Orforglipron

Orforglipron is not a peptide. It is indexed alongside Incretin receptor agonists because it appears in the same research literature and the same search demand; no statement on this site describes it as a peptide.

Identity

Measured identity values, each with the source that reports it
FieldValue
ClassificationNot a peptide
Primary classIncretin receptor agonists
CAS registry number2212020-52-3[1]
PubChem CID137319706[1]
UniProt accessionUnknown No UniProt query was run in v1.
Molecular formulaC48H48F2N10O5[1]
Molecular weight883 g/mol[1]
Amino-acid sequenceUnknown Not reported by the PubChem property set retrieved for this record; no sequence database query was run in v1.
Reported half-lifeUnknown No pharmacokinetics source was retrieved in v1. PubChem does not carry half-life as a property, so this is recorded as not yet sourced rather than estimated.

What the cited literature examines

Orforglipron is not a peptide: it is an oral small-molecule GLP-1 receptor agonist, indexed here because it acts at the same receptor as the peptide members of the class. A 2020 Proceedings of the National Academy of Sciences paper reports the structural basis for GLP-1 receptor activation by LY3502970 as an orally active nonpeptide agonist, and a 2024 Science Translational Medicine paper reports the pharmacological basis for nonpeptide agonism of the receptor. The Drugs@FDA register returned an approved application under this generic name, recorded in the regulatory status field and not what this page describes.

Clinical records include 2023 Diabetes, Obesity and Metabolism phase 1a and 1b studies, a 2023 New England Journal of Medicine paper on daily oral administration in adults with obesity, a 2023 Lancet dose-response study in type 2 diabetes, 2025 New England Journal of Medicine papers in early type 2 diabetes and in obesity, and a 2026 Lancet comparison with oral semaglutide in type 2 diabetes.

[3, 4, 5, 6, 7, 8, 9, 10, 11]

Reported mechanism

A non-peptide oral GLP-1 receptor agonist; the retrieved records report the structural basis of receptor activation.

[3, 4]

Stated in the titles of the cited 2020 Proceedings of the National Academy of Sciences and 2024 Science Translational Medicine papers.

Targets named in the cited records: GLP-1 receptor.

FDA application register

A query of the FDA Drugs@FDA application register on 2026-10-09 returned 1 application record(s) for this compound name (including NDA220934, marketed as FOUNDAYO). Material supplied as a research chemical is not the subject of those applications and is not an FDA-approved product.[2]

Scope statement: this records the result of a single automated query against the openFDA drugsfda endpoint on the stated date. It is not legal advice and is not a jurisdiction-by-jurisdiction legality assessment.

Retrieved 2026-10-09.

Amounts reported in the cited literature

Unknown. No retrieved record in this dataset states an amount, so none is shown. Where an amount is recorded it is what a named study reported administering in its own stated model, in the past tense, and is not a protocol.

No study-reported dose was taken from a source read in v1. Literature-reported values are only recorded where the retrieved citation metadata states the figure.

Adverse effects reported in the cited literature

Unknown. No retrieved record in this dataset reports an adverse effect for this compound, so no row is shown. Absence of a row records the absence of a retrieved report, nothing more.

No adverse-effect row was taken from a source read in v1. Rows are only recorded with the study model named and the reporting citation attached.

Other names

Orforglipron appears under these other names in the cited records or in common usage. Each one resolves to this page rather than to a separate page of its own.

Where this page sits

Research records

Cited research records for Orforglipron, each with its identifier, the publication type it is indexed as, and the study model stated by its assigned subject headings.

Compounds indexed next to it

Named targets in the cited records

Class page: Incretin receptor agonists. Full index: all indexed compounds.

Questions this page answers

What does the cited literature examine for Orforglipron?

Orforglipron is not a peptide: it is an oral small-molecule GLP-1 receptor agonist, indexed here because it acts at the same receptor as the peptide members of the class. A 2020 Proceedings of the National Academy of Sciences paper reports the structural basis for GLP-1 receptor activation by LY3502970 as an orally active nonpeptide agonist, and a 2024 Science Translational Medicine paper reports the pharmacological basis for nonpeptide agonism of the receptor.

Which class is Orforglipron indexed under?

Orforglipron is indexed under Incretin receptor agonists. Incretin receptor agonists are synthetic peptides that bind one or more of the incretin and glucagon family receptors, principally the glucagon-like peptide-1 receptor.

What does the FDA application register show for Orforglipron?

A query of the FDA Drugs@FDA application register on 2026-10-09 returned 1 application record(s) for this compound name (including NDA220934, marketed as FOUNDAYO). Material supplied as a research chemical is not the subject of those applications and is not an FDA-approved product.

Sources

  1. PubChem Compound Summary for CID 137319706, Orforglipron. PubChem, National Library of Medicine (2026). pubchem:137319706
  2. Drugs@FDA application register query for this compound, 1 application(s) returned: NDA220934. U.S. Food and Drug Administration, openFDA drugsfda endpoint (2026). fda:orforglipron
  3. Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist. Proceedings of the National Academy of Sciences of the United States of America (2020). pmid:33177239
  4. The pharmacological basis for nonpeptide agonism of the GLP-1 receptor by orforglipron. Science translational medicine (2024). pmid:39693407
  5. Orforglipron (LY3502970), a novel, oral non-peptide glucagon-like peptide-1 receptor agonist: A Phase 1a, blinded, placebo-controlled, randomized, single- and multiple-ascending-dose study in healthy participants. Diabetes, obesity & metabolism (2023). pmid:37344954
  6. 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, obesity & metabolism (2023). pmid:37264711
  7. Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity. The New England journal of medicine (2023). pmid:37351564
  8. Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study. Lancet (London, England) (2023). pmid:37369232
  9. Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist, in Early Type 2 Diabetes. The New England journal of medicine (2025). pmid:40544435
  10. Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment. The New England journal of medicine (2025). pmid:40960239
  11. Efficacy and safety of once-daily oral orforglipron compared with oral semaglutide in adults with type 2 diabetes (ACHIEVE-3): a multinational, multicentre, non-inferiority, open-label, randomised, phase 3 trial. Lancet (London, England) (2026). pmid:41765029

On each stated value was matched to the record cited for it. That is record matching, not an appraisal of the research. Compiled and checked by: Peptide Monographs editorial desk. No qualified clinical reviewer.

Further reading