Septerna metabolic triple agonist

This program consists of oral small molecule triple agonists targeting the glucagon-like peptide-1 receptor (GLP-1R), the gastric inhibitory polypeptide receptor (GIPR), and the glucagon receptor (GCGR). Developed by Septerna in collaboration with a partner (identified as Vertex Pharmaceuticals), these compounds are designed using Septerna's Native Complex Platform, which enables the discovery of small molecules that target complex GPCRs previously only accessible via peptides. By simultaneously activating all three receptors, the drug aims to maximize weight loss in patients with obesity by reducing appetite (via GLP-1 and GIP pathways) and increasing energy expenditure (via the glucagon pathway). This approach seeks to offer the efficacy of injectable peptide triple agonists, such as retatrutide, with the convenience of an oral small molecule format.

Other names

Septerna metabolic programGLP-1R/GIPR/GCGR triple agonist small moleculeSepterna/Vertex metabolic program