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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 Foundayo™ (orforglipron)?
Foundayo contains orforglipron, a small molecule GLP-1 receptor agonist. It is used with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long-term in adults with obesity or overweight.
See important safety information, including boxed warning, in the attached prescribing information.
Content Overview
What Is the Molecular Description of Orforglipron?
Orforglipron is a novel small-molecule, non-peptide GLP-1 receptor agonist designed for once-daily oral administration with or without food and water restrictions.1-3
Orforglipron is approved in the US under the brand name Foundayo in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in adults with
- obesity, or
- overweight in the presence of at least one weight-related comorbid condition.4
Orforglipron is a non-peptide molecule, meaning it is chemically synthesized and not built from an amino acid chain.2,5,6
The chemical structure of orforglipron calcium is presented in Chemical Structure of Orforglipron Calcium.
What Receptors does Orforglipron Activate?
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.2
There is no evidence linking preclinical receptor pharmacology results of biased agonism towards cAMP accumulation with clinical efficacy in humans.
What is the Mechanism of Action of Orforglipron?
Orforglipron is a GLP-1 receptor agonist that binds to and activates the human GLP-1 receptor.4
GLP-1 is a physiological regulator of appetite and caloric intake. GLP-1 receptors are present in brain regions that regulate appetite. In animal studies, orforglipron distributed to and activated neurons in brain regions that regulate appetite and food intake.4
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.4
Orforglipron delays gastric emptying. The delay is largest after the first dose and diminishes over time.4
What is the Bioavailability of Orforglipron?
In a phase 1 study of healthy adult participants, the arithmetic mean absolute bioavailability of orforglipron was 79.1% following a single 0.8 mg oral dose of orforglipron with approximately 240 mL of water. The geometric mean absolute bioavailability of orforglipron was 77% after a 0.8 mg dose.4,7
Participants completed an overnight fast of at least 10 hours, and remained fasted for approximately 2 hours post oral dose.7
What is the Half-Life of Orforglipron
The elimination half-life is approximately 29 to 49 hours after an oral dose.4
How is Orforglipron Metabolised?
Orforglipron is metabolized primarily via hepatic CYP3A4 to several oxidative metabolites. These oxidative metabolites are excreted into the intestinal lumen.4,7
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Enclosed Prescribing Information
References
The published references below are available by contacting 1-800-LillyRx (1-800-545-5979).
1Pratt E, Ma X, Liu R, et al. Orforglipron (LY3502970), a novel, oral non-peptide glucagon-like peptide-1 receptor agonist: a phase 1b, multicentre, blinded, placebo-controlled, randomized, multiple-ascending-dose study in people with type 2 diabetes. Diabetes Obes Metab. 2023;25(9):2642-2649. https://doi.org/10.1111/dom.15150
2Kawai 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
3Wharton S, Blevins T, Connery L, et al; GZGI Investigators. Daily oral GLP-1 receptor agonist orforglipron for adults with obesity. N Engl J Med. 2023;389(10):877-888. https://doi.org/10.1056/NEJMoa2302392
4Foundayo [package insert]. Indianapolis, IN: Eli Lilly and Company; 2026.
5Ma X, Liu R, Pratt EJ, et al. Effect of food consumption on the pharmacokinetics, safety, and tolerability of once-daily orally administered orforglipron (LY3502970), a non-peptide GLP-1 receptor agonist. Diabetes Ther. 2024;15:819-832. https://doi.org/10.1007/s13300-024-01554-1
6Frias JP, Hsia S, Eyde S, et al. Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study. Lancet. 2023;402(10400):472-483. https://doi.org/10.1016/S0140-6736(23)01302-8
7Morse BL, Bhattachar S, Ma X, et al. Disposition and absolute bioavailability of orally administered orforglipron in healthy participants. Clin Pharmacol Drug Dev. Published online September 1, 2025. https://doi.org/10.1002/cpdd.1594
Date of Last Review: April 01, 2026