Orforglipron

A small-molecule, non-peptide GLP-1 receptor agonist taken as a once-daily tablet. It is not a peptide. In April 2026 the US FDA approved it as FOUNDAYO for weight management, after phase 3 trials; its registration status in Vietnam could not be confirmed from the public DAV lookup as of September 2026.

Last updated: September 2026

What is Orforglipron?

Orforglipron is a small-molecule, non-peptide GLP-1 receptor agonist taken by mouth. It is not a peptide: the US FDA label gives orforglipron calcium the molecular formula C48H47F2N10O5.[0.5]Ca and a molecular weight of 902.0 g/mol, which is small-molecule scale, and describes it as a GLP-1 receptor agonist that binds and activates the human GLP-1 receptor. It is one of the first molecules in the emerging class of non-peptide GLP-1 receptor agonists (PMID 39693407), and its development code was LY3502970. It appears in our peptide library only because readers look for it alongside the injectable peptide GLP-1 drugs.

In April 2026 the US FDA approved orforglipron as FOUNDAYO under NDA 220934, with an approval letter signed 1 April 2026 by Lisa B. Yanoff, MD. The approved use is weight management: in combination with a reduced-calorie diet and increased physical activity, to reduce excess body weight and maintain the reduction long term in adults with obesity, or adults with overweight who also have at least one weight-related condition. The manufacturer is Eli Lilly and Company. No fetched source shows a separate approved type 2 diabetes indication, even though several trials studied diabetes.

Unlike the injectable peptide GLP-1 drugs such as semaglutide, orforglipron is a once-daily tablet taken with or without food, and that oral route is the main reason it draws attention. Its availability in Vietnam is not established from public sources as of 6 September 2026, and no Vietnamese retail price was found. For the injectable GLP-1 that Vietnamese readers ask about most, see our semaglutide in Vietnam guide.

How It Works

Receptor pharmacology: orforglipron is a high-affinity, selective ligand of the human GLP-1 receptor, with an inhibition constant (Ki) of about 1 nM, low intrinsic efficacy for effector activation and negligible beta-arrestin recruitment (PMID 39693407).

Appetite pathway: the FDA label states that GLP-1 regulates appetite and calorie intake, that GLP-1 receptors sit in brain regions controlling appetite, and that in animal studies orforglipron distributed to and activated neurons in those regions; the label says the drug reduces body weight with greater fat mass loss than lean mass loss and decreases food intake (FDA label, NDA 220934).

Pharmacokinetics: the label reports maximum concentration 4 to 8 hours after a dose, dose-proportional exposure, a geometric mean absolute bioavailability of 77% after a 0.8 mg dose, and an elimination half-life of about 29 to 49 hours; a dedicated mass-balance study measured mean absolute oral bioavailability of 79.1%, with most of the drug cleared in feces (FDA label; PMID 40888509).

Metabolism and dosing convenience: orforglipron is metabolised mainly by hepatic CYP3A4, which is why the label caps the dose with strong CYP3A4 inhibitors and says to avoid strong inducers; its long half-life allows once-daily oral dosing without food or water restrictions (FDA label; PMID 37344954).

Benefits

Phase 3 ATTAIN-1, obesity without diabetes: mean body weight change at week 72 was -7.5% at the 6 mg dose, -8.4% at 12 mg and -11.2% at 36 mg, versus -2.1% with placebo; 54.6% of the 36 mg group lost 10% or more and 18.4% lost 20% or more (phase 3 trial result, PMID 40960239)
Phase 3 ATTAIN-2, obesity with type 2 diabetes: mean body weight change at week 72 was -5.1% at 6 mg, -7.0% at 12 mg and -9.6% at 36 mg, versus -2.5% with placebo (phase 3 trial result, PMID 41275875)
Phase 3 ACHIEVE-1, early type 2 diabetes: HbA1c change at week 40 was -1.24 to -1.48 percentage points across the three doses, versus -0.41 with placebo (phase 3 trial result, PMID 40544435)
Phase 2 obesity: a 10% or greater weight reduction by week 36 occurred in 46 to 75% of orforglipron participants versus 9% with placebo (phase 2 trial result, PMID 37351564)
Meta-analysis of five RCTs (4410 participants): dose-dependent placebo-comparator weight reduction from 2.48% at 3 mg to 9.8% at 45 mg, with HbA1c reductions of 0.76% to 1.04% (pooled analysis, not a recommendation, PMID 41296780)
Meta-analysis of three RCTs (774 people, up to 36 weeks): placebo-adjusted weight reduction of 5.48% at 12 mg to 8.84% at 36 mg; the review authors judged 24 to 36 mg the most optimal anti-obesity dose on efficacy versus side effects (pooled analysis, not a recommendation, PMID 38414573)
Exploratory analysis of the two phase 2 trials: significant placebo-adjusted decreases in blood pressure, LDL cholesterol, triglycerides, ApoB, ApoC3 and hsCRP; this was a biomarker analysis, not a cardiovascular outcomes trial (exploratory analysis, PMID 40481478)
A 2025 narrative review summarises HbA1c reduction up to 2.10%, weight reduction up to 10.1 kg and waist circumference reduction up to 8.7 cm in type 2 diabetes, and weight loss up to 13.0 kg in overweight or obesity (narrative review, PMID 41275408)

