The incretin hormones glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) are responsible for up to 65% of postprandial insulin secretion. Tirzepatide, developed by Eli Lilly, is a dual GIP/GLP-1 receptor agonist in the form of a synthetic linear peptide; its acylation technology allows it to bind to albumin, thus making it possible to dose the drug once a week. This review summarizes the key characteristics and pharmacokinetics of tirzepatide. The authors present the results of a phase 1, 2, and 3 clinical trial on the effects of tirzepatide on glycaemic and lipid control and the beneficial effects on body weight in a dose-dependent manner in patients with type 2 diabetes mellitus (T2DM). Tirzepatide has the ability to reduce glycaemic levels, improve insulin sensitivity, reduce body weight, and improve lipid metabolism, which is critically important in T2DM. Tirzepatide administered by weekly subcutaneous injections appears to be a promising drug for the treatment of T2DM as well as cardiometabolic disorders. The mechanism of action and safety profile of tirzepatide potentially fills important gaps in the current treatment of T2DM.