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网站小编 2023-04-19 17:02:21 11次大中小

Introduction

Neratinib, also known as Nerlynx or Neratinib maleate, is a medication used for the treatment of breast cancer. It belongs to the class of drugs called tyrosine kinase inhibitors (TKIs), which work by blocking the action of enzymes that promote the growth and spread of cancer cells. Neratinib is specifically used for patients with HER2-positive breast cancer, which means that the cancer cells have high levels of the HER2 protein on their surface.

Mechanism of Action

Neratinib works by irreversibly binding to the HER2 protein, which prevents it from activating other proteins that promote cell growth and pision. This action leads to the inhibition of cell proliferation and induction of apoptosis (cell death) in HER2-positive breast cancer cells. In addition, neratinib also inhibits other tyrosine kinases, such as EGFR, HER4, and Src, which are involved in the development and progression of cancer.

Clinical Trials

The efficacy and safety of neratinib have been evaluated in several clinical trials. In the ExteNET trial, which involved over 2,800 women with early-stage HER2-positive breast cancer, the addition of neratinib to standard adjuvant therapy (after surgery) significantly reduced the risk of recurrence by 34% compared to placebo. The trial also showed a 2.3% absolute improvement in disease-free survival at 5 years with neratinib. However, neratinib was associated with a high incidence of diarrhea, which led to treatment discontinuation in some patients.

Side Effects

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The most common side effect of neratinib is diarrhea, which occurs in up to 95% of patients. The severity of diarrhea can range from mild to severe and may require treatment with antidiarrheal agents. Other side effects include nausea, vomiting, fatigue, decreased appetite, abdominal pain, and rash. Rare but serious side effects of neratinib include liver toxicity, interstitial lung disease, and cardiac toxicity.

Conclusion

Neratinib is a promising treatment option for patients with early-stage HER2-positive breast cancer. Its mechanism of action and clinical efficacy have been demonstrated in several trials. However, its high incidence of diarrhea and other side effects need to be carefully managed. Further research is needed to explore the optimal dosing and duration of neratinib therapy, as well as its potential use in other types of cancer.

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