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Tirzepatide is a combined glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptor agonist. This review will summarize the pharmacological aspects of tirzepatide with a focus on the clinical efficacy and safety reported in the trial programs underlying the regulatory approval for the treatment of type 2 diabetes (T2D) and obesity in the US and Europe. In a range of trials, tirzepatide has been compared to placebo, insulin and GLP-1 mono-receptor agonists. The trials have included participants with T2D (SURPASS) and obesity (SURMOUNT-1) and have examined tirzepatide in doses ranging from 5 to 15 mg administered once weekly. In the SURPASS trials, tirzepatide led to dose-dependent clinically relevant reductions in HbA1c of up to 20-28 mmol/mol. A head-tohead trial comparing tirzepatide (5-15 mg once weekly) to the GLP-1 mono-receptor agonist semaglutide (1 mg …