orforglipron + metformin

LY900020 is an investigational fixed-dose combination (FDC) tablet developed by Eli Lilly for the treatment of type 2 diabetes mellitus (T2DM). It combines **orforglipron** (LY3502970), a potent, non-peptide, small-molecule glucagon-like peptide-1 receptor (GLP-1R) agonist, with **metformin**, a foundational biguanide therapy. Orforglipron acts as a highly selective agonist at the GLP-1 receptor, stimulating glucose-dependent insulin secretion, suppressing glucagon release, and slowing gastric emptying. Unlike earlier GLP-1 therapies which are peptides, orforglipron is a small molecule designed for optimized oral bioavailability. Metformin complements this by reducing hepatic glucose production through the inhibition of mitochondrial complex I and the subsequent activation of AMP-activated protein kinase (AMPK), while also improving peripheral insulin sensitivity. The combination is intended to provide robust glycemic control in a convenient oral format for patients with T2DM.

Other names

orforglipron/metforminLY3502970/metforminorforglipron/metformin hydrochloride