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This is a combination of three small molecule drugs—obeticholic acid, gemfibrozil, and ursodeoxycholic acid. Obeticholic acid is a potent agonist of the farnesoid X receptor (FXR), which regulates bile and cholesterol metabolism in the liver and intestines. It reduces bile acid synthesis, inflammation, and hepatic fibrosis[2][8]. Ursodeoxycholic acid (UDCA) is a hydrophilic bile acid that improves bile flow and protects hepatocytes from toxic effects of other bile acids; it is standard first-line therapy for primary biliary cholangitis (PBC)[2][6][8]. Gemfibrozil is a peroxisome proliferator-activated receptor alpha (PPARα) agonist used primarily to lower triglycerides by increasing lipoprotein lipase activity. While obeticholic acid plus UDCA are approved for PBC in patients with inadequate response to UDCA alone[2][3][5][6], there are no known approved or established uses for the triple combination with gemfibrozil.
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