Dosing Described in Research and Labels

Phase	Dose	Frequency	Duration
Approved US label (FOUNDAYO, weight management)	Label schedule from 0.8 mg up to a maximum of 17.2 mg once daily (approved US label, not a recommendation, FDA NDA 220934)	Oral tablet once daily, with or without food, swallowed whole	Steps of 0.8, 2.5, 5.5, 9, 14.5 and 17.2 mg, at least 30 days apart (FDA label, revised 04/2026)
Phase 3 ATTAIN-1, obesity without diabetes	6, 12 or 36 mg once daily, investigational formulation (trial dose, not a recommendation, PMID 40960239)	Oral once daily, 3:3:3:4 versus placebo	72 weeks, n=3127 (PMID 40960239)
Phase 3 ATTAIN-2, obesity with type 2 diabetes	6, 12 or 36 mg once daily, investigational formulation (trial dose, not a recommendation, PMID 41275875)	Oral once daily, 1:1:1:2 versus placebo	72 weeks, n=1613 (PMID 41275875)
Phase 3 ACHIEVE-1, early type 2 diabetes	3, 12 or 36 mg once daily (trial dose, not a recommendation, PMID 40544435)	Oral once daily, 1:1:1:1 versus placebo	40 weeks, n=559 (PMID 40544435)
Phase 2 obesity without diabetes (GZGI)	12, 24, 36 or 45 mg once daily (trial dose, not a recommendation, PMID 37351564)	Oral once daily versus placebo	36 weeks, n=272 (PMID 37351564)
Phase 2 type 2 diabetes	3, 12, 24, 36 or 45 mg once daily (trial dose, not a recommendation, PMID 37369232)	Oral once daily, no food or water restriction; dulaglutide 1.5 mg comparator	26 weeks, n=383 (PMID 37369232)
Phase 1a, healthy adults	Single doses 0.3 to 6 mg; repeated dosing escalated to 2 to 24 mg (trial dose, not a recommendation, PMID 37344954)	Oral, single dose then 4 weeks daily	n=92 (PMID 37344954)
Phase 1b, type 2 diabetes	dose not stated in the abstract (trial dose, not a recommendation, PMID 37264711)	Oral daily, five dosing regimens, 3:1 versus placebo	12 weeks, n=51 orforglipron and 17 placebo (PMID 37264711)
Preclinical, humanized and gene-edited GLP-1R rodents	dose not stated in the abstract (animal study, mice and rats, oral orforglipron versus subcutaneous semaglutide, PMID 39693407)	Oral orforglipron compared with subcutaneous semaglutide	Diet-induced obesity model (PMID 39693407)
Animal safety, rat and mouse carcinogenicity	5, 30 and 200 mg/kg/day (animal study, rat 2-year and Tg.RasH2 mouse, oral, FDA NDA 220934)	Oral, daily	Rat 2 years, mouse 26 weeks; reported non-carcinogenic (FDA label, section 13.1)

Two milligram scales appear in this table and are not interchangeable. The phase 3 trials used an investigational formulation dosed at 6, 12 and 36 mg. The approved FOUNDAYO tablets are 0.8, 2.5, 5.5, 9, 14.5 and 17.2 mg, and the label restates the trial arms as equivalent dosages of 5.5, 9 and 17.2 mg, so label 5.5 mg maps to trial 6 mg, label 9 mg to trial 12 mg and label 17.2 mg to trial 36 mg. These figures summarise what published trials and the approved label describe. They are educational, not a recommendation or a personal protocol. Any dose or decision to use a compound belongs with a licensed prescriber.

