Entry 0029Rev 1.0Oral GLP-1 agonist, not a peptide

Orforglipron

Non-peptide small molecule · C48H48F2N10O5

Reviewed

2 Nov 2026

Scientific editor

[Name, PhD]

References

15 sources

Orforglipron is not a peptide. It is a small molecule, taken by mouth, that switches on the GLP-1 receptor, the same target as semaglutide. Chugai discovered it and licensed it to Eli Lilly in 2018.1,2

It sits in this library because it is compared with the peptides on this shelf. The FDA approved it for weight management as Foundayo on 1 April 2026, and the UK followed in August 2026.11,12

Type

Small molecule

Mass

883.0 g/mol

ATTAIN-1, top dose

−11.2% at 72 wk

Licensed

US, UK

01

Identity

Value
ClassNon-peptide small molecule, GLP-1 receptor agonist1
FormulaC48H48F2N10O5; marketed as the calcium salt1
Mass883.0 g/mol1
CAS2212020-52-31
OriginChugai Pharmaceutical (OWL833), licensed to Eli Lilly in 20182
Versus oral semaglutideOral semaglutide is a peptide that needs an absorption enhancer and an empty stomach. Orforglipron needs neither, and its label has no food or water restrictions.11,15
02

History

  1. Chugai licenses OWL833 to Lilly before first human trials.2

  2. Phase 2 in obesity and in type 2 diabetes published.3,4

  3. ACHIEVE-1 (type 2 diabetes), ATTAIN-1 and ATTAIN-2 (obesity) published.5,6,7

  4. ACHIEVE-3 shows better HbA1c control than oral semaglutide.8

  5. FDA approves it as Foundayo for chronic weight management.11

  6. The UK MHRA authorises it for weight management and type 2 diabetes.12

  7. EMA committee gives a positive opinion for both uses.13

03

What the trials measured

TrialPeopleDurationMain resultSource
ATTAIN-13,127 with obesity, no diabetes72 weeks−7.5%, −8.4% and −11.2% by dose vs −2.1% placebo[6]
ATTAIN-21,613 with obesity and type 2 diabetes72 weeks−5.1% to −9.6% vs −2.5% placebo[7]
ACHIEVE-1559 with early type 2 diabetes40 weeksHbA1c −1.24 to −1.48 points vs −0.41 placebo[5]
ACHIEVE-31,698 with type 2 diabetes, vs oral semaglutide52 weeksHbA1c −1.71 and −1.91 vs −1.23 and −1.47; superior[8]
ACHIEVE-42,749 with type 2 diabetes and high heart risk, vs insulin glargineAbout 2 yearsMajor heart events: non-inferior (HR 0.84)[9]
ATTAIN-MAINTAIN376 switched from injectable incretins52 weeksKept 75–79% of earlier weight loss vs 38–49% on placebo[10]

Side effects were gastrointestinal, as with injectable GLP-1 drugs. Against oral semaglutide, more people stopped for side effects (9–10% vs 4–5%).8

04

Regulatory and sport status

As of this revision.

WhereStatus
USApproved 1 April 2026 for chronic weight management; type 2 diabetes application pending.11
UKAuthorised 10 August 2026 for weight management and type 2 diabetes.12
EUPositive CHMP opinion 15 October 2026; awaiting the Commission decision.13
SportNot named on the 2026 WADA list or monitoring programme. As an approved medicine it does not fall under class S0.14
05

Open questions

  1. Heart outcomes in obesity without diabetes. ACHIEVE-4 tested safety in type 2 diabetes against insulin, not against placebo.9
  2. Tolerability against oral semaglutide, given more gastrointestinal stopping and a larger rise in pulse rate in ACHIEVE-3.8
  3. How well trial results carry over to the marketed tablets, which are a different formulation from the trial capsules.
06

Common questions

Is orforglipron a peptide?

No. It is a non-peptide small molecule that activates the GLP-1 receptor.

Who discovered it?

Chugai Pharmaceutical, as OWL833. Lilly licensed it in 2018.

When was it approved?

By the FDA on 1 April 2026 as Foundayo, for chronic weight management, and in the UK in August 2026.

Why is it in a peptide library?

Because it is compared with the incretin peptides on this shelf, and readers search for it alongside them.

Do you sell orforglipron?

No. It is a licensed medicine and not a peptide.

—

See also

Semaglutide Entry 0007Tirzepatide Entry 0008Retatrutide Entry 0005Metabolic Shelf
07

References

  1. PubChem CID 137319706 and KEGG DRUG D12536 / D12529 (orforglipron calcium), checked 3 Nov 2026.
  2. Chugai Pharmaceutical and Eli Lilly. Chugai and Lilly enter into a license agreement for oral GLP-1 agonist OWL833. 26 September 2018. chugai-pharm.co.jp
  3. Wharton S, et al. Daily oral GLP-1 receptor agonist orforglipron for adults with obesity. N Engl J Med. 2023;389(10):877–888. PMID 37351564
  4. Frias JP, et al. Efficacy and safety of oral orforglipron in patients with type 2 diabetes: a multicentre, randomised, dose-response, phase 2 study. Lancet. 2023;402(10400):472–483. PMID 37369232
  5. Rosenstock J, et al. Orforglipron, an oral small-molecule GLP-1 receptor agonist, in early type 2 diabetes. N Engl J Med. 2025;393(11):1065–1076. PMID 40544435
  6. Wharton S, et al. Orforglipron, an oral small-molecule GLP-1 receptor agonist for obesity treatment. N Engl J Med. 2025;393(18):1796–1806. PMID 40960239
  7. Horn DB, et al. Orforglipron for the treatment of obesity in people with type 2 diabetes (ATTAIN-2). Lancet. 2025;406(10522):2927–2944. PMID 41275875
  8. Rosenstock J, et al. Efficacy and safety of once-daily oral orforglipron compared with oral semaglutide in adults with type 2 diabetes (ACHIEVE-3). Lancet. 2026;407(10534):1147–1160. PMID 41765029
  9. Klein KR, et al. Cardiovascular safety of orforglipron versus insulin glargine in adults with type 2 diabetes at increased cardiovascular risk (ACHIEVE-4). Lancet. 2026;408(10564):1557–1570. PMID 42815506
  10. Aronne LJ, et al. Orforglipron for maintenance of body weight reduction: the ATTAIN-MAINTAIN trial. Nat Med. 2026;32(7):2679–2687. PMID 42120723
  11. US Food and Drug Administration. FDA approves first new molecular entity under National Priority Voucher program. 1 April 2026. fda.gov
  12. Medicines and Healthcare products Regulatory Agency. UK first in Europe to authorise orforglipron for weight management and type 2 diabetes. 10 August 2026. gov.uk
  13. European Medicines Agency. Foundayo: summary of opinion (pending EC decision). 16 October 2026. ema.europa.eu
  14. World Anti-Doping Agency. The 2026 Prohibited List (in force 1 January 2026). wada-ama.org And the 2026 Monitoring Program.
  15. US prescribing information for Rybelsus (oral semaglutide), revised January 2026. dailymed.nlm.nih.gov

Peptidarium Library. Orforglipron (entry 0029), revision 1.0, 2 November 2026. peptidarium.com/library/orforglipron

08

Revision history

RevDateChangeBy
1.02 Nov 2026Entry created.[Scientific editor]

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