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This combination therapy consists of pyrotinib, an irreversible pan-ErbB tyrosine kinase inhibitor, alongside the monoclonal antibodies pertuzumab and trastuzumab. It is being evaluated as a precision treatment for HER2-positive salivary gland carcinoma in a Phase 2 umbrella trial sponsored by Peking Union Medical College. Pyrotinib inhibits the intracellular kinase domains of HER1 (EGFR), HER2, and HER4, while trastuzumab and pertuzumab bind to distinct epitopes on the extracellular domain of the HER2 receptor to inhibit dimerization and downstream signaling. This multi-pronged approach aims to achieve more complete blockade of the HER2 pathway to overcome resistance and improve efficacy in HER2-driven malignancies.
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