avacopan: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
avacopan: clinical details
Prescribing considerations
- Initiate and monitor through clinicians experienced in GPA or MPA.
- The MHRA benefit–risk review remains ongoing; reassess individual benefit and risk.
- Avoid initiation where liver tests indicate significant active liver disease.
- Assess serious infection risk and relevant history, including tuberculosis, hepatitis B, hepatitis C and HIV.
- Review vaccination status; safety with live vaccines has not been established.
- Evidence is limited in severe hepatic impairment, advanced renal failure requiring dialysis or plasma exchange, severe alveolar haemorrhage and paediatric patients.
Contraindications and cautions
- Hypersensitivity to avacopan or any product excipient
Monitoring
- Check liver transaminases and total bilirubin before treatment and thereafter as clinically indicated.
- Immediately assess jaundice, pruritus or other features of liver injury; suspected vanishing bile duct syndrome requires permanent discontinuation.
- Obtain a baseline white blood cell count and monitor according to clinical status and accompanying treatment.
- Assess promptly for serious infection, unexpected bruising, bleeding or other evidence of bone-marrow suppression.
- Review interacting medicines, disease activity and adverse effects throughout treatment.
Clinical pharmacology
Avacopan is an oral, selective C5aR1 antagonist. It is highly protein bound, metabolised mainly by CYP3A4 to an active metabolite and acts as a moderate CYP3A4 inhibitor in vivo. Its terminal elimination is prolonged, so interactions and adverse effects may persist after withdrawal.
Formulation and product differences
- The gelatin hard capsule contains macrogolglycerol hydroxystearate, which may contribute to stomach upset or diarrhoea.
- The capsule must be swallowed intact; crushing, chewing and opening are not supported.
- Store in the original bottle to protect from light.
avacopan preparations and strengths
Capsule
Route: Oral
Strengths: 10 mg
avacopan interactions
Avacopan is metabolised mainly through CYP3A4 and can increase exposure to some other medicines. The full medicines and supplement list should be reviewed whenever it changes.
Strong CYP3A4 inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John's wort
These can substantially reduce avacopan exposure and should generally be avoided because disease control may be lost.
Strong CYP3A4 inhibitors, including clarithromycin and azole antifungals
These can increase avacopan exposure, so adverse-effect monitoring may be needed.
Grapefruit and grapefruit juice
These may increase avacopan concentrations and should be avoided.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.