WhatPeptide

Orforglipron

A non-peptide oral GLP-1 receptor agonist discovered by Chugai Pharmaceutical and licensed to Eli Lilly in 2018. The first small-molecule GLP-1 agonist to reach Phase 3. ATTAIN-1 (NCT05869903, 3,127 adults, 72 weeks) showed 12.4% placebo-subtracted weight loss at 36 mg (efficacy estimand) or 11.2% vs 2.1% placebo (treatment-regimen estimand). NDA submitted to FDA December 2025.

Strong evidence Investigational GLP-1 Agonist

Written by WhatPeptide Editorial Team · Last updated 2026-03-18

Currently in clinical trials — not yet approved for any indication.

Half-life

29-49 hours at steady state (single-dose data extend to ~68 hours)

Dosage range

Titration: 1 → 3 → 6 → 12 → 24 → 36 mg every 4 weeks to target dose. Phase 3: 12, 24, or 36 mg once daily oral (ATTAIN-1)

Administration

Oral

Research level

Strong

How Orforglipron works

Small-molecule agonist that binds and activates the GLP-1 receptor, promoting glucose-dependent insulin secretion, suppressing glucagon release, delaying gastric emptying, and reducing appetite via hypothalamic satiety centers. Achieves comparable downstream signaling to injectable GLP-1 agonists despite non-peptide structure.

Also known as: LY3502970, OWL833

Research relevance

Fat Loss
Strong research relevance 80

Side effects & safety

Nausea (dose-dependent, most common) Vomiting Diarrhea Decreased appetite Constipation

Contraindications

Personal or family history of medullary thyroid carcinoma or MEN2 (GLP-1 class warning)
Pregnancy

Consult a healthcare provider before use if any of these apply to you.

FAQ

What is Orforglipron? +
A non-peptide oral GLP-1 receptor agonist discovered by Chugai Pharmaceutical and licensed to Eli Lilly in 2018. The first small-molecule GLP-1 agonist to reach Phase 3. ATTAIN-1 (NCT05869903, 3,127 adults, 72 weeks) showed 12.4% placebo-subtracted weight loss at 36 mg (efficacy estimand) or 11.2% vs 2.1% placebo (treatment-regimen estimand). NDA submitted to FDA December 2025. Its mechanism of action is supported by robust clinical evidence.
What is Orforglipron researched for? +
Orforglipron has the strongest research relevance for Fat Loss. Evidence is supported by robust clinical evidence.
What are the side effects of Orforglipron? +
Reported side effects include Nausea (dose-dependent, most common), Vomiting, Diarrhea, Decreased appetite, Constipation. Key contraindications: Personal or family history of medullary thyroid carcinoma or MEN2 (GLP-1 class warning); Pregnancy.
Is Orforglipron FDA approved? +
Orforglipron is currently in clinical trials and is not yet approved by the FDA.
How is Orforglipron administered? +
Orforglipron is typically administered via oral route. Researched dosage range: Titration: 1 → 3 → 6 → 12 → 24 → 36 mg every 4 weeks to target dose. Phase 3: 12, 24, or 36 mg once daily oral (ATTAIN-1). Half-life: 29-49 hours at steady state (single-dose data extend to ~68 hours).

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