Omaveloxolone: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
Omaveloxolone: clinical details
Prescribing considerations
- Initiation and supervision should be by a physician experienced in treating Friedreich’s ataxia.
- Review hepatic function, cardiovascular and fluid-overload risk, weight, pregnancy potential and interacting medicines before treatment.
- Avoid use in severe hepatic impairment; exposure is increased in moderate hepatic impairment.
- Effects in moderate or severe renal impairment have not been established.
Contraindications and cautions
- Hypersensitivity to omaveloxolone or any excipient.
Monitoring
- Check ALT, AST and bilirubin before treatment, monthly during the first three months, and periodically thereafter as clinically indicated.
- Assess lipids and BNP before treatment and periodically during treatment.
- Monitor body weight and investigate unexplained or clinically significant loss.
- Assess urgently for fluid overload; interrupt treatment while fluid overload is managed.
Clinical pharmacology
Omaveloxolone binds Keap1, permitting Nrf2 nuclear translocation and transcription of antioxidant-response genes. It is primarily metabolised by CYP3A4, is highly protein-bound and is eliminated predominantly through faeces following metabolism.
Formulation and product differences
- The selected UK product is a hard capsule.
- Capsules may be swallowed whole or opened and sprinkled onto apple puree for people unable to swallow them whole.
- The prepared apple-puree mixture must be consumed immediately and must not be stored.
Omaveloxolone preparations and strengths
Capsule
Route: Oral
Strengths: 50 mg
Omaveloxolone interactions
Check all prescribed, over-the-counter and herbal products before treatment.
Strong or moderate CYP3A4 inhibitors, including itraconazole, ketoconazole, clarithromycin, fluconazole, ciprofloxacin, ciclosporin and fluvoxamine
These can increase omaveloxolone exposure and adverse effects; concurrent use should generally be avoided or managed by the specialist.
CYP3A4 inducers, including carbamazepine, phenytoin, phenobarbital, primidone, rifampicin, efavirenz and St John’s wort
These can lower omaveloxolone exposure and reduce its effectiveness, so alternatives should be considered.
Hormonal contraceptives
Omaveloxolone may reduce contraceptive effectiveness; use an alternative or additional non-hormonal method as advised.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.