ObjectiveTo systematically review the effectiveness and safety of GLP-1 receptor agonists versus DPP-4 inhibitors for type 2 diabetes mellitus (T2DM). MethodsDatabases including PubMed, EMbase, The Cochrane Library (Issue 4, 2013), WanFang Data, CBM and CNKI were searched electronically for randomized controlled trials (RCTs) about GLP-1 receptor agonists versus DPP-4 inhibitors for T2DM up to April 2013. Two reviewers independently screened literature according to the inclusion and exclusion criteria, extracted data, and assessed methodological quality of included studies. Then meta-analysis was performed using RevMan 5.2.5 software. ResultsA total of 4 RCTs was included. The results of meta-analysis showed that:compared with DPP-4 inhibitors, GLP-1 receptor agonists were more effective in reducing levels of glycated hemoglobin (MD=-0.46, 95%CI-0.57 to-0.35, P < 0.000 01), fasting blood glucose (MD=-1.13, 95%CI-1.39 to-0.88, P < 0.000 01), and weight (MD=-1.59, 95%CI-1.99 to-1.19, P < 0.000 01). In addition, T2DM patients taking GLP-1 receptor agonists had significantly higher achievement rates of glycosylated haemoglobin ( < 7% and≤6.5%), and higher incidences of nausea (OR=4.31, 95%CI 2.87 to 6.47, P < 0.000 01) and diarrhea (OR=2.11, 95%CI 1.40 to 3.18, P=0.000 4). ConclusionGLP-1 receptor agonists are superior to DPP-4 inhibitors in controlling T2DM patients' levels of blood glucose and reducing weight, but it has more gastrointestinal adverse reaction.