NERLYNX NERATINIB 来那替尼

Neratinib is an oral tyrosine kinase inhibitor, mainly used for the extended adjuvant treatment of early HER2-positive breast cancer and the combined treatment of advanced or metastatic HER2-positive breast cancer. It inhibits the growth and spread of tumor cells by irreversibly blocking receptors such as HER2 and EGFR, and is suitable for specific patient groups to reduce the risk of recurrence. Common side effects include diarrhea, nausea, fatigue, etc., which need to be evaluated and used in combination with individual conditions.

1. Drug type and indications
Neratinib is a small molecule targeted drug, mainly for patients with HER2-positive breast cancer.

Early breast cancer: used for early patients who have completed surgery and trastuzumab (Herceptin) treatment as an extended adjuvant treatment to reduce the probability of recurrence.
Advanced or metastatic breast cancer: often used in combination with chemotherapy drugs (such as capecitabine) to control disease progression.
II. Mechanism of Action
Neratinib blocks downstream signaling pathways (such as PI3K/AKT/mTOR) and inhibits tumor cell proliferation by irreversibly binding to the tyrosine kinase domain of HER2, EGFR, and HER4 receptors. Compared with other HER2 inhibitors, its irreversible properties may prolong the duration of drug efficacy.

III. Usage and Dosage
Standard dose: 240 mg (6 tablets) orally daily for 1 year. It is recommended to take it on an empty stomach (1 hour before or 2 hours after a meal).
Dose adjustment: If severe side effects (such as grade 3 diarrhea) occur, the medication should be suspended or reduced to 160 mg/day, and antidiarrheal drugs should be used in combination.
IV. Common side effects and treatment
Diarrhea: The incidence rate is as high as more than 90%, mostly grade 1-2, but some patients may have severe diarrhea. It is recommended to use loperamide (Imodium) prophylactically and maintain adequate water intake.
Gastrointestinal reactions: such as nausea, vomiting, and abdominal pain, which can be relieved by taking the medicine in divided doses or adjusting the diet.
‌Fatigue and rash‌: Usually mild, and if severe, it is necessary to evaluate whether to stop the drug.
5. Precautions for use
‌Liver function monitoring‌: Liver function should be checked regularly before treatment and during medication to avoid drug accumulation.
‌Drug interactions‌: Avoid combined use with strong CYP3A4 inhibitors (such as ketoconazole), which may increase the blood concentration of neratinib.
‌Pregnancy and breastfeeding‌: May be harmful to the fetus, and strict contraception is required for at least 1 month after discontinuation of medication.
6. Research progress and limitations
‌Efficacy data‌: Clinical trials have shown that the 5-year disease-free survival rate of patients with early HER2-positive breast cancer increased by about 2%-5% after using neratinib.
‌Limitations‌: Ineffective for non-HER2-positive breast cancer; long-term use may produce drug resistance.
7. Patient recommendations
‌Strictly follow the doctor’s advice‌: Do not adjust the dose or stop the drug on your own.
‌Regular review‌: Including imaging examinations and tumor marker monitoring.
‌Lifestyle management‌: Maintain a balanced diet, exercise moderately, and reduce the risk of infection.
Neratinib provides an important treatment option for certain breast cancer patients, but the benefits and risks must be weighed under the guidance of a doctor to ensure safety and effectiveness.