FXR (Farnesoid X Receptor) is a nuclear hormone receptor implicated in a variety of metabolic and liver disorders. Modulators of FXR have been shown to lower triglycerides and improve the cholesterol profile in preclinical models of dyslipidemia and atherosclerosis. These modulators are also highly effective in blocking disease progression in preclinical models of liver disorders. These data suggest that targeting FXR may be useful for the treatment of patients with metabolic syndrome and liver disease.
FXR is being evaluated by Wyeth (now Pfizer), which is responsible for preclinical and clinical development, and commercialization activities for the compound. Small molecule inhibitors of FXR are being evaluated in preclinical studies.