Compounds / Metabolic / Orforglipron

Orforglipron

Orforglipron (LY3502970 — Oral Small-Molecule GLP-1 Receptor Agonist)
MetabolicExtensively StudiedFDA: FDA-APPROVED Apr 2026 (Foundayo)

Overview

ATTAIN-1 Phase III (non-diabetic obese): 12.4% weight loss (27.3 lbs) at 72 weeks with 36mg. 59.6% achieved ≥10% weight loss, 39.6% achieved ≥15% weight loss. ATTAIN-2 (T2DM): 10.5% weight loss. Superior to all existing oral obesity medications.

Mechanism of Action

Non-peptide small molecule GLP-1R agonist (Eli Lilly). Biased signaling: preferential G protein/cAMP pathway activation → insulin secretion, glucagon suppression, gastric emptying delay, appetite reduction — while minimizing receptor desensitization. Half-life 29–49 hours. 79.1% oral bioavailability vs ~1% for oral peptide GLP-1 agonists.

Pharmacokinetics

Half-life
1.2 days
Peak (Tmax)
8 hrs
Cleared
6.0 days

Molecular Profile

Molecular weight
~450 Da

Key Research Findings

79.1% oral bioavailability; 12.4% weight loss Phase III ATTAIN-1; 29–49h half-life; oral GLP-1R agonist; superior to existing oral obesity drugs; FDA-approved Apr 1 2026 as Foundayo (NDA 220934) for obesity/overweight.

Published Research

NEJM (2024)
Wharton S et al. Orforglipron for obesity — ATTAIN-1 Phase 3 trial
View source

Related Metabolic Compounds

SemaglutideTirzepatideRetatrutideCagrilintideMazdutideBioglutide
Clinical Guidance

Research data is not a treatment plan. If you are considering Orforglipron, the questions that matter are whether it suits your history, your labs and your goals. That is a conversation with a licensed physician, not a lookup.

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