Drug Action
Neratinib is a tyrosine kinase inhibitor.
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Drug reference
Neratinib is a tyrosine kinase inhibitor.
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HER2-overexpressed/amplified breast cancer (specialist use only) ▶BY MOUTH ▶Adult: 240 mg once daily for 1 year, dose to be taken with food, preferably in the morning, for dose adjustments due to side-effects—consult product literature
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DUE TO INTERACTIONS ▶Manufacturer advises if concurrent use of potent CYP3A4 inhibitors is unavoidable, reduce neratinib dose to 40 mg once daily.
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Cardiac risk factors or conditions which may affect left ventricular ejection fraction—consider cardiac monitoring, including assessment of left ventricular ejection fraction, as clinically indicated. elderly (increased risk of complications of diarrhoea). gastro-intestinal disorder (significant, chronic) with diarrhoea as a major symptom—no clinical experience
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Prophylactic treatment with an anti-diarrhoeal should be initiated with the first dose, and maintained during the first 1–2 months of treatment—consult product literature. The manufacturer of Nerlynx ® has provided a Risk minimisation materials document for healthcare professionals.
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NICE decisions ▶Neratinib for extended adjuvant treatment of hormone receptor-positive, HER2-positive early stage breast cancer after adjuvant trastuzumab (November 2019) NICE TA612 Neratinib (Nerlynx ®) is recommended as an option for the extended adjuvant treatment of hormone receptor- positive, human epidermal growth factor receptor 2 (HER2)-positive early stage breast cancer in adults who completed adjuvant trastuzumab-based therapy less than 1 year ago only if: . trastuzumab is the only HER2-directed adjuvant treatment they have had, and . if they had neoadjuvant chemotherapy-based regimens, they still had residual invasive disease in the breast or axilla following the neoadjuvant treatment, and . the manufacturer provides neratinib according to the commercial arrangement. Patients whose treatment was started within the NHS before this guidance was published should have the option to continue treatment, without change to their funding arrangements, until they and their NHS clinician consider it appropriate to stop. www.nice.org.uk/guidance/ta612
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→Appendix 1: neratinib
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▶Common or very common Appetite decreased. dehydration . diarrhoea. dry mouth. epistaxis. fatigue. gastrointestinal discomfort. increased risk of infection. mucositis. muscle spasms. nail discolouration. nail disorders. nausea. oral disorders. skin reactions. vomiting. weight decreased ▶Uncommon Renal failure SIDE-EFFECTS, FURTHER INFORMATION Diarrhoea may be severe and associated with dehydration. Diarrhoea is more likely to occur during initiation and may be recurrent. Manufacturer advises prophylactic treatment, with anti- diarrhoeal agent.
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Manufacturer advises females of childbearing potential should use highly effective contraception during treatment and for 1 month after last treatment; an additional barrier method of contraception should be used in females using hormonal contraceptives. Male patients should use effective contraception during treatment and for 3 months after last treatment if their partner is of childbearing potential. See also Pregnancy and reproductive function in Cytotoxic drugs p. 938.
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Manufacturer advises avoid unless potential benefit outweighs risk—toxicity in animal studies. See also Pregnancy and reproductive function in Cytotoxic drugs p. 938.
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Manufacturer advises avoid—no information available.
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Manufacturer advises avoid in severe impairment (risk of increased exposure).
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Manufacturer advises caution in mild to moderate impairment (increased risk of complications of dehydration from diarrhoea); avoid in severe impairment (no information available).
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Manufacturer advises monitor liver function (including ALT, AST, and total bilirubin) at 1 week, then monthly for the first 3 months, and every 6 weeks thereafter, during treatment or as clinically indicated. Treatment should be withheld or permanently discontinued, based on severity, in those who develop hepatotoxicity—consult product literature.
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There can be variation in the licensing of different medicines containing the same drug. Tablet CAUTIONARY AND ADVISORY LABELS 21, 25 A ▶Nerlynx (Pierre Fabre Ltd) Neratinib (as Neratinib maleate) 40 mg Nerlynx 40mg tablets | 180 tablet P £4,500.00
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A patient alert card, patient treatment journal, and patient guide should be provided. Missed doses Manufacturer advises if a dose is missed, the missed dose should not be taken and the next dose should be taken at the normal time. Driving and skilled tasks Manufacturer advises patients and carers should be counselled on the effects on driving and performance of skilled tasks—increased risk of fatigue, dizziness, dehydration, and syncope.
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240 mg once daily for 1 year, dose to be taken
First-line fragment. Read the complete Indications and Dose section above.
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