naquotinib

Naquotinib is an orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor developed primarily for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations. It covalently binds to and inhibits mutant forms of EGFR—including the T790M resistance mutation—thereby blocking EGFR-mediated signaling pathways that drive tumor cell proliferation and survival. Naquotinib has demonstrated antineoplastic activity in preclinical models and clinical trials, showing efficacy against various clinically relevant EGFR mutations such as L858R, exon 19 deletions, T790M-containing mutants, and certain exon 20 insertions. In addition to its primary action on EGFR, naquotinib also inhibits Bruton's tyrosine kinase (BTK), suggesting potential utility in B-cell malignancies like activated B-cell-like diffuse large B-cell lymphoma (ABC DLBCL). The drug was developed by Astellas Pharma but development for NSCLC was discontinued after phase II/III trials.

Other names

naquotinib mesylate