silevertinib

Silevertinib is a potent, orally available, fourth-generation, brain-penetrant, irreversible, adenosine triphosphate (ATP)-competitive small molecule inhibitor targeting a broad spectrum of epidermal growth factor receptor (EGFR) variants. It acts as a "MasterKey" inhibitor, active against classical and non-classical (including uncommon and resistance) EGFR mutations, such as T790M and C797S mutations in non-small cell lung cancer (NSCLC), as well as allosteric EGFR mutant variants found in glioblastoma (e.g., EGFRvIII). Silevertinib is designed to overcome resistance to earlier generation EGFR inhibitors (e.g., osimertinib) and can cross the blood-brain barrier, enabling activity against central nervous system metastases. It is developed primarily for the treatment of NSCLC patients with non-classical EGFR mutations, but is also under investigation for glioblastoma. Developed by Black Diamond Therapeutics, silevertinib is currently in Phase 2 clinical trials for NSCLC and Phase 1/2 studies for glioblastoma[1][3][4][5][7][9][10].

Other names

silevertinib