Products
Obeticholic acid is commercially available in the form of film-coated tablets (Ocaliva). It has been approved in the EU and US since 2016 and in many countries since 2018.
Structure and properties
Obeticholic acid (C26H44O4, Mr = 420.6 g/mol) exists as a white powder that is highly soluble in water at a high pH.
Effects
The effects of obeticholic acid (ATC A05AA04) are due to selective agonism at the nuclear receptor farnesoid X receptor (FXR). Activation of FXR decreases bile acid concentrations in liver cells. FXR is expressed in the liver and intestine. Obeticholic acid, on the one hand, inhibits the synthesis of bile acids from cholesterol and promotes their removal from hepatocytes.
Indications
For the treatment of primary biliary cholangitis.
Dosage
According to the professional information leaflet.
Contraindications
- Hypersensitivity
- Total bile duct obstruction
Full precautions can be found in the drug label.
Interactions
Drug-drug interactions have been described with vitamin K antagonists (warfarin), CYP1A2 substrates, and bile acid-binding resins such as cholestyramine.
Adverse effects
The most common potential adverse effects include pruritus, abdominal pain and discomfort, and fatigue.