827033-10-3

Lixisenatide (also known as AVE0010) is a glucagon-like peptide 1 (GLP-1) analog that received marketing approval in February 2013 from the European Commission for the treatment of type 2 diabetes mellitus (T2DM). GLP-1 mimetics, such as exenatide, liraglutide, and lixisenatide act upon the pancreas to promote glucosedependent insulin secretion and to decrease glucagon secretion. They also act on the gastrointestinal tract to delay gastric emptying thereby reducing glucose load postprandially. GLP-1 is a native peptide that is secreted in the gut in reaction to nutrients, but it has a short (2–3 min) half-life in plasma due to the action of DPP-IV. Several modified GLP-1 analogs confer DPP-IV resistance and prolonged plasma half-life, as demonstrated by exenatide (half-life=2–3 h), which was first isolated and identified from the saliva of Helodermatidae lizards (a.k.a. Gila monster).