Orforglipron

China [CN]

Orforglipron Core Information

Generic Name: Orforglipron (Orforglipron / Orglipron)  Development Code: LY3502970, OWL833 CAS Number: 2212020-52-3 Molecular Formula: C₄₈H₄₈F₂N₁₀O₅ Molecular Weight: 882.96 Chemical Name: 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]pyridine-5-yl]carbonyl]-5-[(4S)-tetrahydro-2,2-dimethyl-2H-pyran-4-yl]-1H-indol-1-yl]-2-methylpropanenitrile

Drug Type and Mechanism of Action

Drug Type: Oral non-peptide small molecule GLP-1 receptor agonist (GLP-1 RA)

Mechanism of Action: Selectively activates GLP-1 receptors, producing glucose-dependent insulin secretion, inhibiting glucagon, delaying gastric emptying, and suppressing appetite, achieving both blood sugar reduction and weight loss.

Core Clinical Value (Latest as of 2026)

Indications: Type 2 diabetes, obesity/overweight (BMI≥27 kg/m²)

Administration: Once daily oral administration, not restricted by food/water intake, no injection required, no refrigeration needed.

Weight Loss (ATTAIN-1, obese without diabetes): 36 mg, average weight loss of 12.4% over 72 weeks, 59.6% of patients achieved ≥10% weight loss.

Blood Sugar Reduction (ACHIEVE-3, Type 2 diabetes): 36 mg, HbA1c over 52 weeks Average reduction of 2.2%, superior to oral semaglutide.

Safety: Primarily mild to moderate gastrointestinal reactions; discontinuation rate of 5%–10%; no risk of severe hypoglycemia, pancreatitis, or thyroid tumors.