Obeticholic acid
Bile acids
Bile acids
A bile acid analogue that activates the FXR receptor, used for primary biliary cholangitis. Serious liver injury has led to restrictions.
Also called: 6-ethylchenodeoxycholic acid
Quick facts
- Group
- Bile acids
- Target
- Farnesoid X receptor (FXR, bile acid receptor)
- Used for
- Primary biliary cholangitis
- Key effects
- Itching · Fatigue and abdominal pain · Sore throat
- Monitor
- Liver function tests before · Severity of itching
- ATC
- A05AA04
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows obeticholic acid (6-ethyl-chenodeoxycholic acid) in the ligand pocket of rat FXR, which is very close to the human receptor.
Obeticholic acid is a modified form of the natural bile acid chenodeoxycholic acid and a strong agonist of FXR, a nuclear receptor in the liver and gut. FXR activation lowers the liver's production of bile acids from cholesterol and increases their transport out of liver cells. Less bile acid builds up in the damaged bile ducts and liver of primary biliary cholangitis.
- Bile acids build up in primary biliary cholangitis
- Obeticholic acid activates FXR in the liver
- Bile acid synthesis falls and export rises
- The liver is exposed to less bile acid
Indications
- Primary biliary cholangitis, with ursodeoxycholic acid when the response is inadequate or alone when it is not tolerated; withdrawn from the US market Primary biliary cholangitis →
Adverse effects
Common
- Itching (pruritus), often severe
- Fatigue and abdominal pain
- Sore throat, dizziness and constipation
- Joint pain and rash
Contraindications
- Primary biliary cholangitis with advanced cirrhosis
- Bile duct obstruction
Key interactions
- Bile acid sequestrants (colestyramine, colestipol, colesevelam)
- Bind it in the gut; taken hours apart
- Caffeine supplements
- Listed as a possible interaction
What is monitored
- Liver function tests before and during treatment
- Signs of liver disease progression: jaundice, ascites, confusion
- Severity of itching
Administration and safety
- Given by mouth, separated from bile acid sequestrants
- Stopped if liver disease progresses or there is no benefit
Pregnancy and breastfeeding
Information on use in pregnancy is limited; patients are asked to tell their doctor if they are pregnant or breastfeeding.
Nursing care
- Teach the warning signs of liver injury: yellow skin or eyes, abdominal swelling, dark urine
- Ask about itching and its effect on sleep
- Check the timing of any bile acid sequestrant
Pharmacokinetics
- Absorption
- Taken by mouth
- Metabolism
- Conjugated in the liver and cycles through bile and gut (enterohepatic circulation)
- Elimination
- Mainly in the faeces
Test yourself
Think of the answer, then tap the question to see it.
Which receptor does obeticholic acid activate?
The farnesoid X receptor (FXR), a nuclear receptor in liver and gut.
What is the most common side effect of obeticholic acid?
Itching (pruritus).
Which serious risk led regulators to restrict obeticholic acid?
Serious liver injury and liver failure, including in patients without cirrhosis.
Connections
← Back to the class: Bile acids
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Obeticholic Acid: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); STRUCTURAL BASIS FOR BILE ACID BINDING AND ACTIVATION OF THE NUCLEAR RECEPTOR FXR (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.