AP-2202

AP-2202 is an orally administered, gut-restricted small molecule antagonist of the **G protein-coupled bile acid receptor 1** (GPBAR1, also known as **TGR5**). Developed by **Hangzhou Anyuan Biopharmaceutical Technology**, it is designed to treat gastrointestinal disorders characterized by excessive bile acid activity, specifically **bile acid diarrhea (BAD)** and **diarrhea-predominant irritable bowel syndrome (IBS-D)**. In these conditions, bile acids in the colon activate TGR5 receptors on enteroendocrine cells and enteric neurons, stimulating fluid secretion and accelerating colonic transit. By selectively antagonizing TGR5, AP-2202 aims to inhibit these pro-secretory and pro-motility pathways, thereby reducing stool frequency and improving consistency. The drug has completed Phase 1 safety studies and is currently undergoing Phase 2 clinical evaluation in China.