Research on incretin hormones has advanced considerably over the past few decades. Although the initial molecule – glucose-dependent insulinotropic polypeptide – failed to stimulate insulin secretion in patients with type 2 diabetes, it led to the discovery of glucagon-like peptide 1 (GLP-1). As GLP-1 impacts on various tissues and cells throughout the body, it allows patients with type 2 diabetes to benefit in many ways, in addition to lowering blood glucose levels. In a bid to harness these benefits pharmacologically, analogues were evolved from GLP-1 to produce a class of peptides known as GLP-1 receptor agonists (GLP-1RAs). The mechanism of action by which GLP-1RAs achieve their effects on lowering glucose levels, body weight, systolic blood pressure as well as lipid profiles, and improving cardiovascular and renal outcomes will be further discussed. With the advancement in research and development, the advent of scientific research and development has greatly accelerated the global implementation and local approved use of the first oral GLP-1RA, allowing the abovementioned benefits to be easily accessed. Oral GLP-1RA is set to bring about a revolution in the management of type 2 diabetes in Singapore.