[From GLP1 receptor agonists to triple hormone receptor activation supplemented with glucagon receptor agonism.].
Winkler. Gábor G; Kis. János Tibor JT; Arapovicsné Kiss. Krisztina K; Schandl. László L
Key Findings
- Retatrutide is the first triple‑receptor agonist (GLP‑1, GIP, glucagon) tested in humans.
- Preclinical human trials reported significant weight loss, better glucose control, and reduced liver fat.
- Safety signals were mild and comparable to existing GLP‑1 therapies.
Practical Outcomes
- For biohackers, retatrutide signals a future option that could outperform current GLP‑1 drugs for weight and metabolic health. Until it’s approved, the main takeaway is to watch upcoming trial results and consider that multi‑hormone activation may become a new strategy for optimizing longevity and body composition.
Summary
The paper reviews a new drug called retatrutide that activates three hormone receptors (GLP‑1, GIP, and glucagon). Early human studies show it may improve blood sugar control, promote weight loss, boost energy use, and help liver fat, with a decent safety profile. While it’s not yet on the market, the data suggest it could become a powerful tool for tackling obesity, diabetes, and related metabolic issues.
Abstract
Following the introduction of mono- and then dual hormone (incretin) receptor agonists into therapy, attention was turned to multiple receptor stimulation, with the additional activation of the glucagon receptor, as a new option for the pharmaceutical treatment of type 2 diabetes and obesity. In addition to its role in carbohydrate metabolism, the article reviews the other important physiological tasks of glucagon, especially its participation in intrainsular paracrine regulation, energy expenditure and the shaping of appetite and food consumption. It covers the potential benefits of the triple combination and briefly touches data on the efficacy and safety of the first triple receptor agonist drug, retatrutide, in preclinical human studies. Further confirmation of the promising results may represent progress in the treatment of these forms of disease and their accompanying conditions, such as steatosis hepatis. Orv Hetil. 2023; 164(42): 1656-1664.
Study Information
pubmed
2023
2023-10-22T00:00:00.000Z
10.1556/650.2023.32894