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Foundayo ™ (orforglipron) tablet
0.8 mg / 2.5 mg / 5.5 mg / 9 mg / 14.5 mg / 17.2 mg
This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling. See Prescribing Information above, if applicable.
What is the mechanism of action of Foundayo™ (orforglipron)?
Orforglipron binds to and activates the human GLP-1 receptor. GLP-1 receptors exist in brain regions that regulate appetite. In animal studies, orforglipron distributed to and activated neurons in brain regions that regulate appetite and food intake.
See important safety information, including boxed warning, in the attached prescribing information.
Orforglipron Mechanism of Action
What is Glucagon-like Peptide-1?
Glucagon-like peptide-1 (GLP-1) is an incretin hormone released from specialized gut cells in response to the absorption of oral glucose.1
Glucagon-like peptide-1 acts on its receptors in the pancreas to stimulate insulin release and suppress glucagon secretion, in the stomach to delay gastric emptying, and in the hypothalamus to decrease appetite and increase satiety.2,3
These effects help
- keep blood glucose levels within acceptable ranges after nutrient intake, and
- people to stop eating when they feel satiated.1
In people living with type 2 diabetes (T2D) or obesity, GLP-1 has a diminished effect compared to those without these conditions.4
How Does Orforglipron Work?
Orforglipron is an oral GLP-1 receptor agonist that binds to and activates the human GLP-1 receptor.5
In animal studies, orforglipron distributed to and activated neurons in brain regions that regulate appetite and food intake.5
Orforglipron reduces body weight, with greater fat mass loss than lean mass loss. Orforglipron decreases food intake. This effect is likely mediated by decreased appetite.5
Orforglipron delays gastric emptying. The delay is largest after the first dose and diminishes over time.5
In preclinical studies, orforglipron was found to be a partial agonist of the GLP-1 receptor. Orforglipron activates the G protein coupled receptor and exhibits biased agonism favoring cyclic adenosine monophosphate (cAMP) accumulation versus β-arrestin recruitment.6
- cAMP signaling was shown to be associated with enhanced glucose-stimulated insulin secretion and decreased food intake.
- β-arrestin recruitment can lead to receptor desensitization and internalization, potentially reducing the efficacy of the drug over time.6
Enclosed Prescribing Information
References
The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).
1Nauck MA, Meier JJ. Incretin hormones: their role in health and disease. Diabetes Obes Metab. 2018;20(suppl 1):5-21. https://doi.org/10.1111/dom.13129
2Samms RJ, Coghlan MP, Sloop KW. How may GIP enhance the therapeutic efficacy of GLP-1? Trends Endocrinol Metab. 2020;31(6):410-421. https://doi.org/10.1016/j.tem.2020.02.006
3Holst JJ. Incretin hormones and the satiation signal. Int J Obes (Lond). 2013;37(9):1161-1168. https://doi.org/10.1038/ijo.2012.208
4Holst JJ. GLP-1 physiology in obesity and development of incretin-based drugs for chronic weight management. Nat Metab. 2024;6(10):1866-1885. https://doi.org/10.1038/s42255-024-01113-9
5Foundayo [package insert]. Indianapolis, IN: Eli Lilly and Company; 2026.
6Kawai T, Sun B, Yoshino H, et al. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proc Natl Acad Sci U S A. 2020;117(47):29959-29967. https://doi.org/10.1073/pnas.2014879117
Date of Last Review: April 01, 2026