brigatinib: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
brigatinib: clinical details
Prescribing considerations
- Initiate and supervise treatment through a clinician experienced in anticancer therapy.
- Confirm ALK-positive advanced NSCLC using a validated assay before treatment.
- Review pulmonary history, recent crizotinib exposure, cardiovascular status, diabetes, visual symptoms and concomitant medicines.
- Severe renal or hepatic impairment increases exposure and requires product-specific specialist management.
- Advise sun protection because photosensitivity can occur.
- Discuss contraception, pregnancy, breastfeeding and potential male fertility effects.
Contraindications and cautions
- Hypersensitivity to brigatinib or any excipient.
- Use particular caution with previous interstitial lung disease or drug-induced pneumonitis, hypertension, bradycardia, visual disorders, diabetes and severe renal or hepatic impairment.
- The tablets contain lactose and are unsuitable for specified rare hereditary disorders of galactose handling.
Monitoring
- Assess promptly for new or worsening respiratory symptoms, especially early in treatment.
- Monitor blood pressure and heart rate.
- Check liver function, fasting glucose, creatine phosphokinase, amylase and lipase at baseline and regularly during treatment.
- Investigate new or worsening visual symptoms; severe symptoms warrant ophthalmological assessment.
- Review blood counts, renal function and electrolytes as clinically indicated.
- Monitor closely when clinically significant CYP or transporter interactions cannot be avoided.
Clinical pharmacology
Brigatinib is an oral tyrosine-kinase inhibitor targeting ALK, ROS1 and IGF-1R. It suppresses ALK autophosphorylation and downstream STAT3 signalling. Metabolism is mainly through CYP2C8 and CYP3A4, and brigatinib can induce CYP3A.
Formulation and product differences
- Film-coated oral tablets contain lactose.
- Tablets must be swallowed whole rather than crushed or dissolved.
- Bottle packs contain a desiccant canister that should remain in the bottle and must not be swallowed.
brigatinib preparations and strengths
Tablet
Route: Oral
Strengths: 30 mg, 90 mg, 180 mg
brigatinib interactions
Check prescribed, non-prescribed and herbal products before starting brigatinib. Important examples include:
Strong CYP3A inhibitors, including itraconazole, voriconazole, clarithromycin and ritonavir
These can substantially increase brigatinib exposure and should generally be avoided unless specialist management is arranged.
CYP3A inducers, including rifampicin, carbamazepine, phenytoin and St John’s wort
These can reduce brigatinib exposure and potentially reduce its effectiveness, so concomitant use should be avoided.
Grapefruit and grapefruit juice
These may increase brigatinib 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.