Omarigliptin

Omarigliptin
Clinical data

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
Synonyms	MK-3102
CAS Number	1226781-44-7
PubChem (CID)	46209133
ChemSpider	28424182
UNII	CVP59Q4JE1
KEGG	D10317
ChEMBL	CHEMBL2105762
Chemical and physical data
Formula	C₁₇H₂₀F₂N₄O₃S
Molar mass	398.427506 g/mol
3D model (Jmol)	Interactive image
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

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

↑ "Pharmacokinetics of Omarigliptin (Mk-3102), A Once-Weekly Dipeptidyl Peptidase-IV (DPP-4) Inhibitor, in Patients With Renal Impairment" (PDF). Merck & Co., Inc. Retrieved 20 September 2015.
↑ McIntosh, C; Demuth, H; Pospisilik, J; Pederson, R (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.
↑ Behme, Margaret T; Dupré, John; McDonald, Thomas J (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.
↑ Dupre, J.; Behme, M. T.; Hramiak, I. M.; McFarlane, P.; Williamson, M. P.; Zabel, P.; McDonald, T. J. (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.
↑ "Merck MARIZEV Once-Weekly DPP-4 Inhibitor For Type2 Diabetes Approved In Japan". NASDAQ. 28 September 2015. Retrieved 29 September 2015.
↑ http://www.mercknewsroom.com/news/company-statements/merck-provides-update-filing-plans-omarigliptin-investigational-dpp-4-inhibi

Biguanides	Buformin^‡ Metformin^# Phenformin^‡

TZDs/"glitazones" (PPAR)	Ciglitazone^§ Darglitazone^§ Englitazone^§ Lobeglitazone Netoglitazone^§ Pioglitazone Rivoglitazone^† Rosiglitazone Troglitazone^‡

Dual PPAR agonists	Aleglitazar^† Muraglitazar^§ Saroglitazar Tesaglitazar^§

Secretagogues

K⁺_ATP

Sulfonylureas	1st generation: Acetohexamide Carbutamide Chlorpropamide Glycyclamide Metahexamide Tolazamide Tolbutamide 2nd generation: Glibenclamide (glyburide)^# Glibornuride Glicaramide Gliclazide Glimepiride Glipizide Gliquidone Glisoxepide Glyclopyramide

Meglitinides/"glinides"	Mitiglinide Nateglinide Repaglinide

GLP-1 agonists

DPP-4 inhibitors/"gliptins"

Free fatty acid receptor 1 (GPR40)

Fasiglifam^†

Analogs/other insulins

fast-acting (Insulin aspart
Insulin glulisine
Insulin lispro)
short-acting (Regular insulin)
long-acting (Insulin detemir
Insulin glargine
NPH insulin)
ultra-long-acting (Insulin degludec)
inhalable (Exubera^‡
Afrezza)

Other

Aldose reductase inhibitors	Epalrestat Fidarestat^§ Ranirestat^† Tolrestat^‡ Zenarestat^§

Alpha-glucosidase inhibitors	Acarbose Miglitol Voglibose

Amylin analog	Pramlintide

Sodium glucose transporter (SGLT2) inhibitors/"gliflozins"	Canagliflozin Dapagliflozin Empagliflozin Ipragliflozin Remogliflozin^§ Sergliflozin^§ Tofogliflozin^†

Other	Benfluorex^‡ Bromocriptine

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

Merck & Co., Inc.

Corporate directors:	Richard Clark Johnnetta Cole William Harrison William Kelley Rochelle Lazarus Thomas Shenk Anne Tatlock Samuel Thier Wendell Weeks Peter Wendell

Products:	Alendronate Aprepitant Ertapenem Ezetimibe Ezetimibe/simvastatin Finasteride Fosaprepitant Indinavir Losartan Lovastatin Montelukast Omarigliptin Raltegravir Rizatriptan Rofecoxib Simvastatin Sitagliptin Vorinostat

Publications:	The Merck Manuals Index Manual Veterinary Geriatrics

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Omarigliptin

History

References

See also