Tirzepatide: a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) dual agonist in development for the treatment of type 2 diabetes

Abstract

Introduction: The glucagon-like peptide-1 (GLP-1) receptor agonists (RA) have increasingly gained prominence in the treatment of type 2 diabetes (T2D) based on their glycemic benefits and favorable body weight and cardiorenal effects. Despite this, continued development of therapeutics with superior efficacy is important to help address persistent challenges in the attainment of metabolic goals in many patients with T2D.

Areas covered: Tirzepatide is an unimolecular dual glucose-dependent insulinotropic polypeptide (GIP)/GLP-1 RA in development for the treatment of T2D. This review summarizes key characteristics of tirzepatide and Phase 1 and Phase 2 clinical trial efficacy and safety results. Additionally, it provides an overview of the ongoing Phase 3 clinical trial program in T2D and briefly summarizes recently initiated studies in patients with obesity and nonalcoholic steatohepatitis. Information in this review comes primarily from published clinical trials, manufacturer's websites, and ClinicalTrials.gov.

Expert opinion: Based on data from Phase 2 trials, tirzepatide has the potential to be the most efficacious therapy in T2D with respect to both glucose and body weight control. Data from the ongoing Phase 3 clinical trial program should start to become available in late 2020 and will determine the future course of this promising therapeutic agent.

Keywords: Dual GIP/GLP-1 receptor agonist; LY3298176; glucagon-like peptide-1 (GLP-1); glucose-dependent insulinotropic polypeptide (GIP); incretin hormones; tirzepatide; type 2 diabetes.