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YH42946 is a novel, orally available small molecule tyrosine kinase inhibitor that targets HER2 (also known as receptor protein-tyrosine kinase erbB-2) and EGFR exon 20 insertion mutations. It has demonstrated potency against diverse HER2 aberrations—including overexpression, amplification, and mutation—as well as activity against EGFR exon 20 insertions. Preclinical studies showed strong efficacy in both in vitro and in vivo models for tumors with these genetic alterations. The drug is being developed primarily for the treatment of locally advanced or metastatic solid tumors with HER2 aberrations or EGFR exon 20 insertions, including non-small cell lung cancer (NSCLC). The developer is Yuhan Corporation; the compound originated from Jintz Bio.
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