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Obeticholic Acid: First Global Approval
Drugs, 2016Obeticholic acid (Ocaliva(TM)) is a farnesoid-X receptor (FXR) agonist that is being developed by Intercept Pharmaceuticals for the treatment of various liver diseases, and has recently been granted accelerated approval in the USA for the treatment of primary biliary cholangitis in combination with ursodeoxycholic acid in adults with an inadequate ...
A, Markham, Susan J, Keam
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Journal of Separation Science, 2021
AbstractA rapid, robust, simple, selective, and sensitive liquid chromatography‐tandem mass spectrometry method was developed for the simultaneous estimation of obeticholic acid and its two pharmacologically active metabolites, glyco‐obeticholic acid, and tauro‐obeticholic acid in human plasma.
Venkat Rao Valluri +6 more
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AbstractA rapid, robust, simple, selective, and sensitive liquid chromatography‐tandem mass spectrometry method was developed for the simultaneous estimation of obeticholic acid and its two pharmacologically active metabolites, glyco‐obeticholic acid, and tauro‐obeticholic acid in human plasma.
Venkat Rao Valluri +6 more
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Obeticholic acid for the treatment of nonalcoholic steatohepatitis
Expert Review of Gastroenterology & Hepatology, 2020NAFLD has grown to become the most prevalent liver disease in the world, with a quarter of the general population estimated to have the disease. NASH, characterized as NAFLD with inflammation, is associated with worsening fibrosis along with increased incidence of HCC.
Raj A, Shah, Kris V, Kowdley
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Obeticholic acid in primary biliary cholangitis
Current Opinion in Gastroenterology, 2019This review will summarize the use of obeticholic acid (OCA) in treatment of primary biliary cholangitis (PBC). It seeks to discuss the mechanism of action, evidence for use, appropriate clinical use, and common adverse effects of OCA.PBC is a chronic, progressive cholestatic liver disease that is a chronic progressive that may lead to end-stage liver ...
Vignan, Manne, Kris V, Kowdley
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Obeticholic acid in primary biliary cholangitis
Clinics and Research in Hepatology and Gastroenterology, 2017In a double-blind, randomized, placebo-controlled study including 217 patients with primary biliary cholangitis, the authors show that obeticholic acid (a potent farnesoid X agonist) administered with ursodeoxycholic acid or as monotherapy significantly decreases serum alkaline phosphatase and bilirubin when compared to placebo.
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A facile synthesis of ursodeoxycholic acid and obeticholic acid from cholic acid
Steroids, 2018A novel synthetic route of producing ursodeoxycholic acid (UDCA) and obeticholic acid (OCA) was developed through multiple reactions from cheap and readily-available cholic acid. The reaction conditions of the key elimination reaction of mesylate ester group were also investigated and optimized, including solvent, base and reaction temperature.
Xiao-Long He +4 more
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Metabolism of obeticholic acid in brown bullhead (Ameiurus nebulosus)
Environmental Science and Pollution Research, 2019Analysis of brown bullhead (Ameiurus nebulosus) bile by ultra performance liquid chromatography high-resolution mass spectrometry (UPLC/HRMS) revealed a series of bile acids similar to those found in humans. Accordingly, we chose this fish as a model organism to examine the metabolism of obeticholic acid, a bile acid used to treat a number of human ...
Samuel Mach +2 more
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Obeticholic acid for the treatment of primary biliary cholangitis
Expert Opinion on Pharmacotherapy, 2016Primary biliary cholangitis (PBC) is an autoimmune disease of the liver characterized by destruction and inflammation of the intrahepatic bile ducts. The disease affects mainly women. The disease is often discovered through abnormal alkaline phosphatase (ALP) activity, and is confirmed when anti-mitochondrial antibodies (AMA) are present.
Ahmad H, Ali, Keith D, Lindor
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Obeticholic acid for the treatment of primary biliary cirrhosis
Expert Review of Gastroenterology & Hepatology, 2016There is significant unmet need in Primary Biliary Cholangitis (PBC) in patients under-responsive to the only approved therapy Ursodeoxycholic Acid (UDCA) who are at increased risk of progressing to end-stage liver disease. Obeticholic Acid (OCA) is a farnesoid X receptor (FXR) agonist which has been evaluated as a second line therapy in PBC and has ...
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