Type 2 diabetes (T2D) and obesity are chronic diseases associated with high morbidity worldwide, seriously threatening people’s life and health. Tirzepatide, as a novel glucagon-like peptide 1 receptor (GLP-1R)/glucose-dependent insulinotropic polypeptide receptor (GIPR) dual-targeted agonist, has been proven to be effective in reducing body weight and controlling blood glucose levels in several clinical studies. Therefore, it has been approved by the Food and Drug Administration (FDA) for treating T2D and managing chronic weight in overweight or obese patients, with good therapeutic effects, safety and tolerability. Metabolic dysfunction-associated steatohepatitis (MASH), a metabolic syndrome related to T2D and obesity, is considered an independent risk factor for cardiovascular disease. It can decrease levels of markers associated with MASH and liver fibrosis and even led to the MASH resolution with no fibrosis worsening in treating T2D patients, without increasing the risk of cardiovascular events. The available evidence suggests that it may have potential therapeutic effects on MASH. This review presents a summary of recent preclinical studies and clinical trials on the application of tirzepatide to treat diabetes, obesity, MASH, cardiovascular disease, and kidney disease and reveals the promising prospect of using tirzepatide as a magic bullet in treating metabolic disorders.