GIPR/GLP-1R dual agonist therapies for diabetes and weight loss—chemistry, physiology, and clinical applications

Aug 17, 2023Cell metabolism

Combined GIP and GLP-1 receptor therapies for diabetes and weight loss: chemistry, body effects, and medical uses

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Abstract

Tirzepatide is the first monomeric peptide with dual activity at both incretin receptors.

  • The incretin system is crucial for regulating metabolism after eating.
  • Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) are key hormones in this system.
  • Pharmacological activation of GLP-1R is effective for managing high blood sugar and aiding weight loss.
  • Clinical trials have demonstrated that tirzepatide significantly lowers blood glucose and body weight.
  • The development of monomeric multi-incretin receptor agonists like tirzepatide represents an advancement in treating metabolic disorders.

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