Saxagliptin: A New Drug for the Treatment of Type 2 Diabetes

Title: Saxagliptin: A New Drug for the Treatment of Type 2 Diabetes

Volume: 10 Issue: 8

Author(s): Suresh Thareja, Saurabh Aggarwal, Priyanka Malla, Diksha Haksar, Tilak Raj Bhardwaj and Manoj Kumar

Affiliation:

Keywords: Diabetes, DPP IV, incretin, gliptin, onglyza

Abstract: Saxagliptin (BMS-477118), a recently FDA approved drug for the management of T2DM, has been developed by Bristol-Myers Squibb and AstraZeneca under the trade name Onglyza™. Saxagliptin is a nitrile-containing selective, potent, reversible and durable DPP IV inhibitor developed as an alternative second-line to Metformin in place of a sulphonylurea. Saxagliptin increases and prolongs the action of incretin hormones by inhibiting the DPP IV enzyme that inactivates incretins usually within minutes. Saxagliptin is well absorbed and has low plasma protein binding and displays slow-binding properties to DPP IV. Saxagliptin is metabolized in vivo to form an active metabolite (BMS-510849), which is twofold less potent than the parent molecule. The X-ray crystallography revealed that Saxagliptin is covalently bound to the DPP IV active site. In drug-naive patients with T2DM and inadequate glycemic control, once-daily Saxagliptin monotherapy for 24 wks demonstrated clinically meaningful with no weight gain and was generally well tolerated.

Cite this article as:

Thareja Suresh, Aggarwal Saurabh, Malla Priyanka, Haksar Diksha, Raj Bhardwaj Tilak and Kumar Manoj, Saxagliptin: A New Drug for the Treatment of Type 2 Diabetes, Mini-Reviews in Medicinal Chemistry 2010; 10 (8) . https://dx.doi.org/10.2174/138955710791572424