11 minute read
Mar. 12, 2024

Orforglipron: A Pioneering Oral Non-Peptide GLP-1R Agonist for Weight Loss


oral non-peptide GLP-1R agonist Ph. III for obesity + type 2 diabetes from LLC-PK1 cell HTS + opt N. Engl. J. Med., June 23, 2023 Chugai, Shizuoka, JP; Eli Lilly, Indianapolis, IN


Orforglipron is an oral non-peptide glucagon-like peptide-1 (GLP-1) receptor partial agonist that entered Ph. III trials to treat obesity and type-2-diabetes mellitus (T2DM). This 2020 and 2023 Molecule of the Year nominee (nominated initially back when it was still in Ph. I) was first discovered by Chugai Pharmaceuticals under the name OWL833, then licensed by Eli Lilly for worldwide development under the name LY3502970. The article discusses where it sits in the GLP-1R agonist landscape, why it’s scientifically notable, how it works with illustrations from cryo-EM structures, its synthesis, and more.



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