Tonichem Pharmaceutical Technology Co., Limited

DPP-4 Inhibitors

DPP-4 Inhibitors

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.



Sitagliptin was approved by the U.S. Food and Drug Administration (FDA) on October 17, 2006, and is marketed in the US as Januvia by Merck & Co. On April 2, 2007, the FDA approved an oral combination of sitagliptin and metformin marketed in the US as Janumet.

Saxagliptin, early development was solely by Bristol-Myers Squibb; in 2007 AstraZeneca joined with Bristol-Myers Squibb to co-develop the final compound and collaborate on the marketing of the drug. In June 2008, it was announced that Onglyza would be the trade name under which saxagliptin will be marketed. The FDA approved Saxagliptin with brand name Onglyza on July 31, 2009.

Vildagliptin,Novartis has since withdrawn its intent to submit vildagliptin to the FDA, as of July 2008.The Food and Drug Administration had demanded additional clinical data before it could approve vildagliptin including extra evidence that skin lesions and kidney impairment seen during an early study on animals have not occurred in human trials. While the drug is still not approved for use in the US, it was approved in February 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions.

Linagliptin (once-daily) was approved by the US FDA on 2 May 2011 for treatment of type II diabetes. It is being marketed by Boehringer Ingelheim and Lilly.

Alogliptin, on January 25 2013, the FDA announced approval of 3 drugs — Nesina (alogliptin) tablets, the fixed-dose combinations Kazano (alogliptin and metformin hydrochloride) tablets, and Oseni (alogliptin and pioglitazone) tablets for use with diet and exercise to improve blood glucose control in adults with type 2 diabetes. All 3 are manufactured by Takeda Pharmaceuticals America, Inc.

There are other two drugs under Clinical trial. One is Dutoliptin developed by Phenomix and Forest Laboratories. The other is Melogliptin, developed by Glenmark.