Must-read for patients: Overview of basic information in the Chinese instructions for neratinib maleate/neratinib

1. Generic names: Neratinib, Neratinib

Product name:Nerlynx, He Li'an

Other names: neratinib, neratinib maleate tablets, neratinib maleate

2. Who can take neratinib? Indications?

1. Extended adjuvant treatment of early-stage breast cancer: Neratinib/Neratinib (Neratinib) as a single drug is suitable for extended adjuvant treatment of adult patients with early-stage human epidermal growth factor receptor 2 (HER2)-positive breast cancer to receive trastuzumab-based adjuvant treatment.

2. Advanced or metastatic breast cancer: Neratinib is combined with capecitabine to treat adult patients with advanced or metastatic HER2-positive breast cancer who have received two or more anti-HER2-based regimens in the metastatic setting.

3. What are the side effects of neratinib?

The most common side effect of neratinib is diarrhea, which affects almost all patients. Other common side effects include nausea, abdominal pain, fatigue, vomiting, rash, stomatitis, decreased appetite, muscle cramps, indigestion, nail abnormalities, dry skin, bloating, nose bleeding, weight loss, and urinary tract infections.

4. How should you take neratinib?

1. Usage and dosage:

(1) Dosage: For extended adjuvant treatment of patients with early-stage breast cancer, the recommended dose of neratinib is 240 mg (6 tablets) taken orally once a day, taken with food, and continued until disease recurrence or up to one year. For patients with advanced or metastatic breast cancer, the recommended dose is also 240mg (6 tablets), atAdminister capecitabine orally once daily with food on days 1-21 of a 21-day cycle, plus capecitabine 750 mg/m2 orally twice daily on days 1-14 of a 21-day cycle until disease progression or unacceptable toxicity occurs.

(2) Usage: Neratinib is a tablet. Patients are instructed to take Neratinib at approximately the same time each day with a meal and should swallow it whole (the tablet should not be chewed, crushed, or separated before swallowing). If a patient misses a dose, do not replace the missed dose and instruct the patient to continue taking neratinib with the next scheduled daily dose.

2. Medication management: The most common side effect of using neratinib is diarrhea. Doctors will instruct patients to take antidiarrheal prevention for 56 days before treatment. The drugs include loperamide on days 1-14. The dose is 4 mg three times a day; the drug dose on days 15-56 is 4 mg twice a day; after the 56th day or when the drug needs to be discontinued due to illness, 4 mg is taken as needed, not exceeding 16 mg per day, and the dose is titrated to achieve 1-2 bowel movements per day. If diarrhea still occurs after prophylaxis, treat with antidiarrheal agents, fluids, and electrolytes as clinically indicated. Interruption and dose reduction of latinib may also be necessary to control diarrhea.

5. How to store neratinib?

Neratinib needs to be stored at controlled room temperature,20°C to 25°C (68°F to 77°F); tolerances to 15°C to 30°C (59°F to 86°F) are allowed.

6. How does neratinib work?

Neratinib is an intracellular kinase inhibitor that irreversibly binds to the epidermal growth factor receptor (EGFR), HER2 and HER4. In vitro, neratinib reduced EGFR and HER2 autophosphorylation, downstream MAPK and AKT signaling pathways, and showed antitumor activity in cancer cell lines expressing EGFR and/or HER2. The human metabolites M3, M6, M7 and M11 of neratinib inhibit the activities of EGFR, HER2 and HER4 in vitro. In vivo, oral neratinib inhibited tumor growth in a mouse xenograft model with tumor cell lines expressing HER2 and EGFR.

7. What will happen if you overdose on neratinib?

There is currently no specific antidote for neratinib, and the benefit of hemodialysis in treating neratinib overdose is unclear. In case of overdose, administration should be discontinued and general supportive measures instituted. Overdose has been reported in a small number of patients during clinical trials. Adverse effects in these patients include diarrhea, nausea, vomiting, and dehydration. The frequency and severity of gastrointestinal disorders (diarrhoea, abdominal pain, nausea, and vomiting) appear to be dose-related.

8. Who cannot use neratinib?

1. Neratinib is contraindicated in patients who are allergic to neratinib and other ingredients.

2. Based on the findings and mechanism of action of animal studies, neratinib can cause fetal damage when administered to pregnant women. For specific medication information, it is recommended that women of reproductive potential, lactating women and their partners consult their doctors.