Bile acids are the natural agonists for the nuclear receptor Farnesoid X Receptor (FXR). Studies utilizing natural and synthetic FXR-agonists and FXR null mice indicate that FXR controls numerous metabolic pathways, including those involved in bile acid, lipid and glucose homeostasis. In addition, FXR functions to control bacterial growth in the intestine, gallstone formation, hepatic regeneration and tumorogenesis. Thus, FXR may represent a novel target for pharmaceutical intervention that may influence various metabolic disorders or diseases.