Side Effects

Common

⚠Nausea, reported in 26% (5.5 mg), 34% (9 mg) and 35% (17.2 mg) of treated patients versus 10% on placebo (approved US label, FDA NDA 220934)
⚠Constipation 20% / 27% / 24%, diarrhea 21% / 23% / 25% and vomiting 13% / 21% / 24% across the 5.5, 9 and 17.2 mg doses, versus 9%, 11% and 4% on placebo (approved US label)
⚠Dyspepsia, abdominal pain, headache, abdominal distension, fatigue, eructation, gastroesophageal reflux disease, flatulence and hair loss were each reported in 5% or more of treated patients (approved US label)
⚠Overall gastrointestinal adverse reactions occurred in 60% (5.5 mg), 68% (9 mg) and 69% (17.2 mg) versus 37% on placebo, mostly mild to moderate and mostly during dose escalation (approved US label)

Rare

•Boxed warning: risk of thyroid C-cell tumors. The label notes orforglipron is not pharmacologically active in rats or mice and did not produce tumors in rodents, and that the human relevance of the class finding is undetermined (approved US label)
•Labeled warnings and precautions also include acute pancreatitis, severe gastrointestinal reactions, acute kidney injury from volume depletion, hypoglycemia, hypersensitivity reactions, diabetic retinopathy complications in type 2 diabetes, acute gallbladder disease, and pulmonary aspiration during general anesthesia or deep sedation (approved US label)
•Hypoglycemia in the type 2 diabetes trial: glucose below 54 mg/dL in 2% on orforglipron versus 0.2% on placebo, rising to 7% when combined with a sulfonylurea (approved US label)
•Permanent discontinuation for adverse reactions: 8% overall on orforglipron (6% at 5.5 mg, 9% at 9 mg, 10% at 17.2 mg) versus 3% on placebo, in a pool of 3155 patients treated up to 72 weeks (approved US label)

Contraindications, Warnings and Cautions

✕Personal or family history of medullary thyroid carcinoma (MTC), or Multiple Endocrine Neoplasia syndrome type 2 (MEN 2): the label lists this as a contraindication and carries a boxed warning about thyroid C-cell tumors (FDA label).
✕Known serious hypersensitivity to orforglipron or any of its excipients (FDA label contraindication).
✕Pregnancy: the label says it may cause fetal harm and to discontinue when pregnancy is recognized (FDA label).
✕Use with another GLP-1 receptor agonist: the label says concomitant use with another GLP-1 receptor agonist is not recommended (FDA label limitation of use).
✕Severe hepatic impairment: the label says use is not recommended (FDA label).
✕Oral contraceptive users: the label advises switching to a non-oral method or adding a barrier method for 30 days after starting and after each dose increase, because delayed gastric emptying can affect oral drug absorption (FDA label).

What to Expect

Weeks 0 to 4

The approved label schedule begins at a low starting dose and steps up no sooner than every 30 days. Nausea, vomiting and diarrhea were most frequent during this dose-escalation window and decreased over time (approved US label).

Weeks 26 to 40

The phase 2 trials measured their primary endpoints between weeks 26 and 36: HbA1c at week 26 in type 2 diabetes and body weight at weeks 26 and 36 in obesity; phase 3 ACHIEVE-1 measured its primary HbA1c endpoint at week 40 in early type 2 diabetes (trial timepoints, PMID 37369232, PMID 37351564, PMID 40544435).

Week 72

The two pivotal phase 3 obesity trials, ATTAIN-1 and ATTAIN-2, measured their primary body-weight endpoint at week 72 (trial timepoints, PMID 40960239, PMID 41275875).

Longer term

No fetched source reports a completed cardiovascular outcomes trial for orforglipron; the cardiovascular biomarker data come from an exploratory analysis of two phase 2 trials, not an outcomes trial (exploratory analysis, PMID 40481478).

