Abstract
Crizotinib has been established as the standard first-line treatment for patients with ALK-rearranged non-small-cell lung cancer. However, despite its superiority to chemotherapy, resistance occurs within approximately 12 months. New ALK-inhibitors are needed to overcome the resistance to crizotinib and to increase drug penetration to CNS. X-396 (ensartinib) is a novel, potent ALK tyrosine kinase inhibitor (TKI). Its phase I/II study showed X-396 is well-tolerated with favorable anti-tumor activities in both ALK TKI-naïve and crizotinib-resistant NSCLC patients, as well as patients with CNS metastases.
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