Abstract
Omarigliptin [Marizev® (Japan)] is a small-molecule dipeptidyl peptidase-4 (DPP-4) inhibitor developed by Merck for the oral treatment of type 2 diabetes (T2DM). Unlike the majority of other approved agents of its class, which are usually administered once daily, omarigliptin can be administered once weekly. Once-weekly omarigliptin has received its first global approval in this indication in Japan, for use in adults. Phase III clinical development of the product is underway in several other countries. This article summarizes the milestones in the development of omarigliptin leading to this first approval for the treatment of T2DM.
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References
Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006;368(9548):1696–705.
MSD. Omarigliptin (MARIZEV tablets 12.5 mg, 25 mg): Japanese prescribing information. Tokyo: MSD; 2015.
Asche C, LaFleur J, Conner C. A review of diabetes treatment adherence and the association with clinical and economic outcomes. Clin Ther. 2011;33(1):74–109.
Merck. Merck submits new drug application to the Japanese Pharmaceuticals and Medical Devices Agency for omarigliptin, an investigational once-weekly DPP-4 inhibitor for type 2 diabetes [media release]. http://www.mercknewsroom.com/news-release/prescription-medicine-news/merck-submits-new-drug-application-japanese-pharmaceuticals-. Accessed 24 Nov 2014.
Merck. MARIZEV® (Omarigliptin), Merck’s once-weekly DPP-4 inhibitor for type 2 diabetes, approved in Japan [media release]. http://www.businesswire.com/news/home/20150928005491/en/MARIZEV%C2%AE-Omarigliptin-Merck%E2%80%99s-Once-Weekly-DPP-4-Inhibitor-Type. Accessed 28 Sep 2015.
Biftu T, Sinha-Roy R, Chen P, et al. Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. J Med Chem. 2014;57(8):3205–12.
Krishna R, Addy C, Tatosian D, et al. Single-/multiple-dose pharmacokinetics (PK) and pharmacodynamics (PD) of omarigliptin, a once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in healthy subjects [abstract no. 1097-P]. Diabetes. 2013;62:A284.
Sheu WH, Gantz I, Chen M, et al. Safety and efficacy of omarigliptin (MK-3102), a novel once-weekly DPP-4 inhibitor for the treatment of patients with type 2 diabetes. Diabetes Care. 2015. doi:10.2337/dc15-0109.
Addy C, Tatosian D, Hou XS, et al. Pharmacokinetic (PK) and pharmacodynamic (PD) effects of multiple-dose administration of omarigliptin, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in obese subjects with and without type 2 diabetes mellitus (T2DM) [abstract no. 1106-P]. Diabetes. 2013;62(Suppl 1):A287.
Tatosian DA, Cardillo Marricco N, Glasgow X, et al. A TQT study confirms early PK/PD modeling that a supratherapeutic dose of omarigliptin, a once-weekly DPP 4 inhibitor, does not prolong the QTC interval [abstract no. PI-100]. Clin Pharmacol Ther. 2015;97(Suppl 1):S50.
Xu S, Kauh A, Tatosian D, et al. Absorption, metabolism, and excretion of [14C]omarigliptin, a once-weekly DPP-4 inhibitor, in humans [abstract no. 1080-P]. Diabetes. 2014;63(Suppl 1):A281.
Tatosian DA, Glasgow S, Caceres M, et al. Pharmacokinetics of omarigliptin (Mk-3102), a once-weekly dpeptidyl peptidase-IV (DPP-4) inhibitor, in patients with renal impairment [abstract no. Poster—PII-087]. In: American Society for Clinical Pharmacology and Therapeutics Annual Meeting. 2014.
Addy C, Tatosian D, Hou XS, et al. Effects of age, gender and obesity on the single dose pharmacokinetics (PK) of omarigliptin, a novel once-weekly dipeptidyl peptidase- 4 (DPP-4) inhibitor [abstract no. 1157-P]. Diabetes. 2013;62(Suppl 1):A301.
Gantz I, Okamoto T, Ito Y. Effect of omarigliptin, a novel once-weekly DPP-4 inhibitor, in Japanese patients with type 2 diabetes: a placebo- and sitagliptin-controlled trial [abstract no. 115]. In: European Association for the Study of Diabetes (EASD). 2015.
Gantz I, Lai E, Suryawanshi S, et al. Omarigliptin, a once-weekly DPP-4 inhibitor, provides similar glycaemic control to sitagliptin in patients with type 2 diabetes mellitus inadequately controlled on metformin [abstract no. 110]. In: European Association for the Study of Diabetes (EASD). 2015.
Okuyama K, Engel SS, Okamoto T, et al. Omarigliptin improves glycemic control and is well tolerated as add-on therapy to oral antihyperglycemic agents in Japanese patients with type 2 diabetes [abstract no. 1231-P]. Diabetes. 2015;64(Suppl 1):A318–9.
Mann K. Novel once-weekly omarigliptin as effective and well tolerated as once-daily sitagliptin in Japanese patients. MD Conference Express, European Association for the Study of Diabetes: 50th annual meeting. 2014. doi:10.1177/155989771432019.
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The preparation of this review was not supported by any external funding. During the peer review process the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from any comments received were made by the author on the basis of scientific completeness and accuracy. C. B. Burness is a salaried employee of Adis, Springer SBM.
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This profile has been extracted and modified from the AdisInsight database. AdisInsight tracks drug development worldwide through the entire development process, from discovery, through pre-clinical and clinical studies to market launch and beyond.
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Burness, C.B. Omarigliptin: First Global Approval. Drugs 75, 1947–1952 (2015). https://doi.org/10.1007/s40265-015-0493-8
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DOI: https://doi.org/10.1007/s40265-015-0493-8