• Expert Opin Emerg Drugs · Sep 2020

    Review

    Emerging MET tyrosine kinase inhibitors for the treatment of non-small cell lung cancer.

    • Toshio Fujino, Kenichi Suda, and Tetsuya Mitsudomi.
    • Division of Thoracic Surgery, Department of Surgery, Kindai University Faculty of Medicine , Osaka-Sayama, Japan.
    • Expert Opin Emerg Drugs. 2020 Sep 1; 25 (3): 229-249.

    AbstractIntroduction MET aberrations, including MET exon 14 skipping mutation and amplification, are present in ~5% of non-small cell lung cancer (NSCLC) cases, and these levels are comparable to the frequency of ALK fusion. MET amplification also occurs as an acquired resistance mechanism in EGFR-mutated NSCLC after EGFR tyrosine kinase inhibitors (TKI) treatment failure. Therefore, the development of therapies for activated MET is urgently needed. Areas covered This review summarizes (1) the mechanisms and frequencies of MET aberrations in NSCLC, (2) the efficacies and toxicities of MET-TKIs under clinical development and (3) the mechanisms of inherent and acquired resistance to MET-TKIs. Expert opinion Type Ia, Ib and II MET-TKIs are currently under clinical development, and phase I/II studies have shown the potent activities of tepotinib, capmatinib and savolitinib; in fact, tepotinib and capmatinib were approved for use by health authorities. However, inherent and acquired resistance through on- and off-target mechanisms has been detected, and strategies to overcome this resistance are being developed.

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