BLU-451

BLU-451 is an investigational, orally administered small molecule inhibitor designed to target cancers with specific genetic alterations in the epidermal growth factor receptor (EGFR) gene, particularly EGFR exon 20 insertion mutations and other atypical EGFR mutations such as G719X and L861Q. It is a central nervous system (CNS)-penetrant, wild-type EGFR-sparing covalent inhibitor that selectively inhibits mutant forms of EGFR while sparing wild-type receptors. The drug is being developed primarily for advanced non-small cell lung cancer (NSCLC), including cases with brain metastases and those that have progressed after prior therapies. BLU-451 has demonstrated preclinical potency against various EGFR exon 20 insertion variants and shows early clinical evidence of tumor reduction—including CNS activity—and circulating tumor DNA response in heavily pretreated patients. The most common adverse events reported are mild to moderate gastrointestinal or skin-related effects[1][2][3][5][9].