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Pyrotinib is an orally administered, irreversible small molecule tyrosine kinase inhibitor that targets multiple members of the ErbB family, specifically epidermal growth factor receptor (EGFR/HER1), human epidermal growth factor receptor 2 (HER2/ErbB2), and HER4. By covalently binding to the ATP-binding site of these receptors' intracellular kinase domains, pyrotinib blocks their phosphorylation and activation, thereby inhibiting downstream signaling pathways such as RAS/RAF/MEK/MAPK and PI3K/AKT. This results in reduced tumor cell proliferation and increased apoptosis. Pyrotinib was developed primarily for the treatment of HER2-positive advanced or metastatic breast cancer, especially in patients previously treated with anthracyclines or taxanes. It has demonstrated efficacy even in trastuzumab-resistant cases and is conditionally approved in China for use in combination with capecitabine for this indication[1][3][4][5][7][8].
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