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SYHA121-28 (also known as HA121-28) is an orally bioavailable, small-molecule multi-targeting tyrosine kinase inhibitor (TKI) developed by CSPC ZhongQi Pharmaceutical Technology (a subsidiary of CSPC Pharmaceutical Group). It primarily targets rearranged during transfection (RET) fusions, while also selectively inhibiting epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor-2 (VEGFR-2), and fibroblast growth factor receptors 1–3 (FGFR1-3). By blocking these signaling pathways, SYHA121-28 exerts dual efficacy, inhibiting both tumor cell proliferation and tumor angiogenesis. It is being clinically evaluated for the treatment of advanced solid tumors, particularly RET fusion-positive non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and biliary tract cancer.
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