Notes from Ho Chi Minh City

The orforglipron question in HCMC is different from the injectable GLP-1 questions, because this one is a pill, not a shot, and people ask whether they can pick it up at Long Chau the way they ask about semaglutide. On the day I checked, the honest answer was that no Vietnamese pharmacy search I could read listed it, and no local price existed to quote. Vietnamese-language coverage of the US approval went up in April 2026, which is usually the first sign a compound is about to be asked about a lot. Whether and when it reaches a Vietnamese shelf is a regulatory question, and whether anyone should take it is a licensed prescriber's call, not a pharmacy-counter one.

Sourcing in Vietnam

Availability in Vietnam is not established from public sources as of 6 September 2026. FOUNDAYO (orforglipron) is approved in the United States, and it is not confirmed registered with the Drug Administration of Vietnam; the DAV public marketing-authorisation lookup could not be queried directly, so no registration record was retrieved either way, which is a tooling limit, not proof of absence. Long Chau's on-site search returns other diabetes products and no orforglipron or FOUNDAYO listing, and Pharmacity's search returns no product record; An Khang's site did not respond to this check. No Vietnamese retail price is published anywhere we could read. Because orforglipron is a prescription medicine, there is no research-chemical vendor market to review and no community price range to quote.

FAQ

Q: Is orforglipron a peptide?

A: No. Orforglipron is a small-molecule, non-peptide GLP-1 receptor agonist; orforglipron calcium has the molecular formula C48H47F2N10O5.[0.5]Ca and a molecular weight of 902.0 g/mol, which is small-molecule scale (FDA label). It is grouped with peptide GLP-1 drugs on this site only because people search for them together. Unlike the injectable peptide GLP-1 agonists, it is taken as a daily tablet.

Q: Is orforglipron approved?

A: In the United States, yes: the FDA approved it as FOUNDAYO on 1 April 2026 under NDA 220934, for weight management in adults with obesity, or overweight with at least one weight-related condition, alongside a reduced-calorie diet and more physical activity (FDA approval letter and label). No fetched source shows a separate approved type 2 diabetes indication, even though the trials studied diabetes.

Q: Why are the milligram doses in the trials different from the tablet strengths?

A: The phase 3 trials used an investigational formulation dosed at 6, 12 and 36 mg. The approved FOUNDAYO tablets are 0.8, 2.5, 5.5, 9, 14.5 and 17.2 mg, and the label restates the trial arms as equivalent dosages of 5.5, 9 and 17.2 mg. So label 5.5 mg maps to trial 6 mg, label 9 mg to trial 12 mg, and label 17.2 mg to trial 36 mg. The two milligram scales are not interchangeable (FDA label; PMID 40960239; PMID 41275875).

Q: Can I buy orforglipron in Vietnam?

A: As of 6 September 2026 we found no orforglipron or FOUNDAYO listing on Long Chau or Pharmacity and no Vietnamese retail price anywhere. An Khang's site did not respond to our check, and the Drug Administration of Vietnam lookup could not be queried, so we are not claiming it is unregistered, only that no record was retrieved. For the injectable GLP-1 that people ask about most, see our semaglutide in Vietnam guide.

Q: What are the most common side effects?

A: In the pooled approved-label trials the most common adverse reactions were gastrointestinal: nausea in 26 to 35% of treated patients versus 10% on placebo, plus constipation, diarrhea and vomiting, mostly mild to moderate and mostly during dose escalation. The label also carries a boxed warning about thyroid C-cell tumors seen with this drug class in rodents, though orforglipron itself did not produce tumors in rodents and the human relevance is undetermined (FDA label).

Availability of Orforglipron in Vietnam

Orforglipron is a prescription medicine approved in the United States as FOUNDAYO. As of 6 September 2026 we found no Vietnamese retail listing or price, and its Drug Administration of Vietnam registration status could not be confirmed from the public lookup. There is no research-chemical vendor market to review for this compound. For the injectable GLP-1 that Vietnamese readers ask about most, see the semaglutide guide.

