1 Medicinsk Afdeling GLO, Amager and Hvidovre Hospital, The Capital Region of Denmark2 Klinisk Genetisk Klinik, Juliane Marie Centre, Rigshospitalet, The Capital Region of Denmark3 Internal Medicine, Gentofte, Herlev and Gentofte Hospital, The Capital Region of Denmark
Lixisenatide (trade name Lyxumia®), a short-acting glucagon-like peptide 1 receptor (GLP-1R) agonist, was approved for the treatment of type 2 diabetes by the European Medicines Agency in early 2013. In preclinical investigations, acceptable toxicity and carcinogenicity profiles were demonstrated, as well as pancreatic beta cell-preserving actions and favorable effects on glycemic control. Following subcutaneous administration in humans, lixisenatide displays linear pharmacokinetics and an absorption-dependent elimination half-life of 2-3 hours. In clinical trials of up to 1 year duration in patients with type 2 diabetes, treatment with lixisenatide alone and in combination with insulin and various oral antidiabetics conferred significant reductions in HbA1c, fasting and postprandial plasma glucose. In direct comparison with the other GLP-1R agonists on the market (exenatide and liraglutide), lixisenatide appears to be less efficient, or at best non-inferior in terms of reducing HbA1c, fasting plasma glucose and body weight. Nevertheless, lixisenatide confers fewer adverse events than the other currently marketed GLP-1R agonists, while exhibiting a clinically valuable effect on postprandial hyperglycemia.
Drugs of Today, 2013, Vol 49, Issue 9, p. 537-53
Animals; Blood Glucose; Body Weight; Diabetes Mellitus, Type 2; Drug Evaluation, Preclinical; Drug Interactions; Half-Life; Humans; Hypoglycemic Agents; Peptides