neratinib maleate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
neratinib maleate: clinical details
Prescribing considerations
- Initiation and supervision by a clinician experienced with systemic anticancer treatment.
- Plan preventive and reactive diarrhoea management before treatment begins.
- Closely assess patients with chronic gastrointestinal disease, renal impairment, cardiac risk factors or symptomatic skin disease.
- Review all medicines, supplements and dietary interactions involving CYP3A4, P-gp, BCRP or gastric pH.
Contraindications and cautions
- Hypersensitivity to neratinib or an excipient.
- Severe hepatic impairment.
- Concurrent strong CYP3A4/P-gp inducers such as carbamazepine, phenytoin, rifampicin or St John’s wort.
Monitoring
- Liver tests before and regularly during treatment, with prompt reassessment if hepatotoxicity is suspected.
- Stool frequency, hydration, renal function and weight where diarrhoea is significant.
- Cardiac function, including left ventricular ejection fraction, when clinically indicated in patients with cardiac risk factors.
- Toxicity and interacting medicines throughout treatment.
Clinical pharmacology
Neratinib is an oral, irreversible inhibitor of EGFR, HER2 and HER4. It is primarily metabolised by CYP3A4, is a P-gp substrate, is highly protein-bound and is eliminated mainly in faeces.
Formulation and product differences
- The selected UK product is a red, oval film-coated tablet marked “W104”.
- Tablets are supplied in a moisture-protective bottle containing a desiccant and should not be crushed or dissolved.
neratinib maleate preparations and strengths
Tablet
Route: Oral
Strengths: 40 mg
neratinib maleate interactions
Check all prescription, non-prescription and herbal products with the oncology pharmacist. Important examples include:
Strong CYP3A4/P-gp inducers, including carbamazepine, phenytoin, rifampicin and St John’s wort
These can markedly reduce neratinib exposure and are contraindicated.
Strong or moderate CYP3A4/P-gp inhibitors, including clarithromycin, azole antifungals, ritonavir, verapamil and diltiazem
These may increase neratinib exposure and toxicity; concurrent use is not recommended unless specialist management is possible.
Proton-pump inhibitors, including omeprazole and lansoprazole
Reduced stomach acidity can lower neratinib absorption, so concurrent use is not recommended.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.