Read the Semaglutide in Vietnam guide Back to the peptide library

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Peptide Library Semaglutide in Vietnam HGH & GLP-1 Peptides

Research & Sources

Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment · N Engl J Med (2025) (PMID: 40960239)
Phase 3 ATTAIN-1 obesity trial, n=3127, 72 weeks; investigational doses 6, 12 and 36 mg. NCT05869903, the FDA label Trial 1.
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 (2026) (PMID: 41275875)
Phase 3 ATTAIN-2, n=1613, 72 weeks; investigational doses 6, 12 and 36 mg. NCT05872620, the FDA label Trial 2.
Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist, in Early Type 2 Diabetes · N Engl J Med (2025) (PMID: 40544435)
Phase 3 ACHIEVE-1, n=559, 40 weeks; doses 3, 12 and 36 mg. NCT05971940.
Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity · N Engl J Med (2023) (PMID: 37351564)
Phase 2 obesity (GZGI), n=272, 36 weeks; doses 12, 24, 36 and 45 mg. NCT05051579.
Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study · Lancet (2023) (PMID: 37369232)
Phase 2 type 2 diabetes, n=383, 26 weeks; doses 3, 12, 24, 36 and 45 mg. NCT05048719.
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 Obes Metab (2023) (PMID: 37344954)
Phase 1a, n=92; single doses 0.3 to 6 mg, repeated dosing escalated to 2 to 24 mg.
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) (PMID: 37264711)
Phase 1b, n=51 orforglipron and 17 placebo, 12 weeks; specific milligram doses not stated in the abstract.
The pharmacological basis for nonpeptide agonism of the GLP-1 receptor by orforglipron · Sci Transl Med (2024) (PMID: 39693407)
Receptor pharmacology and animal work; Ki about 1 nM. Animal doses not stated in the abstract.
Disposition and Absolute Bioavailability of Orally Administered Orforglipron in Healthy Participants · Clin Pharmacol Drug Dev (2026) (PMID: 40888509)
Absolute oral bioavailability 79.1%; most of the dose recovered in feces.
Efficacy and Safety of Orforglipron in Obese Adults With or Without Diabetes: A Systematic Review and Meta-Analysis · Endocrinol Diabetes Metab (2025) (PMID: 41296780)
Five RCTs, 4410 participants; dose-dependent weight reduction 2.48% at 3 mg to 9.8% at 45 mg.
Orforglipron, a novel non-peptide oral daily glucagon-like peptide-1 receptor agonist as an anti-obesity medicine: A systematic review and meta-analysis · Obes Sci Pract (2024) (PMID: 38414573)
Three RCTs, 774 people; placebo-adjusted weight reduction 5.48% at 12 mg to 8.84% at 36 mg.
Treatment with orforglipron, an oral glucagon like peptide-1 receptor agonist, is associated with improvements of CV risk biomarkers in participants with type 2 diabetes or obesity without diabetes · Cardiovasc Diabetol (2025) (PMID: 40481478)
Exploratory post hoc analysis of two phase 2 trials, not a cardiovascular outcomes trial.
Orforglipron in type 2 diabetes mellitus and obesity: an overview · Expert Rev Clin Pharmacol (2025) (PMID: 41275408)
Narrative review; summarises HbA1c, weight and waist changes across the program.
FOUNDAYO (orforglipron) tablets, US Prescribing Information (NDA 220934) · US FDA, Center for Drug Evaluation and Research · FDA approved labeling (2026) Link
Revised 04/2026. Tablet strengths 0.8 to 17.2 mg; the label restates investigational trial arms of 6, 12 and 36 mg as equivalent dosages of 5.5, 9 and 17.2 mg. Source of the boxed warning and adverse-reaction tables.
NDA 220934 Approval Letter, Foundayo (orforglipron) tablets · US FDA, Center for Drug Evaluation and Research · FDA approval letter (2026) Link
Application received 20 January 2026; approved 1 April 2026 for weight management. Reference ID 5773652.

Important Disclaimer

Educational content only, not medical advice. Orforglipron is a small-molecule GLP-1 receptor agonist, not a peptide; it is covered here because readers look for it alongside peptide GLP-1 drugs. It is approved in the United States as FOUNDAYO for weight management (FDA NDA 220934). Its registration status with the Drug Administration of Vietnam (DAV, Cuc Quan ly Duoc) could not be confirmed from the public lookup as of 6 September 2026, and no Vietnamese retail listing or price was found at Long Chau or Pharmacity. This page reports what published trials and the approved label describe; it does not recommend any dose. Consult a licensed physician before any use.