Orforglipron

Fat LossFDA-approved oral small-molecule GLP-1 agonistEstablished

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.

Calculate Dose

For research use only.

Key Facts

CAS: 2212020-52-3
Molecular Weight (MW): 883 g/mol
Half-life: Approximately 29–49 hours after an oral dose; steady state after about 1 week of daily dosing
FDA status: Approved
Evidence level: FDA Approved
Human dose established: Yes
Administration Route: Oral
Frequency: Once daily, with or without food
Last updated: Oct 5, 2026
Reviewed: Aug 30, 2026
Targets: GLP-1 receptor

Vendor price snapshot

Each vendor counts once, at the median price per mg of its own listings; the typical range is the middle half of vendors. From public vendor listings collected in Oct 2026, so confirm the live price on the vendor site. Peptide Library does not sell peptides.

Vendors listing this peptide: 6
Listed offers: 7
Median price per mg: $0.833/mg; Typical $0.665–$8.67/mg

Open calculator · Compare vendors

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.

Orforglipron dosage chart

Orforglipron has an FDA-approved human dosage. It was approved in April 2026 as FOUNDAYO, a once-daily oral tablet for reducing excess body weight and maintaining the reduction long term in adults with obesity, or overweight with at least one weight-related condition. The label starts at 0.8 mg once daily and escalates after at least 30 days at each step, to 2.5 mg and then 5.5 mg; the dose may then be raised to 9 mg, 14.5 mg or 17.2 mg, and 17.2 mg once daily is the maximum. Orforglipron is a small-molecule, non-peptide GLP-1 receptor agonist taken with or without food, and there is no injectable form.

FDA Approved

Dosage evidence summary for Orforglipron
Human dosing established	Yes
Studied dose range	0.8–17.2 mg once daily (FOUNDAYO tablets)
Route	Oral
Frequency	Once daily, with or without food
Duration studied	Long term; at least 30 days at each dosage before escalating
Titration	0.8 mg once daily for at least 30 days, then 2.5 mg once daily for at least 30 days, then 5.5 mg once daily. After at least 30 days at the current dosage the dose may be raised to the next level (9 mg, 14.5 mg, then 17.2 mg) based on response and tolerability. Maximum 17.2 mg once daily. If 7 or more consecutive doses are missed, escalation restarts at a lower dosage.
Half-life	Approximately 29–49 hours after an oral dose; steady state after about 1 week of daily dosing
Evidence level	FDA Approved
Last reviewed	2026-10-05

Research-reported dosing

Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.

Research-reported dosing for Orforglipron, one row per studied regimen
Study / context	Population	Dose	Route	Frequency	Duration	Outcome studied	Source
FDA label — FOUNDAYO, weight reduction and long-term maintenanceFDA-approved label · FDA prescribing information	Adults with obesity, or with overweight and at least one weight-related comorbid condition	0.8 mg starting dose, escalated to 2.5 mg and then 5.5 mg; may be increased to 9 mg, 14.5 mg or 17.2 mg; maximum 17.2 mg	Oral tablet, swallowed whole	Once daily, with or without food	Long term, alongside a reduced-calorie diet and increased physical activity	Reduction of excess body weight and long-term maintenance of the reduction	FOUNDAYO (orforglipron) tablets — FDA prescribing information, DailyMed
ATTAIN-1 — phase 3 obesity trial without diabetes, investigational formulation (NCT05869903)Clinical trial · Phase 3 double-blind randomised placebo-controlled trial	Adults with obesity, or overweight with a weight-related condition, without diabetes (n=3127)	6 mg, 12 mg or 36 mg	Oral	Once daily	72 weeks	Percentage change in body weight at week 72 — −7.5%, −8.4% and −11.2% with 6, 12 and 36 mg versus −2.1% with placebo	Wharton S et al. Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment. N Engl J Med. 2025.
ATTAIN-2 — phase 3 obesity trial in type 2 diabetes, investigational formulation (NCT05872620)Clinical trial · Phase 3 double-blind randomised placebo-controlled trial	Adults with BMI ≥27 and type 2 diabetes with HbA1c 7–10% (n=1613)	6 mg, 12 mg or 36 mg	Oral	Once daily	72 weeks	Percentage change in body weight at week 72 — −5.1%, −7.0% and −9.6% with 6, 12 and 36 mg versus −2.5% with placebo	Horn DB et al. 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. 2025.
ACHIEVE-3 — phase 3 against oral semaglutide in type 2 diabetes (NCT06045221)Clinical trial · Phase 3 open-label randomised active-controlled non-inferiority trial	Adults with type 2 diabetes inadequately controlled with metformin, HbA1c 7.0–10.5% and BMI ≥25 (n=1698)	12 mg or 36 mg	Oral	Once daily	52 weeks	Change in HbA1c at week 52 versus oral semaglutide 7 mg and 14 mg — both orforglipron doses were non-inferior and superior, with more gastrointestinal events and more discontinuations due to adverse events	Rosenstock J et al. 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. 2026.

