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Lunbotinib (also known as A400, EP0031, or KL590586) is an orally bioavailable, next-generation selective RET tyrosine kinase inhibitor developed by Sichuan Kelun-Biotech Biopharmaceutical (Kelun Group) and licensed to Ellipses Pharma for development outside of Greater China. It is designed to target RET fusions and mutations, including solvent front resistance mutations (such as RET G810R/S/C) that emerge after treatment with first-generation RET inhibitors like selpercatinib and pralsetinib. Lunbotinib has demonstrated high potency, favorable blood-brain barrier penetration, and robust clinical efficacy in patients with RET fusion-positive non-small cell lung cancer (NSCLC), medullary thyroid cancer (MTC), and other RET-altered solid tumors. A New Drug Application (NDA) for lunbotinib fumarate has been accepted for review by the National Medical Products Administration (NMPA) of China for the treatment of RET fusion-positive locally advanced or metastatic NSCLC.
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