RDX-023

RDX-023 is a potent, orally active, small molecule agonist of the TGR5 receptor (also known as GPBAR1), developed by Ardelyx. TGR5 is a G protein-coupled receptor that responds to bile acids and is involved in regulating metabolic processes, bile acid homeostasis, and inflammatory responses. By activating TGR5, RDX-023 was designed to stimulate the release of glucagon-like peptide-1 (GLP-1) and other gastrointestinal hormones, as well as modulate bile acid signaling. The primary development focus for RDX-023 was the treatment of cholestatic liver diseases, such as primary biliary cholangitis (PBC), and metabolic conditions like type 2 diabetes. However, development progress has been limited in recent years as the developer prioritized other assets like tenapanor.