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Benefit-Risk Assessment of Exenatide in the Therapy of Type 2 Diabetes Mellitus

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Abstract

Exenatide is the first incretin mimetic, introduced into type 2 diabetes mellitus therapy in 2005, with first approval in the US. It is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used for treatment by twice-daily injection. A long-acting release formulation for once-weekly injection is in clinical development. Clinical studies and postmarketing experience with exenatide have shown a significant and sustained reduction in glycosylated haemoglobin (HbA1c) by approximately 1% together with other gylcaemic parameters without an intrinsic risk for hypoglycaemias, and a reduction in bodyweight by 5.3 kg in 82 weeks. Blood pressure and lipids are also favourably affected, but hard cardiovascular endpoints are not yet available. Animal studies show an improvement of β-cell function and an increase in β-cell mass after exenatide treatment. The most frequent adverse events associated with exenatide therapy are nausea and antibody formation (both approximately 40%). Nausea, mostly mild and transient, was responsible for a 6% dropout rate in clinical studies. A recent review on the association of acute pancreatitis with exenatide treatment showed no increased risk (relative risk 1.0; 95% CI 0.6, 1.7). This review gives a benefit-risk assessment of exenatide.

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Acknowledgements

Professor Gallwitz has been paid honoraria for lectures on various topics related to diabetes by Eli Lilly. He has been participating and is currently involved as investigator or principal investigator in clinical studies sponsored by Eli Lilly. No sources of funding were used to assist in the preparation of this review.

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  1. Department of Medicine IV, Eberhard Karls University, Otfried-Müller-Strasse 10, 72076, Tübingen, Germany

    Baptist Gallwitz

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Gallwitz, B. Benefit-Risk Assessment of Exenatide in the Therapy of Type 2 Diabetes Mellitus. Drug-Safety 33, 87–100 (2010). https://doi.org/10.2165/11319130-000000000-00000

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