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Brigatinib/Brigatinib (Brigatinib) mechanism of action
Brigatinib/Brigatinib inhibits the proliferation and in vitro viability of cells expressing the fusion protein EML4-ALK and 17 cyclozotinib-resistant ALK mutants. Its effect extends to cells expressing EGFR deletion, ROS1-L2026M, FLT3-F691L and FLT3-D835Y. In a mouse EML4-ALK xenograft model, brigatinib had a dose-dependent inhibition of tumor growth, tumor burden, and prolonged survival. The time course and exposure-response studies of brigatinib are unclear. At clinically achievable concentrations (≤500 nM), brigatinib inhibits the in vitro viability of cells expressing EML4-ALK and 17 mutant forms associated with resistance to ALK inhibitors, including crizotinib.
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