FXR Agonist (Primary Biliary Cholangitis) Pregnancy: There are no data on the use of obeticholic acid in pregnant women; animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid use during pregnancy. Breast-feeding: it is unknown whether obeticholic acid is excreted in human milk — a decision must be made whether to discontinue breast-feeding or to discontinue/abstain from therapy.

Obeticholic Acid

Brand names: Ocaliva

Obeticholic acid is a farnesoid X receptor agonist used as second-line treatment for primary biliary cholangitis, usually combined with ursodeoxycholic acid when response is inadequate or as monotherapy in intolerance.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: Starting dose 5 mg once daily for the first 6 months. After the first 6 months, for patients who have not achieved an adequate reduction in alkaline phosphatase (ALP) and/or total bilirubin and who are tolerating obeticholic acid, increase to a maximum dose of 10 mg once daily.

Route: Oral — tablet taken with or without food

Frequency: Once daily

Max: 10 mg once daily

Prior to initiation the patient's hepatic status must be known; determine whether the patient has decompensated cirrhosis (including Child-Pugh Class B or C) or a prior decompensation event, because obeticholic acid is contraindicated in these patients. No dose adjustment of concomitant UDCA is required. Dose adjustment for severe pruritus: the dose may be reduced to 5 mg every other day (for patients intolerant to 5 mg once daily) or to 5 mg once daily (for patients intolerant to 10 mg once daily); the dose may be temporarily interrupted for up to 2 weeks followed by restarting at a reduced dose; the dose may be increased to 10 mg once daily, as tolerated, to achieve optimal response. Discontinuation may be considered for persistent, intolerable pruritus. Bile acid binding resins: administer obeticholic acid at least 4 to 6 hours before or 4 to 6 hours after the resin, or at as great an interval as possible. Missed dose: skip the missed dose and resume the normal schedule; do not take a double dose. Elderly (>=65 years): no dose adjustment required (limited data). Hepatic impairment: contraindicated in decompensated cirrhosis (e.g. Child-Pugh Class B or C) or a prior decompensation event. Paediatric population: the SPC states 'There is no relevant use of obeticholic acid in the paediatric population in the treatment of PBC.' NOTE: the fetched SPC section 4.4 was truncated at the source-fetch limit and section 4.5 (interactions) was not retrieved — the interaction list below is therefore incomplete.

Dose adjustments

Renal

No dose adjustment is required for patients with renal impairment.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients
Patients with decompensated cirrhosis (e.g. Child-Pugh Class B or C) or a prior decompensation event
Patients with complete biliary obstruction

Side effects

Pruritus (very common; reported in 63% of patients, and the most common reaction leading to discontinuation)
Fatigue (very common; 22%)
Abdominal pain and discomfort (common)
Arthralgia (common)
Eczema and rash (common)
Hepatic failure, blood bilirubin increased, jaundice, hepatic cirrhosis (frequency not known)

Interactions

Bile acid binding resins — obeticholic acid should be administered at least 4 to 6 hours before or 4 to 6 hours after taking a bile acid binding resin, or at as great an interval as possible (stated in SPC section 4.2, cross-referencing section 4.5; section 4.5 itself was NOT retrieved in this fetch, so this list is incomplete)

Clinical monograph

How it works

As a potent agonist of the nuclear farnesoid X receptor, it modulates bile acid synthesis, transport and secretion, reducing the hepatic accumulation of toxic bile acids that drives cholestatic liver injury.

Prescribing in practice

It is contraindicated in decompensated cirrhosis and complete biliary obstruction, and the MHRA has warned of serious liver injury and the need for careful dosing and monitoring in those with hepatic impairment.
Dose-related pruritus is the most common adverse effect and can limit tolerability, sometimes requiring dose adjustment or symptomatic treatment.
It can reduce HDL cholesterol and may require less frequent dosing in moderate to severe hepatic impairment.

Monitoring

Monitor liver biochemistry regularly to assess response and detect hepatotoxicity, and review for worsening cholestatic itch and signs of hepatic decompensation.

Counselling the patient

Report any worsening itching, which is common and can often be managed.
Seek prompt advice if you notice jaundice, dark urine, abdominal swelling or confusion.
Attend your blood tests so your liver function can be checked.

Evidence & guidelines

Obeticholic acid is recommended by NICE as an option for primary biliary cholangitis inadequately controlled by, or intolerant of, ursodeoxycholic acid, with MHRA safety advice on hepatic monitoring.

Reference: NICE TA443 (obeticholic acid for PBC); Nevens et al. Lancet 2016 (POISE trial); MHRA Drug Safety Update 2021 (hepatic decompensation); EASL PBC Clinical Practice Guidelines 2017; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways