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Home/Compounds/Orforglipron
GLP-1 agonistRx required

Orforglipron

Also known as: LY3502970

Investigational once-daily oral non-peptide GLP-1 receptor agonist in Phase 3 trials.

B
Grade B
Human observational studies
Human studies26
PubMed citations30
Routeoral
Regulatory (US)Rx required
Last verified2 days ago

Mechanism of action

Small-molecule (non-peptide) GLP-1 receptor agonist. Oral bioavailability is its key differentiator vs injectable GLP-1s.

Evidence summary

26
Human studies
30
PubMed citations
25
Clinical trials
B
Evidence grade

Phase 2 and Phase 3 data in obesity and T2D. ACHIEVE and ATTAIN trial programs ongoing as of 2025.

Dosing protocols

Educational information only. Consult a licensed provider before using any peptide.
Administration routes
oral

Side effects & safety

From the FDA label
Source
abdominal painacute kidney injuryconstipationdiabetic retinopathydiarrheadizzinessdyspepsiaeructationfatiguegastroesophageal reflux diseaseheadachehypoglycemianauseapancreatitistachycardiavomiting

Terms pulled directly from the referenced source. We don't fabricate frequencies — when a label doesn't publish a percentage, we don't either.

Interactions

No documented drug interactions on file.

Regulatory status

United States
Not FDA approved

Investigational — Phase 3 clinical trials

Compounding
Not permitted

Not available via 503A/503B compounding pharmacies.

Regulatory data last verified 4/19/2026

Clinical trials

NCT07241390A Phase 3, Randomized, Double-Blind, Placebo-Controlled, Event-Driven Study to Investigate the Effect of Orforglipron on the Incidence of Major Adverse Cardiovascular Events in Participants With Established Atherosclerotic Cardiovascular Disease and/or Chronic Kidney DiseaseRecruiting · Phase 3 · Atherosclerosis Cardiovascular Disease · n=7140NCT07153471A Phase 3 Study to Investigate the Efficacy and Safety of Orforglipron Once Daily in Participants Who Have Obesity or Overweight and Osteoarthritis of the Knee: A Multicenter, Randomized, Double-Blind, Parallel-Arm, Placebo-Controlled TrialRecruiting · Phase 3 · Osteoarthritis · n=800NCT07202884A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Tablet Once Daily Compared With Placebo in Female Participants With Stress Urinary Incontinence Who Have Obesity or OverweightRecruiting · Phase 3 · Urinary Incontinence,Stress · n=1000NCT05803421A Phase 3, Open-Label Study of Once Daily LY3502970 Compared With Insulin Glargine in Adult Participants With Type 2 Diabetes and Obesity or Overweight at Increased Cardiovascular RiskCompleted · Phase 3 · Type 2 Diabetes · n=2749NCT06952530A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Once Daily in Participants With Hypertension and Obesity or Overweight: Randomized, Double-Blind, Placebo-Controlled Trials (ATTAIN-HYPERTENSION)Recruiting · Phase 3 · Hypertension · n=487NCT07223593A Study to Investigate the Efficacy and Safety of Orforglipron Once Daily in Participants With Peripheral Artery Disease: A Randomized, Double-Blind, Placebo Controlled TrialRecruiting · Phase 3 · Peripheral Arterial Disease · n=1205NCT06948435A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Once Daily in Participants With Hypertension and Obesity or Overweight: Randomized, Double-Blind, Placebo-Controlled Trials (ATTAIN-HYPERTENSION)Recruiting · Phase 3 · Hypertension · n=487NCT06972459A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Tablet Once Daily Compared With Placebo in Participants With Obesity or Overweight With and Without Type 2 DiabetesRecruiting · Phase 3 · Obesity · n=600NCT06993792A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Tablet Once Daily Compared With Placebo in Participants With Obesity or Overweight With and Without Type 2 DiabetesRecruiting · Phase 3 · Obesity · n=1200NCT06948422A Master Protocol to Investigate the Efficacy and Safety of Orforglipron Once Daily in Participants With Hypertension and Obesity or Overweight: Randomized, Double-Blind, Placebo-Controlled Trials (ATTAIN-HYPERTENSION)Recruiting · Phase 3 · Hypertension · n=974NCT06672549A Master Protocol for a Randomized, Controlled, Clinical Platform Trial to Investigate the Efficacy and Safety of Interventions for Chronic Weight Management in Pediatric Participants With Obesity or OverweightRecruiting · Phase 3 · Obesity · n=125NCT06824051A Phase 1, Double-blind, Two-arm, Mechanism of Action Study to Investigate the Effect of Orforglipron on Body Composition in Adult Participants With Obesity or Overweight, Without DiabetesCompleted · Phase 1 · Obesity · n=120

