ASC48

ASC48 is a potentially first-in-class, oral small molecule glucose-dependent insulinotropic polypeptide receptor (GIPR) agonist developed by Ascletis Pharma. Discovered using the company's proprietary Artificial Intelligence-assisted Structure-Based Drug Discovery (AISBDD) technology, ASC48 exhibits high potency (EC50 of 1 pM in the hGIPR cAMP activation assay) and selectivity for GIPR without activity at GLP-1R or GCGR. It is designed for once-daily oral dosing, demonstrating excellent oral bioavailability, drug exposure, and a long half-life in preclinical models. ASC48 is being developed primarily for chronic weight management (obesity), both as a monotherapy and as part of fixed-dose combinations, including ASC30_48FDC (a dual GLP-1R/GIPR agonist combination with ASC30) and ASC30_48_39FDC (a triple GLP-1R/GIPR/amylin receptor agonist combination with ASC30 and ASC39).