Pharmacological profile, efficacy and safety of lixisenatide in type 2 diabetes mellitus

Introduction: The global prevalence of type 2 diabetes mellitus (T2DM) is rapidly increasing and is associated with a high risk of microvascular and macrovascular complications. Although some glucose-lowering therapies are associated with hypoglycemia and weight gain, glucagon-like peptide-1 (GLP-1) receptor agonists represent a significant advance in the treatment of T2DM, as they provide effective glycemic control with a low incidence of hypoglycemia and a beneficial effect on body weight, as well as potential improvements in cardiovascular outcomes. Areas covered: This article evaluates the pharmacological and clinical profile of the once-daily prandial GLP-1 receptor agonist lixisenatide for the treatment of T2DM. Expert opinion: Once-daily prandial lixisenatide has been evaluated in an extensive clinical trials program, in which it was shown to have a favorable safety and tolerability profile, and to effectively improve metabolic control. The unique pharmacological properties of lixisenatide clearly differentiate it from other GLP-1 receptor agonists. As a once-daily agonist with a high affinity for the GLP-1 receptor, lixisenatide improves overall glycemic control, with particularly strong effects on postprandial plasma glucose levels. These attributes encourage the application of lixisenatide in those patients with extensive postprandial glucose excursions, or in combination with other antidiabetic drugs that have prevailing effects on fasting glucose levels.