BDTX-700

BDTX-700 is a small molecule, CNS-penetrant, irreversible inhibitor of oncogenic Epidermal Growth Factor Receptor (EGFR) mutations, specifically designed to target allosteric mutations in the extracellular domain (ECD) commonly found in glioblastoma (GBM). Developed by Black Diamond Therapeutics using their Mutation-Allostery-Pharmacology (MAP) platform, BDTX-700 aims to address the limitations of earlier EGFR inhibitors, such as poor brain penetration and narrow mutational coverage. It demonstrates high potency against a broad spectrum of GBM-relevant EGFR mutants while maintaining selectivity over wild-type EGFR. Its optimized pharmacokinetic profile allows for significant blood-brain barrier penetration, which is essential for eliciting robust target engagement in brain tumors.