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Afatinib + pyrotinib is a combination therapy of two tyrosine kinase inhibitors (TKIs) that target the ErbB family of receptors. Afatinib is a potent and selective, irreversible ErbB family blocker that covalently binds to and blocks signaling from EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4). Pyrotinib is an irreversible ErbB TKI targeting EGFR/HER1, HER2, and HER4. This combination has shown promising efficacy in treating non-small cell lung cancer (NSCLC) with HER2 mutations or amplifications, including cases with acquired resistance to EGFR-TKIs. Clinical studies have demonstrated significant treatment responses with manageable toxicity profiles.
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