BDTX-507

BDTX-507 is a CNS-penetrant, irreversible small molecule inhibitor of the Epidermal Growth Factor Receptor (EGFR), specifically designed to target allosteric oncogenic EGFR mutations commonly found in glioblastoma (GBM). Developed by Black Diamond Therapeutics using their Mutation-Allostery-Pharmacology (MAP) platform, it belongs to a series of compounds (including BDTX-1535 and BDTX-700) that aim to overcome the limitations of earlier EGFR inhibitors, such as poor brain penetration and narrow mutational coverage. BDTX-507 demonstrates potent activity against a broad spectrum of GBM-relevant EGFR mutations, including those in the extracellular domain, while maintaining selectivity over wild-type EGFR. In preclinical studies, it has shown robust tumor regression and improved survival in intracranial patient-derived xenograft models of glioblastoma.