tigozertinib

Tigozertinib (BLU-945) is an investigational, fourth-generation, oral small-molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor designed to selectively inhibit activating and resistance EGFR mutations, including C797S, that emerge after treatment with third-generation EGFR TKIs in non-small cell lung cancer (NSCLC).[10][14] Developed by Blueprint Medicines, it was evaluated primarily in patients with EGFR-mutant NSCLC who had progressed on prior EGFR-targeted therapies, but clinical development was discontinued in early 2024.[10][14] The molecule was optimized for potent, mutant-selective EGFR inhibition with reduced activity on wild-type EGFR to improve tolerability compared with earlier-generation inhibitors.[10][14]