Showing 12 of 25 indexed studies. View all on ClinicalTrials.gov →

Citations

PMID 40888509Morse BL, Bhattachar S et al. · Disposition and Absolute Bioavailability of Orally Administered Orforglipron in Healthy Participants.Clinical pharmacology in drug development (2026)HumanPMID 41054801Son JW, le Roux CW et al. · Novel GLP-1-based Medications for Type 2 Diabetes and Obesity.Endocrine reviews (2026)HumanPMID 41683830Kansakar U, Jankauskas SS et al. · Orforglipron: A Comprehensive Review of an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity and Type 2 Diabetes.International journal of molecular sciences (2026)HumanPMID 41765029Rosenstock J, Yabe D 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 (London, England) (2026)HumanPMID 41053816Santulli G · From needles to pills: oral GLP-1 therapy enters the obesity arena.Cardiovascular diabetology. Endocrinology reports (2025)PMID 40544435Rosenstock J, Hsia S et al. · Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist, in Early Type 2 Diabetes.The New England journal of medicine (2025)HumanPMID 39952695Kokkorakis M, Chakhtoura M et al. · Emerging pharmacotherapies for obesity: A systematic review.Pharmacological reviews (2025)HumanPMID 41398455Pillai AA, Sharma AM et al. · Orforglipron: A Novel Oral GLP-1 Agonist for the Treatment of Obesity and Diabetes.Cardiology in review (2025)PMID 40481478Wharton S, Rosenstock J et al. · 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.Cardiovascular diabetology (2025)HumanPMID 40960239Wharton S, Aronne LJ et al. · Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment.The New England journal of medicine (2025)HumanPMID 40813122Nong K, Jeppesen BT et al. · Medications for adults with type 2 diabetes: a living systematic review and network meta-analysis.BMJ (Clinical research ed.) (2025)HumanPMID 40042613Himmerich H · [Glucagon-like peptide-1 receptor agonists: a new pharmacological treatment option for psychiatric illnesses?].Der Nervenarzt (2025)HumanPMID 40604322Caruso I, Cignarelli A et al. · Incretin-based therapies for the treatment of obesity-related diseases.npj metabolic health and disease (2025)PMID 41275408Panou T, Gouveri E et al. · Orforglipron in type 2 diabetes mellitus and obesity: an overview.Expert review of clinical pharmacology (2025)HumanPMID 39305981Xie Z, Zheng G et al. · Seven glucagon-like peptide-1 receptor agonists and polyagonists for weight loss in patients with obesity or overweight: an updated systematic review and network meta-analysis of randomized controlled trials.Metabolism: clinical and experimental (2024)HumanPMID 38414573Dutta D, Nagendra L et al. · Orforglipron, a novel non-peptide oral daily glucagon-like peptide-1 receptor agonist as an anti-obesity medicine: A systematic review and meta-analysis.Obesity science & practice (2024)PMID 39693407Sloop KW, Cox AL et al. · The pharmacological basis for nonpeptide agonism of the GLP-1 receptor by orforglipron.Science translational medicine (2024)HumanPMID 38511400Hong SH, Choi KM · Gut hormones and appetite regulation.Current opinion in endocrinology, diabetes, and obesity (2024)HumanPMID 38275036Al-Horani RA, Aliter KF et al. · Future is Brighter: New Potential Paradigm-Shifting Medications and Regimens for Diabetes and Obesity.Current diabetes reviews (2024)HumanPMID 38753454Gogineni P, Melson E et al. · Oral glucagon-like peptide-1 receptor agonists and combinations of entero-pancreatic hormones as treatments for adults with type 2 diabetes: where are we now?Expert opinion on pharmacotherapy (2024)Human

Showing 20 of 30 papers. View all on PubMed →