Abstract

Tucatinib (TUC), a highly selective HER2-directed TKI with minimal EGFR inhibition, is approved in combination with trastuzumab (Tras) and capecitabine for adult patients (pts) with HER2 overexpressed/amplified (HER2+) locally-advanced unresectable or metastatic (LAUM) breast cancer (BC). Dual targeting of HER2 with TUC and Tras showed superior activity to either agent alone in HER2+ and HER2-mutated (HER2-mut) xenograft models. Currently, HER2-directed therapies are approved only in HER2+ BC and gastric cancer.

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