Omarigliptin
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Omarigliptin (MK-3102) is a potent, long-acting oral
antidiabetic drug Drugs used in diabetes treat diabetes mellitus by altering the glucose level in the blood. With the exceptions of insulin, most GLP receptor agonists ( liraglutide, exenatide, and others), and pramlintide, all are administered orally and are t ...
of the
DPP-4 inhibitor Inhibitors of dipeptidyl peptidase 4 (DPP-4 inhibitors or gliptins) are a class of oral hypoglycemics that block the enzyme dipeptidyl peptidase-4 (DPP-4). They can be used to treat diabetes mellitus type 2. The first agent of the class – sitag ...
class used for once-weekly treatment of
type 2 diabetes Type 2 diabetes, formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent urination, ...
and currently under development by Merck & Co. It inhibits DPP-4 to increase
incretin Incretins are a group of metabolic hormones that stimulate a decrease in blood glucose levels. Incretins are released after eating and augment the secretion of insulin released from pancreatic beta cells of the islets of Langerhans by a blood-gl ...
levels (
GLP-1 Glucagon-like peptide-1 (GLP-1) is a 30- or 31-amino-acid-long peptide hormone deriving from the tissue-specific posttranslational processing of the proglucagon peptide. It is produced and secreted by intestinal enteroendocrine L-cells and certa ...
and GIP), which inhibit
glucagon Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It raises concentration of glucose and fatty acids in the bloodstream, and is considered to be the main catabolic hormone of the body. It is also used as a Glucagon (medicati ...
release, which in turn increases
insulin Insulin (, from Latin ''insula'', 'island') is a peptide hormone produced by beta cells of the pancreatic islets encoded in humans by the ''INS'' gene. It is considered to be the main anabolic hormone of the body. It regulates the metabolism o ...
secretion, decreases gastric emptying and decreases
blood glucose Glycaemia, also known as blood sugar level, blood sugar concentration, or blood glucose level is the measure of glucose concentrated in the blood of humans or other animals. Approximately 4 grams of glucose, a simple sugar, is present in the blo ...
levels.


History

Marizev (omarigliptin) 25 mg and 12.5 mg tablets were approved by Japan's
Pharmaceuticals and Medical Devices Agency The (PhMDA) is an Independent Administrative Institution responsible for ensuring the safety, efficacy and quality of pharmaceuticals and medical devices in Japan. It is similar in function to the Food and Drug Administration in the United State ...
(PMDA) on 28th Sept 2015. Japan was the first country to have approved omarigliptin. However Merck has announced that the company will not submit marketing application in the US and Europe.


References


See also

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Dipeptidyl peptidase-4 inhibitor Inhibitors of dipeptidyl peptidase 4 (DPP-4 inhibitors or gliptins) are a class of oral hypoglycemics that block the enzyme dipeptidyl peptidase-4 (DPP-4). They can be used to treat diabetes mellitus type 2. The first agent of the class – sita ...
*
Alogliptin Alogliptin, sold under the brand names Nesina and Vipidia,) is an oral anti-diabetic drug in the DPP-4 inhibitor (gliptin) class. Alogliptin does not decrease the risk of heart attack and stroke. Like other members of the gliptin class, it cause ...
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Linagliptin Linagliptin, sold under the brand name Tradjenta among others, is a medication used to treat type 2 diabetes (but not type 1) in conjunction with exercise and diet. It is generally less preferred than metformin and sulfonylureas as an initial tr ...
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Saxagliptin Saxagliptin, sold under the brand name Onglyza, is an oral hypoglycemic (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class. Early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Mye ...
*
Sitagliptin Sitagliptin, sold under the brand name Januvia among others, is an anti-diabetic medication used to treat type 2 diabetes. In the United Kingdom it is listed as less preferred than metformin or a sulfonylurea. It is taken by mouth. It is also a ...
*
Vildagliptin Vildagliptin, sold under the brand name Galvus and others, is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4 ...
Dipeptidyl peptidase-4 inhibitors Fluoroarenes Sulfonamides Phenylethanolamine ethers Merck & Co. brands {{gastrointestinal-drug-stub