DPP-4 Inhibitor for Type 2 Diabetes". Merck Sharp & Dohme Corp. April 8, 2016.

See also

  • v
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  • e
Oral diabetes medication, insulins and insulin analogs, and other drugs used in diabetes (A10)
fast-acting
short-acting
long-acting
ultra-long-acting
inhalable
  • Exubera‡
  • Afrezza
Non-insulins
Insulin sensitizers
Biguanides
TZDs/"glitazones" (PPAR)
Dual PPAR agonists
Amylin analogs and DACRAs
Secretagogues
K+ATP
Sulfonylureas
Meglitinides/"glinides"
GLP-1 receptor agonists
GLP1 poly-agonist peptides
DPP-4 inhibitors/"gliptins"
Other
Aldose reductase inhibitors
Alpha-glucosidase inhibitors
SGLT2 inhibitors/"gliflozins"
Other
Combinations
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  • e
Corporate directors
Subsidiaries
Products
Schering-Plough
Facilities
Publications


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