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YH43946 is an orally bioavailable, small-molecule tyrosine kinase inhibitor (TKI) that selectively targets the Human Epidermal Growth Factor Receptor 2 (HER2). Developed by Yuhan Corporation, it is a new chemical entity (NCE) currently in Phase 1 clinical development for the treatment of HER2-positive cancers, including solid tumors. The drug is designed to inhibit the intracellular kinase activity of HER2, thereby blocking the downstream signaling pathways, such as PI3K/AKT and MAPK, that drive tumor cell proliferation and survival. By specifically targeting HER2, YH43946 aims to provide a potent therapeutic option for patients with malignancies characterized by HER2 overexpression or activating mutations, potentially offering improved selectivity and reduced off-target effects compared to multi-kinase inhibitors.
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