The therapeutic approach to type 2 diabetes mellitus increasingly includes therapy based on the incretin system, especially glucagon-like peptide-1 agonists. These agents mimic the secretion of the endogenously produced incretin hormone GLP-1, leading to increased insulin secretion and suppressed glucagon secretion, which is essential for maintaining glucose homeostasis. The pancreatic effects of GLP-1 receptor analogues are manifested by increased glucose-dependent insulin secretion from pancreatic β-cells and inhibition of glucagon secretion from α-cells of the pancreatic islets. β-cell proliferation, inhibition of apoptosis and enhanced insulin synthesis are some of the beneficial effects on pancreatic tissue. Beyond their pancreatic effects, GLP 1R analogues show some systemic benefits, especially in the protection of the cardiovascular system and weight loss. Clinical studies conducted to prove cardiovascular safety have shown that GLP-1 receptor analogues reduce the risk of a major adverse cardiovascular event, which includes cardiovascular death, non-fatal myocardial infarction or non-fatal stroke. It exerts cardioprotective effects through several mechanisms, including the regulation of glycemia, blood pressure, lipid levels and body weight. Also, GLP-1R analogues have shown renal protection by slowing the progression of diabetic nephropathy by preserving eGFR and reducing albuminuria. Therapy with GLP-1 receptor analogues also affects the function of the gastrointestinal system. It slows down gastric emptying and intestinal motility and provides a feeling of satiety, which all together results in reduced food intake. This advantage is used for better body weight management. Finally, recent data provide information on neuroprotective effects and alleviation of cognitive disorders, while leaving room for the realization of therapeutic potential in this area as well.