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Neratinib was approved by the FDA on February 25, 2020, in combination with capecitabine for the treatment of patients with advanced or metastatic HER2-positive breast cancer, provided that the patient has received at least two anti-HER2 therapies in the metastatic setting.
1. Generic name: Neratinib (neratinib)
2. Trade name: NERLYNX®
It is used for extended adjuvant treatment of early-stage HER2 overexpression/amplification breast cancer in adults and needs to be used after adjuvant treatment with trastuzumab.
1. Tablet: 40mg (equivalent to 48.31mg neratinib maleate).
2. Properties: film-coated tablets.
1. Active ingredient: neratinib (tyrosine kinase inhibitor)
2. Excipients: colloidal silica, mannitol, microcrystalline cellulose, crospovidone, povidone, magnesium stearate, purified water (tablet core); polyvinyl alcohol, titanium dioxide, polyethylene glycol, talc, iron oxide red (coating).
1. Recommended dose : 240mg (6 tablets) once a day, taken orally with food, for continuous use for 1 year.
2. Diarrhea prevention : Start using loperamide when first administered, continue for the first 2 cycles (56 days), and maintain 1-2 bowel movements per day.
4. Treatment of missed doses : Skip the dose of the day and take the medicine as originally planned the next day.
1. Diarrhea management :
Grade 1 diarrhea or grade 2 diarrhea (<5 days): adjust antidiarrheal drugs and maintain fluid rehydration.
Grade 2 diarrhea (≥5 days) or grade 3 diarrhea: suspend medication and reduce dosage after recovery.
Grade 4 diarrhea or recurrence after dose reduction to 120 mg: Permanently discontinue treatment.
2. Hepatotoxicity :
Grade 3 liver enzyme abnormalities: suspend until recovery and then reduce dose.
Grade 4 liver enzyme abnormalities: Permanent discontinuation.
3. Hepatic insufficiency : The starting dose is reduced to 80mg in patients with severe liver impairment (Child-PughC).
1. Medication time : It needs to be taken with meals and at a fixed time every day.
2. Gastric acid regulator :
Avoid combined use with proton pump inhibitors (PPI) or H2 receptor antagonists.
Antacids should be taken 3 hours apart.
3. Drug interactions :
Avoid the combined use of strong/moderate CYP3A4 inhibitors (such as ketoconazole) or inducers (such as rifampicin).
Monitor adverse reactions to P-gp substrates (such as digoxin).
1. Pregnant women: may cause fetal harm. Effective contraception is required during treatment and within 1 month after the last dose.
2. Lactation : Breastfeeding is prohibited during treatment and within 1 month after the last dose.
3. Liver insufficiency : Severe liver damage requires dose reduction.
4. Children’s : safety and effectiveness have not been established.
1. Common (>5%) : diarrhea (95%), nausea (43%), abdominal pain (36%), fatigue (27%), vomiting (26%), rash (18%).
2. Serious adverse reactions :
Diarrhea (40% grade 3, 0.1% grade 4)
Hepatotoxicity (1.7% leading to discontinuation)
There are no absolute contraindications, but it should be used with caution in those known to be allergic to ingredients.
1. CYP3A4 inhibitor/inducer : significantly affects the plasma concentration of neratinib, so combined use should be avoided.
2. P-gp substrate : may increase the toxicity of digoxin and other drugs.
Save at room temperature (20-25°C) and avoid moisture.