The ever-increasing burden of obesity, type 2 diabetes mellitus (T2DM) and related comorbidities is demanding a better pathophysiological understanding as well as new treatment options. Incretin based therapies are already available while the recent Food and Drug Administration (FDA) approval of the dual glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist tirzepatide appears to revolutionize the treatment of T2DM and obesity. GLP-1 and GIP exert pleiotropic physiological actions, including enhancement of insulin secretion, glycemic and appetite control, cardioprotection, and adipose tissue improved function among others. Evidence from recent clinical trials has shown that tirzepatide is at least or more effective compared to classic metabolic therapeutic agents, including insulin, when it comes to glycemic control in T2DM. Of importance, it also exerts remarkable weight-lowering actions, emerging as an alternative to bariatric surgery for obesity treatment. Overall, current data show that tirzepatide is a highly effective therapeutic option for T2DM. Numerous ongoing randomized controlled clinical trials are further examining its potential as a treatment for obesity.