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Obeticholic acid is a bile acid analog and farnesoid X receptor agonist used to treat primary biliary cholangitis in adult patients with inadequate clinical response or intolerance to UDCA. Primary biliary cirrhosis, or PBC, is a progressive and chronic condition that leads to hepatic injury often resulting in end-stage liver failure that requires liver transplantation.
- Mechanism
- Curator reviewed · 4 references
Primary biliary cirrhosis is an autoimmune process by which the bile ducts and liver are damaged progressively, leading to fibrosis and cirrhosis. Bile acids increase the risk of damage and fibrosis to the damaged bile ducts.
Obeticholic acid is a potent agonist of the farnesoid X receptor, which serves to regulate the hepatic metabolism of bile and cholesterol. This drug acts by binding to the farnesoid X receptor (FXR), found in the nucleus of liver and intestinal cells, which in turn increases liver bile flow, suppressing its production and decreasing hepatocyte exposure to excess levels of bile with cholestasis. Cholestasis is a process that normally causes inflammation and cirrhosis of the liver.
- Primary indication
- Obeticholic acid is indicated for the treatment of primary biliary cholangitis in combination with ursodeoxycholic acid (UDCA) in adults with an inadequate response to UDCA.Curator reviewed · 2 structured indications
- Formula / weight
- C26H44O4 · 420.6252 g/mol (avg)
- First approval
- Canada, 2022 · United States, 2016
- Also known as
- 6-alpha-ethylchenodeoxycholic acid · 6-ECDCA · 6-Ethyl-CDCA
- Code names
- DSP-1747 · INT-747
- Brand names
- Ocaliva
Resolves to
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Which drugs share a target with Obeticholic acid, and which of those have an active Phase 3 trial?