HERNIX
NERATINIB MALEATE
What it does
Neratinib is a medication used to treat certain types of breast cancer. It works by blocking cancer cell growth.
Commonly used for: breast cancer (breast carcinoma)
Read more in plain English ↓Plain-language summary for general understanding - not medical advice. Always follow your pharmacist/doctor.
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Source: Pharmacy and Poisons Board · fetched 2026-01-28 19:57:12 · updated 2026-08-03 03:06:30
Drug Interactions
48Pharmacodynamic Warnings
Neratinib appears in TABLE 1: Drugs that cause hepatotoxicity
Severe (3)
Neratinib - increases exposure
Antifungals, azoles (fluconazole, isavuconazole, posaconazole) are predicted to increase the exposure to neratinib. Avoid moderate CYP3A4 inhibitors or adjust neratinib dose and monitor for gastrointe
Neratinib - increases exposure
Grapefruitjuiceispredictedtoincreasetheexposureto neratinib.Avoid.rTheoretical
Neratinib - decreases exposure
StJohn’swortispredictedtodecreasetheexposureto neratinib.Avoid.rTheoretical
Moderate (1)
Bictegravir - increases exposure
Neratinib is predicted to increase the exposure to bictegravir. Use with caution or avoid.
Unknown (44)
Afatinib - increases exposure
Neratinib is predicted to increase the exposure to afatinib.
Aliskiren - increases exposure
Neratinib is predicted to increase the exposure to aliskiren.
Antihistamines,non-Sedating - increases exposure
Neratinib is predicted to increase the exposure to antihistamines, non-sedating (fexofenadine).
Apixaban - increases exposure
Neratinibispredictedtoincreasetheexposuretoapixaban. oTheoretical
Berotralstat - increases exposure
Neratinib is predicted to increase the exposure to berotralstat.
Data from BNF 85 (British National Formulary). This is not a substitute for professional medical advice. Matched via: exact
About this medicine
Neratinib is a medication used to treat certain types of breast cancer. It works by blocking cancer cell growth.
What it treats
- breast cancer (breast carcinoma)
How it works
Neratinib interferes with the signals that help cancer cells grow, which can slow down or stop their growth.
Who it's for
This medication is for adults with specific types of breast cancer that are hormone receptor-positive.
Cautions
- • Use with caution if you are taking other drugs that can harm the liver.
AI-assisted summary grounded in BNF data - general information only, not medical advice. Always confirm with your pharmacist or doctor.
Clinical monograph: Neratinib
BNF-referencedNeratinib is a targeted therapy that functions as a tyrosine kinase inhibitor, primarily used in the treatment of HER2-overexpressed or amplified breast cancer. It irreversibly binds to and inhibits the activity of human epidermal growth factor receptors, specifically EGFR, HER2, and HER4, leading to reduced cell proliferation and tumor growth. It is administered orally and has specific considerations for prophylactic treatment to manage diarrhea associated with its use.
Indications
- HER2-overexpressed or amplified breast cancer
- Extended adjuvant treatment of hormone receptor-positive, HER2-positive early-stage breast cancer after adjuvant trastuzumab therapy
Dosage
Adults: 40 mg once daily for 1 year. Prophylactic treatment with an anti-diarrhoeal should be initiated with the first dose and maintained during the first 1-2 months of treatment.
Mechanism of action
Neratinib binds to and irreversibly inhibits EGFR, HER2, and HER4. This action prevents autophosphorylation of tyrosine residues on these receptors, thereby reducing oncogenic signaling through the mitogen-activated protein kinase and Akt pathways.
Pharmacodynamics
As a tyrosine kinase inhibitor, Neratinib exhibits antitumor activity against carcinomas that are positive for Epidermal Growth Factor Receptor (EGFR), HER2, and Human Epidermal Growth Factor Receptor 4 (HER4). Its pharmacodynamic effects include inhibiting cancer cell growth and inducing apoptosis in these receptor-positive tumors.
Pharmacokinetics
Neratinib is absorbed following oral administration, with a bioavailability that may be affected by food. It is extensively metabolized in the liver, primarily by the CYP3A4 enzyme. The elimination half-life is approximately 24 hours, allowing for once-daily dosing. It is primarily eliminated via feces, with a small portion excreted in urine. Drug interactions, particularly with CYP3A4 inhibitors or inducers, may significantly impact its pharmacokinetic profile.
Adverse effects
- diarrhoea
- dehydration
- appetite decreased
- dry mouth
- epistaxis
- fatigue
- gastrointestinal discomfort
- increased risk of infection
- mucositis
- muscle spasms
- nail discolouration
- nausea
- vomiting
- weight decreased
- renal failure
Interactions
- antifungals, azoles (severe - increases exposure)
- grapefruit juice (severe - increases exposure)
- St. John's Wort (severe - decreases exposure)
- bictegravir (moderate - increases exposure)
- afatinib (unknown - increases exposure)
- aliskiren (unknown - increases exposure)
- dronedarone (unknown - increases exposure)
- fexofenadine (unknown - increases exposure)
- berotralstat (unknown - increases exposure)
- ciclosporin (unknown - increases exposure)
Precautions
- consider cardiac monitoring in patients with cardiac risk factors or left ventricular ejection fraction conditions
- initiate prophylactic treatment with anti-diarrhoeal agents at the start of therapy
Pregnancy
Manufacturer advises females of childbearing potential to use highly effective contraception during treatment and for 1 month after last treatment.
Breast-feeding
Manufacturer recommends caution, as it is unknown whether neratinib is excreted in human milk.
Storage
Store at room temperature, away from moisture and light.
Formulations
- {'name': 'Nerlynx', 'strength': '40 mg', 'form': 'tablet'}
AI-synthesized from BNF references - general information only, not a substitute for professional medical advice or the current BNF. Verify doses with a pharmacist.
Molecular reference: Neratinib
PubChem CID 9915743Molecular formula: C30H29ClN6O3
Mechanism of action
Neratinib binds to and irreversibly inhibits EGFR, HER2, and HER4. This prevents auotphoshorylation of tyrosine residues on the receptor and reduces oncogenic signalling through the mitogen-activated protein kinase and Akt pathways.
Pharmacodynamics
Neratinib is a tyrosine kinase inhibitor which exhibits antitumor action against Epidermal Growth Factor Receptor (EGFR), HER2, and Human Epidermal Growth Factor Receptor 4 (HER4) postive carcinomas.
Biological pathways
Source: PubChem (NCBI) · pathways from PathBank, Reactome, WikiPathways & PharmGKB.