Retatrutide is an engineered single-peptide chain studied as a triple hormone receptor agonist, examined in relation to three endocrine pathways simultaneously.
GLP-1 receptor
Research examined interaction with insulinotropic mechanisms, gastric motility, and appetite feedback markers.
GIP receptor
Studies examined GIP pathway engagement alongside GLP-1 in relation to glucose-dependent insulin secretion and adipose tissue dynamics.
Glucagon receptor
Research examined glucagon receptor engagement in relation to resting metabolic energy expenditure and hepatic lipid oxidation.
Retatrutide
GLP-1 engagement
GIP engagement
Glucagon engagement
Metabolic homeostasis examined
Peer-reviewed references
Jastreboff AM, et al. Triple-hormone-receptor agonist retatrutide for obesity, a phase 2 trial. New England Journal of Medicine. 2023;389(6):514-526. doi.org/10.1056/NEJMoa2301972
Rosenstock J, Frias J, Jastreboff AM, et al. Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo and active-controlled, parallel-group, phase 2 trial conducted in the USA. Lancet. 2023;402(10401):529-544. doi.org/10.1016/S0140-6736(23)01053-X
Retatrutide adds a third receptor to the incretin approach, activating GIP, GLP-1, and glucagon receptors at once. Two phase 2 trials in humans were published in 2023, in the New England Journal of Medicine and the Lancet.
Retatrutide is the first triple GIP, GLP-1, and glucagon receptor agonist to reach late-stage human trials. Two phase 2 trials in humans were published in 2023, one in the New England Journal of Medicine and one in the Lancet.
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