Incretin & metabolic research compounds
Orforglipron
Also known as LY3502970
An oral, small-molecule (non-peptide) GLP-1 receptor agonist taken once daily without food restrictions.
In 60 seconds
Phase 3 programme in type 2 diabetes and obesity (2025–2026), including a head-to-head versus oral semaglutide. Phase 1–3 trials report the class gastrointestinal profile.
- A phase 2 trial measured weight change with once-daily oral orforglipron in adults with obesity.
- A phase 3 multinational trial examined three orforglipron doses for obesity.
- Structural work showing how a non-peptide molecule activates the GLP-1 receptor.
Mechanism
Orforglipron activates the GLP-1 receptor despite not being a peptide: structural studies show it binds a pocket distinct from GLP-1 itself, producing biased signalling. Being a small molecule, it is orally bioavailable without the absorption enhancer oral semaglutide needs.
Research status
Phase 3 programme in type 2 diabetes and obesity (2025–2026), including a head-to-head versus oral semaglutide.
Key studies
A phase 2 trial measured weight change with once-daily oral orforglipron in adults with obesity.
Daily Oral GLP-1 Receptor Agonist Orforglipron for Adults with Obesity — N Engl J Med, 2023 · PMID 37351564
A phase 3 multinational trial examined three orforglipron doses for obesity.
Orforglipron, an Oral Small-Molecule GLP-1 Receptor Agonist for Obesity Treatment — N Engl J Med, 2025 · PMID 40960239
Structural work showing how a non-peptide molecule activates the GLP-1 receptor.
Structural basis for GLP-1 receptor activation by LY3502970, an orally active nonpeptide agonist — Proc Natl Acad Sci U S A, 2020 · PMID 33177239
ACHIEVE-3 compared orforglipron with oral semaglutide in type 2 diabetes.
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 · PMID 41765029
Safety signals in the literature
Phase 1–3 trials report the class gastrointestinal profile.
Legal status (South Africa)
Approved incretin medicines are prescription-only (scheduled) in South Africa and available only through a prescriber; research-grade material is not a medicine and is not for human use.
Related compounds we stock
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Comparisons
Questions
What is Orforglipron?
An oral, small-molecule (non-peptide) GLP-1 receptor agonist taken once daily without food restrictions. Orforglipron activates the GLP-1 receptor despite not being a peptide: structural studies show it binds a pocket distinct from GLP-1 itself, producing biased signalling. Being a small molecule, it is orally bioavailable without the absorption enhancer oral semaglutide needs.
What is the research status of Orforglipron?
Phase 3 programme in type 2 diabetes and obesity (2025–2026), including a head-to-head versus oral semaglutide.
What safety signals are reported for Orforglipron?
Phase 1–3 trials report the class gastrointestinal profile.
Does Living Water Labs stock Orforglipron?
Not at present. Orforglipron is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Approved incretin medicines are prescription-only (scheduled) in South Africa and available only through a prescriber; research-grade material is not a medicine and is not for human use.
More in Incretin & metabolic
Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.
