Orforglipron
GLP-1 Receptor Agonist (Non-Peptide, Oral)investigationalAlso known as: LY3502970, OWL833, Oral Non-Peptide GLP-1
A first-in-class oral non-peptide GLP-1 receptor agonist in late-stage clinical development for obesity and type 2 diabetes, offering once-daily dosing without fasting requirements.
Overview
Orforglipron is a small molecule (non-peptide) GLP-1 receptor agonist developed by Eli Lilly, currently in Phase 3 clinical trials. Unlike semaglutide and other peptide-based GLP-1 agonists, orforglipron is a small molecule that can be taken orally without special absorption enhancers or fasting requirements. In Phase 2 trials, it demonstrated up to 14.7% body weight loss over 36 weeks, rivaling injectable GLP-1 agonists. Its non-peptide nature means easier manufacturing, better shelf stability, and potentially lower cost. If approved, it could dramatically expand access to GLP-1 therapy by eliminating injection barriers.
Mechanism of Action
Orforglipron is a non-peptide agonist that binds to and activates the GLP-1 receptor: (1) Stimulates glucose-dependent insulin secretion from pancreatic beta cells; (2) Suppresses glucagon release; (3) Slows gastric emptying to prolong satiety; (4) Acts on hypothalamic appetite centers to reduce food intake; (5) As a small molecule, it has high oral bioavailability without needing absorption enhancers, allowing flexible dosing conditions.
Molecular Formula
C30H33F3N4O3
Molecular Weight
554.6 g/mol
Sequence
Non-peptide small molecule
Dosage Protocols
Dose Range
12mg – 45mg
Frequency
Once daily
Route
oral
Cycle Length
36+ weeks
Phase 2 trials tested 12mg, 24mg, 36mg, and 45mg daily doses. Titrated up over several weeks. No fasting requirements.
Source: Phase 2 clinical trial (NEJM 2023)
🧮 Personalized Dosage Calculator
💰 Estimated Pricing
Typical Supply
Oral tablet
Last Updated
2026-02
Eli Lilly oral non-peptide GLP-1 agonist. In Phase 3 trials. Not yet commercially available. Pricing estimated based on market positioning.
⚠️ Prices are estimates based on publicly available data and may vary significantly by vendor, location, and prescription status. This is not medical or financial advice.
Side Effects
| Effect | Severity |
|---|---|
| Nausea | moderate |
| Vomiting | moderate |
| Diarrhea | mild |
| Constipation | mild |
| Decreased appetite | mild |
Pros & Cons
Oral non-peptide molecule — no injections, no fasting requirements, no special storage
Weight loss of up to 14.7% in Phase 2 trials, comparable to injectable GLP-1 agonists
Potential for lower manufacturing cost and wider accessibility than peptide-based drugs
Room temperature stable, simple daily pill format
Still in clinical trials (Phase 3) — not yet approved or commercially available
GI side effects comparable to other GLP-1 agonists with ~10% discontinuation rate
Long-term safety data not yet available
Technically not a peptide, though functionally mimics one — relevance to peptide community is indirect
Research Studies
🩸 Blood Work
No specific bloodwork requirements reported for this peptide. General health panels are always recommended before starting any peptide protocol.
Legal Status
Investigational drug in Phase 3 clinical trials (Eli Lilly). Not yet approved by any regulatory agency. Not available for purchase outside of clinical trials.
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