Where sources disagree

Orforglipron is not a peptide. It is a small-molecule, non-peptide GLP-1 receptor agonist, supplied as orforglipron calcium, and it is listed alongside peptides because it acts on the same receptor as semaglutide and tirzepatide. It is also not oral semaglutide (Rybelsus): that is a tablet form of a peptide, with a different molecule, label and dose scale.
There is no injectable orforglipron. FOUNDAYO is a film-coated tablet, and the label states it is only for oral use and describes orforglipron calcium as insoluble in water. No registered trial gives orforglipron by subcutaneous injection; the only non-oral dosing in the registered programme is an intravenous radiolabelled tracer in a phase 1 pharmacokinetic study (NCT06085482). Vials sold as orforglipron for reconstitution and injection are not the approved product, and no published study supports their dosing.
Trial doses and tablet strengths are not interchangeable milligram for milligram. The phase 3 trials used an investigational formulation and report doses of 6, 12 and 36 mg once daily; the FOUNDAYO label presents the same trial arms as equivalent dosages of 5.5, 9 and 17.2 mg. A trial figure such as 36 mg describes that formulation and is above the 17.2 mg label maximum, so it should not be read as a FOUNDAYO dose.
The FOUNDAYO label directs one tablet once daily with or without food, swallowed whole and not broken, crushed or chewed, and sets no fasting period or water limit. The oral semaglutide label requires an empty stomach with up to 4 ounces of water and a 30-minute wait before eating, so administration rules written for one should not be applied to the other.
The label's only indication is weight reduction and long-term weight maintenance in adults. Type 2 diabetes trials such as ACHIEVE-3 report glycaemic results, but as of the July 2026 label revision orforglipron is not approved for glycaemic control; people with type 2 diabetes appear on the label only within the weight-management indication (ATTAIN-2).
The 0.8 mg and 2.5 mg dosages are escalation steps, and the label's efficacy data come from arms equivalent to 5.5, 9 and 17.2 mg, so 14.5 mg is a labelled step without its own randomised arm in those trials. The label also lowers the maximum to 9 mg once daily alongside a strong CYP3A4 inhibitor, advises avoiding strong CYP3A4 inducers, and does not recommend use in severe hepatic impairment, so a single maximum dose depends on concomitant medicines.

Handling & administration

Reconstitution Guide: Tablet — no reconstitution
Timing Notes: Educational catalog only — not medical advice

Sequence & molecular data

Sequence and molecular data for Orforglipron
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

GLP-1 receptor

Studies

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.

Regulatory and research status for Orforglipron
FDA status	Approved
Availability	Prescription-Only
WADA (sport)	Permitted
Library classification	FDA-Approved

Benefits

Oral GLP-1 without peptide injectionNo food/water window like Rybelsus

Orforglipron side effects

The effects below are drawn from Orforglipron's prescribing information, which lists the full adverse-reaction data.

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?

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

Related research, comparisons & guides

Related peptides

Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Oct 5, 2026 · Version 2

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

Track Orforglipron research, inventory and reconstitution in the free Peptide Library app. Get the app for iOS or Android →