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HA121-28 is an orally available, small molecule, multi-targeted tyrosine kinase inhibitor developed by CSPC ZhongQi Pharmaceutical Technology. It primarily inhibits the rearranged during transfection (RET) proto-oncogene receptor tyrosine kinase, as well as the epidermal growth factor receptor (EGFR) and vascular endothelial growth factor receptors (VEGFR). By targeting these kinases, HA121-28 blocks key signaling pathways involved in tumor cell proliferation and neovascularization. The drug has shown promising efficacy in patients with advanced RET fusion-positive non-small cell lung cancer (NSCLC), with a confirmed objective response rate of approximately 27% and a disease control rate over 70% in clinical trials. It is also being investigated for medullary thyroid carcinoma and biliary tract cancer[1][3][4][5]. The most common adverse events include diarrhea, rash, and QTc prolongation; cardiotoxicity requires monitoring.
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