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Lixisenatide: clinical profile and available evidence

Ilaria Dicembrini, Michela Bigiarini & Edoardo Mannucci

Incretin-based therapies, which exploit the physiological actions of GLP‑1, have attracted interest as a novel therapeutic option for Type 2 diabetes. In particular, GLP‑1 receptor agonists provide significant improvements in HbA1c, with a low risk of hypoglycemia, as well as improvements in a wide spectrum of extraglycemic factors. These drugs can be categorized as either short- or long-acting compounds. Their efficacy on glucose homeostasis and safety profiles seems to be significantly affected by pharmacokinetics, thus enabling incretin-based therapy to be tailored for each patient affected by Type 2 diabetes. This review gives an overview of pharmacological, preclinical and clinical evidence of the most recently developed short-acting GLP‑1 receptor agonist lixisenatide. Medline was searched for English‑language articles that evaluated pharmacodynamics, pharmacokinetics, metabolism and mechanism of action of lixisenatide. An extensive Medline and Embase search for ’lixisenatide’ and ‘glucagon-like peptide-1 receptor agonist’ was performed, collecting all randomized clinical trial data for humans. Completed but still unpublished trials were identified through a search of the www.clinicaltrials.gov website. US FDA and EMA reviews were also searched for data from unpublished trials. The most relevant papers and meeting abstracts published up to June 2013 were identified for inclusion in this review.