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Neratinib tablets

Updated 2 Feb 2023 | Breast cancer


Oral formulations of neratinib.

Drugs List

  • neratinib 40mg film coated tablets
  • NERLYNX 40mg film coated tablets
  • Therapeutic Indications


    HER2 +ve early breast cancer

    Indicated for the extended adjuvant treatment of adult patients with early stage hormone receptor positive HER2 overexpressed or amplified breast cancer and who completed adjuvant trastuzumab-based therapy less than a year ago.


    Whilst the doses stated below are those recommended by the manufacturer, local cancer network protocols for the relevant indication should be consulted.


    Initial dose: 240mg daily, continuously for one year
    First dose reduction: 200mg daily
    Second dose reduction: 160mg daily
    Third dose reduction: 120mg daily

    Discontinue neratinib for patients who:
    Fail to recover to grade 1 or less from treatment-related toxicity,
    Toxicities that result in a treatment delay of more than 3 weeks,
    Unable to tolerate a dose of 120mg daily.

    Additional Dosage Information

    If concurrent use of a moderate CYP3A4/P-pg inhibitor is necessary, reduce dose to 40mg once daily. If tolerated, increase dose by 40mg at least every 7 days. Maximum dose 160mg daily. If concurrent use of a potent CYP3A4/P-gp inhibitor is necessary, reduce dose to 40mg daily.

    Missed dose
    Missed doses should not be replaced and treatment should resume with the next scheduled daily dose.

    Severity of toxicity
    Grade 3: Stop neratinib treatment until recovery to less than or equal to grade 1 or baseline toxicity within 3 weeks of stopping treatment. Resume neratinib at the next lowest dose.

    Severity of diarrhoea
    Grade 1 (increase of more than 4 stools per day over baseline), Grade 2 (increase of 4-6 stools per day over baseline) lasting more than 5 days or Grade 3 (increase of 7 or more stools per day over baseline) lasting 2 or more days:
    Adjust anti-diarrhoeal treatment
    Modify diet
    Intake of 2 litres of fluid to avoid dehydration
    Once event resolves to Grade 1 or baseline, consider restarting anti-diarrhoea prophylaxis if appropriate with each neratinib administration.

    Any grade with complicated features, Grade 2 lasting 5 days or longer or Grade 3 lasting between 2 days and 3 weeks:
    Interrupt treatment
    Modify diet
    Intake of 2 litres of fluid to avoid dehydration
    If resolved to Grade 1 or less in one week, then resume treatment at the same dose
    If resolved to Grade 1 or less in longer than one week, then resume treatment at reduced dose
    Once event resolves to Grade 1 or baseline, consider restarting anti-diarrhoea prophylaxis if appropriate with each neratinib administration.
    If Grade 3 diarrhoea persists longer than 3 weeks, discontinue neratinib permanently.

    Diarrhoea recurs to Grade 2 or higher at 120mg per day: Discontinue neratinib.

    Grade 3 ALT (greater than 5 times the normal upper limit) or Grade 3 bilirubin (greater than 3 times the normal upper limit):
    Stop neratinib until recovery to less than or equal to Grade 1
    Evaluate alternative causes
    Resume neratinib at next lowest dose if recovery to Grade 1 or less within 3 weeks. Discontinue if Grade 3 reoccurs despite dose reduction.


    Children under 18 years
    Severe hepatic impairment
    Severe renal impairment

    Precautions and Warnings

    History of cardiac disorder
    Reduced left ventricular function
    Renal impairment

    Advise ability to drive/operate machinery may be affected by side effects
    Anti-diarrhoeals may be required during treatment
    Avoid H2 antagonists 10 hours before or 2 hours after dose
    Treatment to be initiated and supervised by a specialist
    Consult local policy on the safe use of oral anti-cancer drugs
    Staff: Not to be handled by pregnant staff
    Perform liver tests at 1 week, monthly for 3 months, then every 6 weeks
    Consider monitoring LVEF in patients who develop cardiac signs/symptoms
    Monitor patients with renal impairment
    Monitor renal function in elderly patients
    Advise patient to monitor for and report any skin changes
    Discontinue if grade 4 toxicity occurs
    Discontinue permanently if AST or ALT level exceeds 20 x ULN
    Discontinue permanently if grade 4 diarrhoea occurs
    Discontinue treatment if total bilirubin > 10 x ULN
    Interrupt therapy if elevations in bilirubin of > 3 x ULN occur
    Interrupt treatment for any grade 3 toxicity
    Interrupt treatment if ALT or AST > 5 x ULN
    Recurrent grade 2 diarrhoea or higher at 120mg/day: Discontinue permanently
    Advise patient not to take St John's wort concurrently
    Avoid antacids within 3 hours of dose
    Advise patient to avoid grapefruit products
    Advise patient to avoid pomegranate products
    Female: Barrier or non-hormonal contraception required during treatment
    Female: Contraception required during and for 1 month after treatment
    Male: Use barrier contraception during and for 3 months after treatment
    Avoid concurrent use of proton pump inhibitors

    Instruct patient to initiate prophylactic treatment with anti-diarrhoeal product with first dose of neratinib, and maintain regular dosing of anti-diarrhoeal for first 1 to 2 months of neratinib.

    Monitor patients with chronic gastrointestinal disorder with diarrhoea as a major symptom.

    Perform cardiac monitoring, including assessment of left ventricular ejection fraction in patients with known cardiac risk factors.

    Pregnancy and Lactation


    Neratinib is contraindicated during pregnancy.

    The manufacturer does not recommend using neratinib during pregnancy. Animal studies have shown teratogenic effects. Human data is limited and as such a potential risk cannot be ruled out.


    Neratinib is contraindicated during breastfeeding.

    The manufacturer advises that the patient either discontinues neratinib or discontinues breastfeeding. The presence of neratinib in human breast milk and the effect on exposed infants are unknown.


    Take with or just after food, or a meal, preferably in the morning.

    Swallow this medicine whole, do not chew or crush.

    Do not take proton pump inhibitors while taking this drug.

    Do not take H2 antagonists 10 hours before or 2 hours after dose.

    Advise patient to avoid grapefruit products.

    Advise patient to avoid pomegranate products.

    Advise patient to report any skin changes.

    Female patients should be advised that contraception is required during and for one month after treatment. Barrier or non hormonal contraception is required.

    Male patients should be advised to use barrier contraception during and for three months after treatment.

    May affect ability to drive or operate machinery.

    Side Effects

    Abdominal distension
    Abdominal pain
    Alanine aminotransferase increased
    Aspartate aminotransferase increased
    Decreased appetite
    Dry mouth
    Dry skin
    Mouth ulcers
    Mucosal inflammation
    Muscle spasm
    Nail disorders
    Oral mucosal blistering
    Renal failure
    Serum bilirubin increased
    Serum creatinine increased
    Skin fissures
    Upper abdominal pain
    Urinary tract infections
    Weight loss


    It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.

    The following number will direct the caller to the relevant local centre (0844) 892 0111

    Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( ) or if this is unavailable at the backup site ( ).

    Further Information

    Last Full Review Date: November 2019

    Reference Sources

    Summary of Product Characteristics: Nerlynx 40mg Film-coated Tablets. Pierre Fabre Limited. Revised April 2022.

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