Type 2 diabetes mellitus (T2DM) is a chronic disease with a significant socioeconomic impact, whose therapeutic management has undergone substantial evolution in recent years, driven by the development of novel pharmacological strategies. This progress has been made possible by an increasingly refined understanding of the underlying pathophysiological mechanisms, including insulin resistance, pancreatic $\beta $ -cell dysfunction, and impairment of the incretin axis. This article aims first to analyse the pathophysiological aspects of the key molecules currently at the centre of pharmacological research: glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and glucagon. It will then discuss the characteristics and potential clinical benefits of dual agonists (primarily GIP/GLP-1 and GLP-1/glucagon) and triple agonists, with particular attention to differences in efficacy and safety profiles compared to dual therapies. For each pharmacological class, the main therapeutic agents either approved for clinical use or in development will be examined, summarising the most recent data from preclinical and clinical studies regarding efficacy, safety, and tolerability. In addition to improvements in glycaemic control and body weight reduction, the article will highlight the pleiotropic effects of these drugs on other organs and systems, including the cardiovascular, renal, and hepatic systems. The objective is to outline current therapeutic perspectives and provide an updated overview of ongoing research directions in the treatment of T2DM. Preliminary data appear promising, but further long-term studies will be needed to confirm the safety and efficacy of these innovative therapeutic approaches.