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Inhibitors of dipeptidyl peptidase 4, also DPP-4 inhibitors or gliptins, are a class of oral hypoglycemics that block DPP-4. They can be used to treat diabetes mellitus type 2. The first agent of the class - sitagliptin - was approved by the FDA in 2006.〔 〕 Glucagon increases blood glucose levels, and DPP-4 inhibitors reduce glucagon and blood glucose levels. The mechanism of DPP-4 inhibitors is to increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels. A recent meta analysis found no favorable or harmful effect of DPPIV inhibitors on all-cause mortality, cardiovascular mortality, or stroke, but a marginally statistically significant increase in heart failure. ==Examples== Drugs belonging to this class are : * Sitagliptin (FDA approved 2006, marketed by Merck & Co. as Januvia), * Vildagliptin (EU approved 2007, marketed in the EU by Novartis as Galvus), * Saxagliptin (FDA approved in 2009, marketed as Onglyza), * Linagliptin (FDA approved in 2011, marketed as Tradjenta by Eli Lilly Co and Boehringer Ingelheim), * Anagliptin (approved in Japan in 2012, marketed by Sanwa Kagaku Kenkyusho Co., Ltd. and Kowa Company, Ltd.)〔http://www.pmda.go.jp/english/service/pdf/list/NewdrugsFY2012.pdf〕 * Teneligliptin (approved in Japan in 2012) * Alogliptin (FDA approved 2013, marketed by Takeda Pharmaceutical Company) * Trelagliptin, approved for use in Japan in 2015 * Gemigliptin (being developed by LG Life Sciences)〔(【引用サイトリンク】title=LG Life Science )〕 * Dutogliptin (being developed by Phenomix Corporation), Phase III〔"Forest Splits With Phenomix", San Diego Business Journal, Tuesday, April 20, 2010 http://www.sdbj.com/news/2010/apr/20/forest-splits-phenomix/〕 * Omarigliptin (MK-3102) (approved in Japan in 2015, developed by Merck & Co., research showed that omarigliptin can be used as once-weekly treatment and generally well-tolerated throughout the base and extension studies〔(【引用サイトリンク】 title=Safety and Efficacy of Omarigliptin (MK-3102), a Novel Once-Weekly DPP-4 Inhibitor for the Treatment of Patients With Type 2 Diabetes )〕) Other chemicals which inhibit DPP4 include: * Berberine, the common herbal dietary supplement, too inhibits dipeptidyl peptidase-4, which at least partly explains its antihyperglycemic activity. * Lupeol, found in mango, red alder (Alnus rubra), and dandelion coffee. 抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)』 ■ウィキペディアで「Dipeptidyl peptidase-4 inhibitor」の詳細全文を読む スポンサード リンク
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