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Objective: Provide a comprehensive overview of efficacy and safety data on incretin-based agents in the treatment of type 2 diabetes.

Data sources: A PubMed search was conducted for the years 2000–2009, using as keywords the names of glucagon-like peptide-1 (GLP-1) receptor agonists (exenatide and liraglutide) and dipeptidyl peptidase-4 (DPP-4) inhibitors (sitagliptin, alogliptin,
and saxagliptin). World Diabetes Congress abstracts from 2008 to 2009 were also searched for clinical studies of these agents.

Study selection: The author included randomized controlled trials of incretin therapies that were published in English and enrolled ≥100 participants.

Data extraction: Data on the effects of incretins on glycemic control, weight,beta-cell function, blood pressure, lipid levels, safety, and tolerability were extracted and summarized.

Data synthesis: A total of 27 randomized controlled studies of incretin therapy were identified and included in the review. GLP-1 receptor agonists and DPP-4 inhibitors were evaluated at different points in the diabetes treatment spectrum, i.e.,
added to diet and exercise alone (monotherapy) or added to oral antihyperglycemic regimens (combination therapy).

Conclusion: In addition to decreasing glycemia in type 2 diabetes, incretin therapies may improve other important parameters, including beta-cell function, blood pressure, and lipid levels, with a low risk for hypoglycemia. A comparison of the study data differentiates the clinical profiles of the GLP-1 receptor agonists, which are associated with weight loss, and DPP-4 inhibitors, which are weight neutral, as well as the individual agents within each class.

Keywords: Type 2 diabetes, GLP-1 receptor agonists, DPP-4 inhibitors, liraglutide, exenatide LAR, sitagliptin, saxagliptin, alogliptin.