If you wish to report an adverse event or product complaint, please call 1-800-LILLYRX (1-800-545-5979)
Orforglipron-Obesity
This information is provided in response to your request. Resources may contain information about doses, uses, formulations and populations different from product labeling.
What is orforglipron?
Orforglipron is a chemically synthesized, non-peptide glucagon-like peptide-1 receptor agonist designed for daily oral administration.
Orforglipron Molecular Description
Orforglipron is a chemically synthesized, non-peptide glucagon-like peptide-1 (GLP-1) receptor agonist designed for daily oral administration.1
Orforglipron is an investigational molecule and is not currently approved in the United States.2
The structure of orforglipron is presented in Orforglipron Structure.
Receptor Activation
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.3
There is no evidence linking preclinical receptor pharmacology results of biased agonism towards cAMP accumulation with clinical efficacy in humans.
Bioavailability
In a phase 1 study of healthly adult participants, the absolute oral bioavailability of orforglipron was 79.1% following a single 1 mg oral capsule dose of orforglipron with approximately 240 mL of water. 4
Participants completed an overnight fast of at least 10 hours, and remained fasted for approximately 2 hours post oral dose.4
Half-Life
Metabolism
Orforglipron undergoes hepatic oxidative metabolism primarily via CYP3A4, with minimal contribution of reductive metabolism of orforglipron and oxidative metabolites in the gut.4
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
2Medicines in development. Eli Lilly and Company. Clinical Development Pipeline website. Accessed May 1, 2025. https://www.lilly.com/pipeline
3Kawai 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
4Morse 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: September 19, 2025