BLU-945 + osimertinib

BLU-945 + osimertinib is an investigational, fully oral combination therapy for the treatment of non-small cell lung cancer (NSCLC) with activating and resistance mutations in the epidermal growth factor receptor (EGFR). BLU-945 is a next-generation, reversible EGFR tyrosine kinase inhibitor (TKI) designed to selectively target both activating EGFR mutations and key resistance mutations such as T790M and C797S while sparing wild-type EGFR. Osimertinib is a third-generation irreversible EGFR TKI approved for use in NSCLC with specific EGFR mutations. The combination aims to overcome acquired resistance to prior EGFR TKIs, particularly post-osimertinib progression. Preclinical and early clinical data demonstrate that this combination results in dose-dependent inhibition of mutant EGFR alleles, robust ctDNA reduction, tumor shrinkage—including partial responses—in heavily pretreated patients with complex genomic profiles. The safety profile shows most adverse events are mild or moderate; dose escalation studies are ongoing to determine optimal dosing[1][2][3][5].

Brand names

Tagrisso