Regulated as medicinal products

Orforglipron

Last reviewed

Reviewed by HelixEvoLabs Research Team

Technical, analytical and regulatory reference for orforglipron as a manufactured small-molecule material.

Identity and nomenclature

INN
orforglipron
Synonyms
orforglipron calcium, orforglipron hemicalcium
Development codes
LY3502970, LY-3502970, OWL833

Mechanism

Orforglipron is a non-peptide small molecule that binds and activates the human glucagon-like peptide-1 receptor. Because it is not a peptide it has no amino acid sequence, and peptide-specific analytical characterisation does not apply to it.

The approved labelling characterises the mechanism in a single sentence, stating that the product is a GLP-1 receptor agonist that binds to and activates the human GLP-1 receptor. The labelling does not characterise the agonism as either full or partial.

Published sources are not consistent on that point. The FDA press announcement issued at approval described the compound as a GLP-1 receptor partial agonist, while a 2026 peer-reviewed review described it as a full agonist. This reference records the discrepancy rather than resolving it, because no primary source settles it.

The compound was discovered by Chugai Pharmaceutical and licensed to Eli Lilly in 2018, at which point Chugai described it as an oral non-peptidic GLP-1 receptor agonist.

Analytical and manufacturing profile

Analytical data sheet

Orforglipron

Identity

Molecular formula
C48H48F2N10O5
Molecular weight
902.0 g/mol (orforglipron calcium, the approved drug substance; the free-base molecular weight is not stated in any primary source)
CAS number
2212020-52-3
UNII
7ZW40D021M
Chemical name
calcium bis{3-[(1S,2S)-1-({2-(4-fluoro-3,5-dimethylphenyl)-3-({3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridine-5-yl}carbonyl)-5-[(4S)-2,2-dimethyloxan-4-yl]-1H-indol-1-yl}-2-methylcyclopropyl]-5-oxo-1,2,4-oxadiazol-4(5H)-ide}
Appearance
White to practically white to light brown solid; hygroscopic

Structural notes

  • Non-peptide small molecule. No amino acid sequence exists, and no peptide-specific analytical characterisation applies.
  • Marketed as the hemicalcium salt, orforglipron calcium: CAS 2415797-61-2, UNII VI5M9OZV2X, molecular weight 902.0 g/mol per FDA labelling section 11.
  • The systematic name of the acid moiety specifies two stereocentres, at the 1S,2S-substituted cyclopropyl and the 4S-substituted oxane.

Solubility

Water
Insoluble

Storage

FormTemperatureDuration
Film-coated tablet, finished product20-25 °C, excursions permitted between 15 °C and 30 °CNot verified

Stability

  • The drug substance is hygroscopic. The finished product is packaged in bottles with a desiccant, consistent with that property.
  • The finished product is light sensitive; labelling directs that it be protected from light by retention in the original bottle and carton.

Analytical methods

No validated method or acceptance criterion is published for this compound in a primary source. Where an approved product exists, limits are commonly withheld from the public assessment record as commercially confidential.

Impurities and degradation products

No impurity profile established from a primary source.

Handling

  • Handled as a hygroscopic, light-sensitive pharmaceutical solid. Containment and environmental controls are determined by the receiving facility under its own occupational assessment.

Clinical development

ATTAIN-1

NCT05869903
Phase
3
Enrolment
3127
Duration
72 weeks
Status
reported
Population
Adults with obesity, or overweight with weight-related comorbidities, without type 1 or type 2 diabetes
Primary endpoint
Mean percentage change from baseline in body weight at week 72

