CAS Insight

molecules of the month


oral EGFR mutant inhibitor

Ph. I/II candidate oncology

>25k compound library screening and opt

J. Med. Chem

Blueprint Medicines, Cambridge, MA

BLU-945 Chemical Structure oral EGFR mutant inhibitor - Blueprint Medicines, Cambridge, MA
5 mins read

Context. BLU-945 (Blueprint Medicines) is an oral EGFR mutant inhibitor being developed for treatment-resistant non-small-cell lung cancer (NSCLC). Although three generations of EGFR TKIs are available for EGFR-mutant NSCLC, drug resistance and associated disease relapse are still highly prevalent. The widely used third-generation agent osimertinib demonstrates activity against the highly prevalent T790M resistance mutation and the exon 19 deletion (ex19del) and L858R sensitizing mutations. However, it’s inactive against the C797S acquired resistance mutation. Consequently, no approved therapies exist for patients with disease progression following treatment with third-generation agents. Another key challenge in EGFR TKI development is selectivity against wildtype (WT) EGFR, with current agents being associated with dermatological and other toxicities due to their concomitant WT-targeting properties. BLU-945, which we…

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