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Insights into the Mechanism of Action of Tirzepatide: A Narrative Review

Abstract

Tirzepatide is the first dual long-acting glucose-dependent insulinotropic polypeptide receptor and glucagon-like peptide-1 receptor agonist indicated for the treatment of type 2 diabetes in adults, for reducing excess body weight and maintaining long-term weight reduction in adults with obesity or overweight and at least one weight-related comorbid condition, and for treating obstructive sleep apnea in adults with obesity. Recent studies found beneficial effects on heart failure with preserved ejection fraction and on metabolic dysfunction–associated steatohepatitis; its effects on cardiovascular outcomes in people with type 2 diabetes, as well as on reducing morbidity and mortality in people with obesity/overweight, remain under investigation. Here, we review the mechanistic activity of tirzepatide and its effect on glycemic control, body weight, the cardiorenal system, and lipid metabolism.
Title
Insights into the Mechanism of Action of Tirzepatide: A Narrative Review
Authors
Rodolfo J. Galindo
Alice Y. Y. Cheng
Christine Longuet
Minrong Ai
Tamer Coskun
Raleigh Malik
Jennifer Peleshok
Joshua A. Levine
Julia P. Dunn
Publication date
06-11-2025
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Image Credits
Marble run/© Juan L Zavala / iStock / Getty Images Plus, Woman monitoring glucose level with sensor and an app on her phone while training at swimming pool/© (M) Goffkein, stock.adobe.com (symbolic image with model), Person walking/© _KUBE_ / Stock.adobe.com