Reported outcomes

Outcomes as reported by ATTAIN-1, attributed to trial arm and timepoint
MetricArmValueComparatorTimepoint
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 6 mg once daily, oral-7.5%, 95% CI -8.2 to -6.8Placebo -2.1%, 95% CI -2.8 to -1.4Week 72
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 12 mg once daily, oral-8.4%, 95% CI -9.1 to -7.7Placebo -2.1%, 95% CI -2.8 to -1.4Week 72
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 36 mg once daily, oral-11.2%, 95% CI -12.0 to -10.4Placebo -2.1%, 95% CI -2.8 to -1.4Week 72
Proportion achieving body weight reduction of 10 per cent or more (treatment-regimen estimand)Orforglipron 36 mg once daily, oral54.6%Placebo 12.9%Week 72
Proportion achieving body weight reduction of 20 per cent or more (treatment-regimen estimand)Orforglipron 36 mg once daily, oral18.4%Placebo 2.8%Week 72

Figures as reported by this trial. They are not statements about what the compound does for a person.

Sponsor Eli Lilly and Company · New England Journal of Medicine, 2025 · doi:10.1056/NEJMoa2511774 · PMID 40960239 · verified 2026-07-30

ATTAIN-2

NCT05872620
Phase
3
Enrolment
1613
Duration
72 weeks
Status
reported
Population
Adults with obesity or overweight and type 2 diabetes, with glycated haemoglobin between 7 and 10 per cent, naive to GLP-1 receptor agonists and DPP-4 inhibitors
Primary endpoint
Mean percentage change from baseline in body weight at week 72

Reported outcomes

Outcomes as reported by ATTAIN-2, attributed to trial arm and timepoint
MetricArmValueComparatorTimepoint
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 6 mg once daily, oral-5.1%, 95% CI -6.0 to -4.2; estimated treatment difference -2.7Placebo -2.5%, 95% CI -3.0 to -1.9Week 72
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 12 mg once daily, oral-7.0%, 95% CI -7.8 to -6.2; estimated treatment difference -4.5Placebo -2.5%, 95% CI -3.0 to -1.9Week 72
Mean percentage change from baseline in body weight (treatment-regimen estimand)Orforglipron 36 mg once daily, oral-9.6%, 95% CI -10.5 to -8.7; estimated treatment difference -7.1Placebo -2.5%, 95% CI -3.0 to -1.9Week 72
Change from baseline in glycated haemoglobin, from a baseline of 8.05 per cent (treatment-regimen estimand)Orforglipron 36 mg once daily, oral-1.66 percentage pointsPlacebo -0.47 percentage pointsWeek 72

Figures as reported by this trial. They are not statements about what the compound does for a person.

Sponsor Eli Lilly and Company · The Lancet, 2025 · doi:10.1016/S0140-6736(25)02165-8 · PMID 41275875 · verified 2026-07-30

ACHIEVE-1

NCT05971940

Topline results only — not peer reviewed

Phase
3
Enrolment
559
Duration
40 weeks
Status
reported
Population
Adults with type 2 diabetes and inadequate glycaemic control on diet and exercise alone, with glycated haemoglobin between 7.0 and 9.5 per cent, a body mass index of at least 23, naive to recent antihyperglycaemic medication and weight stable for 90 days
Primary endpoint
Change from baseline in glycated haemoglobin at week 40. Registry-posted least-squares mean values are recorded here rather than publication figures

Reported outcomes

Outcomes as reported by ACHIEVE-1, attributed to trial arm and timepoint
MetricArmValueComparatorTimepoint
Change from baseline in glycated haemoglobin (least-squares mean, registry-posted)Orforglipron 3 mg once daily, oral (n=143)-1.26 percentage points (SE 0.114)Placebo -0.15 percentage points (SE 0.113), n=138Week 40
Change from baseline in glycated haemoglobin (least-squares mean, registry-posted)Orforglipron 12 mg once daily, oral (n=137)-1.59 percentage points (SE 0.087)Placebo -0.15 percentage points (SE 0.113), n=138Week 40
Change from baseline in glycated haemoglobin (least-squares mean, registry-posted)Orforglipron 36 mg once daily, oral (n=141)-1.45 percentage points (SE 0.104)Placebo -0.15 percentage points (SE 0.113), n=138Week 40

Figures as reported by this trial. They are not statements about what the compound does for a person.

