Obeticholic acid is a farnesol X receptor agonist that indirectly inhibits the gene expression of cytochrome 7A1 (CYP7A1) by activating the farnesol X receptor. Since CYP7A1 is the rate-limiting enzyme for bile acid biosynthesis, obeticholic acid inhibits bile acid synthesis and is used for the treatment of primary biliary cirrhosis and non-alcoholic fatty liver disease.
Obeticholic acid was developed by Intercept Pharmaceuticals, Inc. and is the first drug to be developed for the treatment of cholestatic liver disease in two decades. The study was used in patients who did not respond adequately to the old standard of care drug ursodeoxycholic acid or who could not tolerate it. In placebo-controlled phase III clinical trials, ursodeoxycholic acid (OCA) increased the levels of two biomarkers associated with a reduced risk of liver transplantation. The composite endpoint of the clinical study was a decrease in alkaline phosphatase of at least 15%, with serum alkaline phosphatase activity below 1.67 times the upper limit of normal and bilirubin within the normal range. Alkaline phosphatase is a biomarker used to indicate the severity of liver disease.
Translated with www.DeepL.com/Translator (free version)
English
中文版