safiglipron + metformin

safiglipron + metformin is an investigational combination therapy consisting of safiglipron (formerly known as HRS-7535 or KAI-7535), an orally administered, nonpeptide small-molecule agonist of the glucagon-like peptide-1 receptor (GLP-1R), and metformin, an established biguanide antidiabetic drug. Safiglipron acts as an orthosteric partial agonist of GLP-1R, promoting glucose-dependent insulin secretion, suppressing glucagon release, and delaying gastric emptying to improve glycemic control and induce weight loss. Metformin primarily inhibits mitochondrial complex I, leading to downstream activation of AMP-activated protein kinase (AMPK) and subsequent reduction of hepatic glucose production. The combination is being developed by Jiangsu Hengrui Pharmaceuticals (and its subsidiary Shandong Suncadia Medicine) and Kailera Therapeutics for the treatment of type 2 diabetes mellitus. In Phase 3 clinical trials (such as OUTSTAND-2), once-daily oral safiglipron added to background metformin therapy demonstrated superior glycemic control and modest weight reduction compared to dapagliflozin, with a favorable safety profile characterized mainly by mild-to-moderate gastrointestinal adverse events.

Other names

KAI-7535 + metforminsafiglipron + metformin