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BLU-701 + osimertinib is an investigational oral combination therapy under clinical development for patients with EGFR-mutant non-small cell lung cancer (NSCLC), particularly for those harboring activating EGFR mutations (exon 19 deletion, L858R) and acquired resistance mutations, including C797X. BLU-701 is a fourth-generation, reversible, highly selective, wildtype-sparing, brain-penetrant EGFR tyrosine kinase inhibitor (TKI), designed to overcome known resistance to earlier EGFR TKIs. Osimertinib is a third-generation, irreversible EGFR TKI approved for EGFR-mutant NSCLC, targeting both activating and T790M resistance mutations. The combination is designed to enhance inhibition of heterogeneous tumor populations and prevent or overcome resistance, with activity including CNS metastases.
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