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<p>HER2-positive breast cancer is characterized by aggressive tumor biology and intrinsic resistance to conventional therapies, underscoring the need for novel targeted treatment approaches. Pyrotinib, an irreversible pan-HER tyrosine kinase inhibitor (TKI), covalently binds to the intracellular kinase domains of HER1 (EGFR), HER2, and HER4, thereby inhibiting downstream signaling pathways and inducing tumor cell apoptosis. Clinical investigations have consistently demonstrated the substantial therapeutic efficacy of pyrotinib in both early-stage and advanced HER2-positive breast cancer. Moreover, its ability to traverse the blood-brain barrier confers potential therapeutic advantages in patients with brain metastases. This comprehensive review provides a systematic overview of the pharmacological profile and mechanism of action of pyrotinib, with emphasis on recent clinical trials assessing pyrotinib-based regimens in HER2-positive breast cancer.</p>

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Advances in the study of pyrotinib for the treatment of HER2-positive breast cancer

  • 期刊论文

  • 出版模式：

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  • 发表日期：

    2026年3月3日

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  • Yan Li,
  • Wen Wang,
  • Yan Liang,
  • Houyun Lai,
  • Kun Mi,
  • Purong Zhang,
  • Jianhui Zhang,
  • Yixin Wang

摘要

HER2-positive breast cancer is characterized by aggressive tumor biology and intrinsic resistance to conventional therapies, underscoring the need for novel targeted treatment approaches. Pyrotinib, an irreversible pan-HER tyrosine kinase inhibitor (TKI), covalently binds to the intracellular kinase domains of HER1 (EGFR), HER2, and HER4, thereby inhibiting downstream signaling pathways and inducing tumor cell apoptosis. Clinical investigations have consistently demonstrated the substantial therapeutic efficacy of pyrotinib in both early-stage and advanced HER2-positive breast cancer. Moreover, its ability to traverse the blood-brain barrier confers potential therapeutic advantages in patients with brain metastases. This comprehensive review provides a systematic overview of the pharmacological profile and mechanism of action of pyrotinib, with emphasis on recent clinical trials assessing pyrotinib-based regimens in HER2-positive breast cancer.