Omarigliptin

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.

Omarigliptin
Clinical data
Other namesMK-3102
Routes of
administration		Oral
ATC code
  • None
Legal status
Legal status
  • Developing
Identifiers
IUPAC name
  • (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)oxan-3-amine
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.207.924
Chemical and physical data
FormulaC17H20F2N4O3S
Molar mass398.43 g·mol−1
3D model (JSmol)
SMILES
  • 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

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. Merck & Co., Inc. 95 (S1): 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


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