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Neratinib: Uses, Mechanism of Action & Side Effects

Neratinib is a targeted cancer medicine used to treat HER2-positive breast cancer. It blocks growth signals in tumour cells and is taken as an oral tablet once daily.

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Things worth knowing about "Neratinib"

Neratinib is a targeted cancer medicine used to treat HER2-positive breast cancer. It blocks growth signals in tumour cells and is taken as an oral tablet once daily.

What is Neratinib?

Neratinib is an orally administered, targeted therapy belonging to the class of tyrosine kinase inhibitors (TKIs). It is used in oncology -- the medical specialty focused on the diagnosis and treatment of cancer -- and was specifically designed to block certain proteins on the surface of cancer cells that drive uncontrolled tumour growth.

Approved Indications and Uses

Neratinib has been approved by both the European Medicines Agency (EMA) and the US Food and Drug Administration (FDA) for the following indications:

Extended adjuvant treatment of early-stage, HER2-positive breast cancer in adults: Neratinib is used following the completion of trastuzumab-based adjuvant therapy to reduce the risk of disease recurrence.
Combination therapy for advanced HER2-positive breast cancer: In combination with the chemotherapy agent capecitabine in patients who have received at least two prior HER2-directed regimens.

HER2 (Human Epidermal Growth Factor Receptor 2) is a receptor found on the surface of cells that, when overexpressed, promotes the growth and spread of certain breast cancers.

Mechanism of Action

Neratinib acts as an irreversible pan-HER tyrosine kinase inhibitor. This means it permanently and covalently binds to the tyrosine kinase domains of the HER receptor family, specifically:

HER1 (also known as EGFR, Epidermal Growth Factor Receptor)
HER2 (also known as ErbB2)
HER4 (also known as ErbB4)

By blocking these receptors, neratinib prevents the transmission of growth signals into the tumour cell. As a result, cancer cells can no longer divide uncontrollably and undergo programmed cell death. Because the binding is irreversible, neratinib provides more sustained inhibition compared to reversible inhibitors in the same class.

Dosage and Administration

Neratinib is taken orally as a film-coated tablet at a standard dose of 240 mg once daily, together with food. In the extended adjuvant setting, the standard duration of treatment is twelve months. The exact dosage is determined individually by the treating physician and may be adjusted in response to side effects.

Side Effects

The most frequent and clinically significant side effect of neratinib is diarrhoea, which occurs in the majority of patients, particularly at the start of treatment, and can lead to dehydration if severe. To minimise this risk, prophylactic treatment with loperamide is strongly recommended at the beginning of therapy.

Other possible side effects include:

Nausea and vomiting
Abdominal pain and cramping
Decreased appetite and weight loss
Fatigue and general weakness
Skin rash and dry skin
Elevated liver enzyme levels (hepatotoxicity)
Inflammation of the mucous membranes in the mouth (stomatitis)

Patients should seek prompt medical advice if they experience persistent or severe side effects.

Interactions and Contraindications

Neratinib is metabolised primarily by the liver enzyme CYP3A4. Substances that inhibit this enzyme (e.g., certain antifungal agents or antibiotics) can increase neratinib blood levels and thus raise the risk of side effects. Conversely, CYP3A4 inducers (e.g., rifampicin or St. John's wort) can reduce the effectiveness of neratinib. Neratinib is contraindicated in patients with severe hepatic impairment and must not be used during pregnancy or breastfeeding due to potential harm to the unborn child.

References

European Medicines Agency (EMA): Neratinib (Nerlynx) - EPAR Product Information. Available at: www.ema.europa.eu (accessed 2024)
Martin M. et al. - Neratinib after trastuzumab-based adjuvant therapy in HER2-positive breast cancer. New England Journal of Medicine, 2017; 376(24):2336-2346.
Chan A. et al. - Neratinib after adjuvant chemotherapy and trastuzumab in HER2-positive early breast cancer (ExteNET): 5-year analysis of a randomised, double-blind, placebo-controlled, phase 3 trial. The Lancet Oncology, 2016; 17(3):367-377.

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