Orforglipron is an oral, small molecule GLP-1 receptor agonist used as part of a weight management regimen. Developed to circumvent the adherence barriers and strict administration requirements of peptide-based GLP-1 therapies, its small-molecule structure enables once-daily oral dosing without food or water restrictions.
- Mechanism
- Curator reviewed · 4 references
Orforglipron is a first-in-class, non-peptide, small molecule agonist of the human GLP-1 receptor. Unlike endogenous GLP-1 or peptide-based agonists that bind to the extracellular domain, orforglipron acts as an allosteric agonist, binding within a distinct hydrophobic transmembrane pocket formed primarily by TM1, TM2, TM3, TM7, and ECL2. It exhibits biased signaling, favoring G protein activation and intracellular cAMP accumulation over β-arrestin recruitment. Activation of the GLP-1 receptor enhances glucose-dependent insulin secretion, suppresses inappropriate glucagon release, and engages hypothalamic and brainstem circuits involved in satiety and appetite regulation to facilitate weight loss.
- Primary indication
- Orforglipron is indicated in combination with a reduced-calorie diet and increased physical activity to reduce excess body weight and maintain weight reduction long term in overweight or obese adults in the presence of at least...Curator reviewed · 2 structured indications
- Formula / weight
- C48H48F2N10O5 · 882.974 g/mol (avg)
- First approval
- United States, 2026
- Also known as
- 1,2,4-Oxadiazol-5(2H)-one, 3-[(1S,2S)-1-[2-[[(4S)-2-(4-fluoro-3,5-dimethylphenyl)-3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2,3-dihydro-2-oxo-1H-imidazol-1-yl]-2,4,6,7-tetrahydro-4-methyl-5H-pyrazolo[4,3-c]pyridin-5-yl]carbonyl]-5-[(4S)-tetrahydro-2,2-dim · 3-[(1S,2S)-1-({2-(4-fluoro-3,5-dimethylphenyl)-3-({3-[3-(4-fluoro-1-methyl-1H-indazol-5-yl)-2-oxo-2,3-dihydro-1H-imidazol-1-yl]-4-methyl-2,4,6,7-tetrahydro-5H-pyrazolo[4,3-c]pyridin-5-yl}carbonyl)-5-[(4S)-2,2-dimethyloxan-4-yl]-1H-indol-1-yl}-2-methylcyc
- Code names
- LY-3502970
- Brand names
Resolves to
USUWIEBBBWHKNI-KHIFEHGGSA-NSMILES[H][C@@]1(CCOC(C)(C)C1)C1=CC=C2N(C(=CC2=C1)C(=O)N1CCC2=NN(C(N3C=CN(C3=O)C3=CC=C4N(C)N=CC4=C3F)=C2[C@@H]1C)C1=CC(C)=C(F)C(C)=C1)[C@]1(C[C@@H]1C)C1=NOC(=O)N1What you can answer from here — as of September 23, 2026
Which drugs share a target with Orforglipron, and which of those have an active Phase 3 trial?
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