Lixisenatide: a once-daily glucagon-like peptide-1 receptor agonist

Authors

  • Tushar Balchand Chudiwal Department of Pharmacology, Ananta Institute of Medical Science and Research Center, Rajsamand, Rajasthan, India
  • Indrajeet Omprakash Sharma Department of Pharmacology, Ananta Institute of Medical Science and Research Center, Rajsamand, Rajasthan, India

DOI:

https://doi.org/10.18203/2319-2003.ijbcp20164085

Keywords:

Glucagon-like peptide-1 receptor agonist, Insulin, Lixisenatide, Type 2 diabetes

Abstract

Lixisenatide (AVE0010) is a once-daily glucagon-like peptide-1 (GLP-1) receptor agonist used in the treatment of type 2 diabetes. Phase II dose-finding and pharmacodynamic studies identified the 20 µg once-daily dose as having the optimum combination of efficacy, convenience and tolerability. Lixisenatide was prospectively investigated in a series of 11 multinational, randomised, controlled phase III trials (GLP-1 agonist AVE0010 in patients with type 2 diabetes mellitus for Glycemic control and safety evaluation [Getgoal] programme) that included a direct head-to-head study with exenatide. The Getgoal programme established the efficacy and safety profile of lixisenatide 20 µg once daily across the spectrum of patients with type 2 diabetes, including patients not treated with anti-diabetic agents, those failing on oral agents and as an adjunct to basal insulin therapy. The main efficacy endpoints were met in all studies, with the baseline to endpoint reductions in HbA1c consistently ranging from 0.7% to 1.0%. In a head-to-head comparison with exenatide 10 µg twice daily, lixisenatide 20 µg once daily was non-inferior for HbA1c reduction, achieved with threefold fewer patients with symptomatic hypoglycemia events and better gastrointestinal tolerability. Three randomised trials of lixisenatide treatment added to basal insulin showed significantly improved glycemic control over placebo, with pronounced postprandial glucose reductions and good tolerability. Discontinuations for adverse events were consistently low, ranging from 2.5% to 10.4%. As the provision of individualized care moves center stage in diabetes management, lixisenatide with once-daily dosing, a single maintenance dose and fixed-dose pens offers an important treatment option for type 2 diabetes.

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Published

2016-12-21

How to Cite

Chudiwal, T. B., & Sharma, I. O. (2016). Lixisenatide: a once-daily glucagon-like peptide-1 receptor agonist. International Journal of Basic & Clinical Pharmacology, 5(6), 2311–2320. https://doi.org/10.18203/2319-2003.ijbcp20164085

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Section

Review Articles