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: A pioneering oral non-peptide GLP-1 receptor partial agonist for obesity Orforglipron is an oral non-peptide Glucagon-like peptide-1 (GLP-1) receptor partial agonist that is entering Ph. III trials to treat obesity and type-2-diabetes mellitus (T2DM). This 2020 Molecule of the Year nominee, which was nominated 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. GLP-1 agonists such as exenatide (approved in 2005) have been successfully used clinically for nearly 20 years to treat diabetes, but have recently been all over the news (and TikTok! – when was the last time you saw a hashtag for a drug like Ozempic?)…