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Agnieszka Jakubowska 1 Article
Diabetes, obesity and metabolism
The Road towards Triple Agonists: Glucagon-Like Peptide 1, Glucose-Dependent Insulinotropic Polypeptide and Glucagon Receptor - An Update
Agnieszka Jakubowska, Carel W. le Roux, Adie Viljoen
Endocrinol Metab. 2024;39(1):12-22.   Published online February 14, 2024
DOI: https://doi.org/10.3803/EnM.2024.1942
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  • 6 Web of Science
  • 8 Crossref
AbstractAbstract PDFPubReader   ePub   
Obesity is the fifth leading risk factor for global deaths with numbers continuing to increase worldwide. In the last 20 years, the emergence of pharmacological treatments for obesity based on gastrointestinal hormones has transformed the therapeutic landscape. The successful development of glucagon-like peptide-1 (GLP-1) receptor agonists, followed by the synergistic combined effect of glucose-dependent insulinotropic polypeptide (GIP)/GLP-1 receptor agonists achieved remarkable weight loss and glycemic control in those with the diseases of obesity and type 2 diabetes. The multiple cardiometabolic benefits include improving glycemic control, lipid profiles, blood pressure, inflammation, and hepatic steatosis. The 2023 phase 2 double-blind, randomized controlled trial evaluating a GLP-1/GIP/glucagon receptor triagonist (retatrutide) in patients with the disease of obesity reported 24.2% weight loss at 48 weeks with 12 mg retatrutide. This review evaluates the current available evidence for GLP-1 receptor agonists, dual GLP-1/GIP receptor co-agonists with a focus on GLP-1/GIP/glucagon receptor triagonists and discusses the potential future benefits and research directions.

Citations

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    International Journal of Molecular Sciences.2024; 25(8): 4407.     CrossRef
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    Frontiers in Pharmacology.2024;[Epub]     CrossRef
  • Mechanisms of Glucagon Receptor Agonism and GLP-1/Glucagon/GIP Receptor Triple Agonism for Treatment of Diabetes and Obesity
    Se Hee Min
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  • Structural insights into the triple agonism at GLP-1R, GIPR and GCGR manifested by retatrutide
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  • Molecular Mechanisms behind Obesity and Their Potential Exploitation in Current and Future Therapy
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  • GLP-1 Receptor Agonists and SGLT2 Inhibitors in Type 2 Diabetes: Pleiotropic Cardiometabolic Effects and Add-on Value of a Combined Therapy
    André J. Scheen
    Drugs.2024;[Epub]     CrossRef
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