Who this trial excluded

The trial establishes nothing about these groups. An outcome table cannot show this, so it is recorded alongside the results.

  • Type 1 diabetes mellitus
  • Recent diabetic ketoacidosis or hyperosmolar hyperglycaemic events
  • New York Heart Association Class IV heart failure
  • Acute or chronic pancreatitis
  • Current treatment for diabetic retinopathy
Sponsor Eli Lilly and Company · verified 2026-08-05

Regulatory status by jurisdiction

  • United States

    FDA
    Approved medicine

    Approved on 1 April 2026 under New Drug Application 220934 as Foundayo, the fifth approval and the first new molecular entity issued under the Commissioner’s National Priority Voucher pilot programme.

    FDA approves first new molecular entity under National Priority Voucher programVerified 2026-07-30

  • European Union

    European Medicines Agency
    Investigational — no marketing authorisation

    No marketing authorisation. Under evaluation by the Committee for Medicinal Products for Human Use as procedure EMEA/H/C/006632, at the Day 120 list-of-questions stage as of the May 2026 meeting, and not among the medicines recommended for approval at the July 2026 meeting.

    Agenda, CHMP meeting 18-21 May 2026 (EMA/CHMP/93949/2026)Verified 2026-07-30

  • United Kingdom

    MHRA
    Investigational — no marketing authorisation

    No marketing authorisation. The MHRA products database returns no result for either the international nonproprietary name or the United States brand name, and no application has been confirmed from a primary source.

    MHRA products database search result for orforglipronVerified 2026-07-30

Supply classification and permitted use

Orforglipron is an approved medicinal product in the United States. HelixEVO does not supply medicinal products for human administration. Material is supplied to businesses for research and manufacturing purposes only.

  • Approval in the United States does not extend to any other jurisdiction. The compound holds no marketing authorisation in the European Union or the United Kingdom.
  • Supply of material does not constitute authorisation to place a finished medicinal product on any market.

How supply classifications work · Documented safety signals

References

  1. [1]RegulatorFOUNDAYO (orforglipron) tablets, for oral use — prescribing information — US Food and Drug Administration, 2026 · accessed
  2. [2]RegulatorFDA approves first new molecular entity under National Priority Voucher program — US Food and Drug Administration, 2026 · accessed
  3. [3]RegulatorORFORGLIPRON — Global Substance Registration System record, UNII 7ZW40D021M — US Food and Drug Administration, 2026 · accessed
  4. [4]RegulatorORFORGLIPRON CALCIUM — Global Substance Registration System record, UNII VI5M9OZV2X — US Food and Drug Administration, 2026 · accessed
  5. [5]RegulatorAgenda, CHMP meeting 18-21 May 2026 (EMA/CHMP/93949/2026) — European Medicines Agency, 2026 · accessed
  6. [6]RegulatorMeeting highlights from the Committee for Medicinal Products for Human Use, 20-23 July 2026 — European Medicines Agency, 2026 · accessed
  7. [7]RegulatorMHRA products database search result for orforglipron — Medicines and Healthcare products Regulatory Agency, 2026 · accessed
  8. [8]DeveloperFDA approves Lilly’s Foundayo (orforglipron), the only GLP-1 pill for chronic weight management — Eli Lilly and Company, 2026 · accessed
  9. [9]DeveloperChugai and Lilly enter into a license agreement for oral GLP-1 agonist, OWL833 — Chugai Pharmaceutical, 2018 · accessed
  10. [10]Peer-reviewedShirley M. Orforglipron: First Approval — Springer, Drugs, 2026 · doi:10.1007/s40265-026-02363-5 · accessed
  11. [11]Peer-reviewedKansakar S, et al.. Review of incretin receptor pharmacology including orforglipron receptor agonism — MDPI, International Journal of Molecular Sciences, 2026 · doi:10.3390/ijms27031409 · accessed