Orforglipron
Also known as: Foundayo, LY3502970, Non-peptide oral GLP-1
Orforglipron (also called Foundayo or LY3502970) is an FDA-approved oral small-molecule GLP-1 agonist. Orforglipron is a non-peptide small molecule that activates the GLP-1 receptor. Because it is not a peptide it is not degraded by gastrointestinal proteases, so unlike oral semaglutide it needs no absorption enhancer and can be taken without restrictions on food, water or timing.
For research use only.
Key Facts
- CAS
- 2212020-52-3
- Molecular Weight (MW)
- 883 g/mol
- Half-life
- —
- FDA status
- Approved
- Administration Route
- Oral
- Frequency
- Once daily
- Last updated
- Aug 30, 2026
- Reviewed
- Aug 30, 2026
- Targets
- GLP-1 receptor
Research summary
FDA-approved April 1, 2026 (Foundayo). Once-daily non-peptide oral GLP-1 receptor agonist for chronic weight management without food or water timing restrictions.
Peptide Library's Orforglipron profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.
Protocol
- Dosage Range
- Once-daily oral titration per Foundayo label
- Frequency
- Once daily
- Cycle
- Long-term as prescribed
- Administration Route
- Oral
- Reconstitution Guide
- Tablet — no reconstitution
- Timing Notes
- Educational catalog only — not medical advice
Not yet checked against primary sources
These figures are compiled from earlier reference material. They have not been verified against FDA labelling, registered trials or published literature, no citation is attached to them, and none of them is a recommended dose. Orforglipron is queued for dosage evidence review.
Compare reported doses across the whole librarySequence & molecular data
| Molecular formula | C48H48F2N10O5 |
|---|---|
| Molecular weight | 883 g/mol |
| CAS number | 2212020-52-3 |
| Appearance | Oral tablet |
| Formulation | Oral tablet |
| PubChem CID | 137319706 |
| ChEMBL | CHEMBL4446782 |
Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.
Science
Mechanism of Action
Orforglipron is a non-peptide small molecule that activates the GLP-1 receptor. Because it is not a peptide it is not degraded by gastrointestinal proteases, so unlike oral semaglutide it needs no absorption enhancer and can be taken without restrictions on food, water or timing. It binds an allosteric site on the GLP-1 receptor distinct from the orthosteric peptide-binding pocket and shows biased signalling, favouring the cyclic AMP pathway over beta-arrestin recruitment, which limits receptor internalisation. Downstream pharmacology is conventional for the class: glucose-dependent insulin secretion, glucagon suppression, slowed gastric emptying and centrally mediated appetite reduction.
Origin
Discovered by Chugai; developed by Lilly.
Targets
Studies
- Safety and efficacy of the new, oral, small-molecule, GLP-1 receptor agonists orforglipron and danuglipron for the treatment of type 2 diabetes and obesity: systematic review and meta-analysis of randomized controlled trials
- 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
- Orforglipron, an oral small-molecule GLP-1 receptor agonist, for the treatment of obesity in people with type 2 diabetes (ATTAIN-2): a phase 3, double-blind, randomised, multicentre, placebo-controlled trial
- Orforglipron for maintenance of body weight reduction: the double-blind, randomized phase 3b ATTAIN-MAINTAIN trial
- Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment
Regulatory & research status
Orforglipron is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines.
| FDA status | Approved |
|---|---|
| Availability | Prescription-Only |
| WADA (sport) | Permitted |
| Library classification | FDA-Approved |
Benefits
Potential Side Effects
Side Effects
- GI class effects
Storage & stability
Lyophilized (freeze-dried) peptide powder is far more stable than the reconstituted solution. Keep sealed vials cold, dry and away from light; long-term storage is typically frozen, with short-term refrigeration for vials in use.
Once reconstituted in bacteriostatic water, keep the solution refrigerated, avoid repeated freeze–thaw cycles and agitation, and label the vial with the reconstitution date and concentration. Discard any solution that turns cloudy or shows particulates.
Degradation rates differ by sequence: peptides containing methionine, cysteine, asparagine or glutamine are more prone to oxidation and deamidation, so shelf life after reconstitution is compound-specific rather than universal.
Read the full guide: how to store peptides before and after reconstitution →
Source: Manning MC, Chou DK, Murphy BM, Payne RW, Katayama DS. Stability of protein pharmaceuticals: an update. Pharm Res. 2010;27(4):544–575. (PMID 20143256). General guidance for research handling; not product-specific instructions.
Orforglipron: frequently asked questions
What is Orforglipron?
FDA-approved April 1, 2026 (Foundayo). Once-daily non-peptide oral GLP-1 receptor agonist for chronic weight management without food or water timing restrictions.
How does Orforglipron work?
Orforglipron is a non-peptide small molecule that activates the GLP-1 receptor. Because it is not a peptide it is not degraded by gastrointestinal proteases, so unlike oral semaglutide it needs no absorption enhancer and can be taken without restrictions on food, water or timing.
Is Orforglipron FDA approved?
Yes. Orforglipron is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product.
Is Orforglipron banned in sport?
Orforglipron is recorded here as permitted in sport. Anti-doping status is revised annually, so athletes subject to testing should confirm against the current WADA Prohibited List before use.
What peptides are similar to Orforglipron?
Compounds most often compared with Orforglipron include Semaglutide, Tirzepatide, Retatrutide and Liraglutide. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ.
References
- FDA — approval of Foundayo (orforglipron), 2026External reference
- Safety and efficacy of the new, oral, small-molecule, GLP-1 receptor agonists orforglipron and danuglipron for the treatment of type 2 diabetes and obesity: systematic review and meta-analysis of randomized controlled trials — Metabolism, 2023External reference
- 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, 2026External reference
- Orforglipron, an oral small-molecule GLP-1 receptor agonist, for the treatment of obesity in people with type 2 diabetes (ATTAIN-2): a phase 3, double-blind, randomised, multicentre, placebo-controlled trial — Lancet, 2026External reference
- Orforglipron for maintenance of body weight reduction: the double-blind, randomized phase 3b ATTAIN-MAINTAIN trial — Nat Med, 2026External reference
- Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment — N Engl J Med, 2025External reference
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Aug 30, 2026 · Version 1
This Orforglipron profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error
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