Entrectinib is a multiple kinase inhibitor (NTRK 1/2/3, ROS1, or ALK) that exhibits antitumor activity and is known for central nervous system efficacy. Most of the side effects were Grade 1-2 and manageable. Ignyta, an American biotechnology company, announced updated results of three trials at the 18th World Conference on Lung Cancer (WCLC). The data showed 32 patients with locally advanced or metastatic non-small cell lung cancer (NSCLC) that harbored ROS1 fusions were treated with entrectinib and demonstrated an objective response rate (ORR) of 69% (by Blinded Independent Central Review, 95% CI: 50.0, 83.9). For median follow-up of 12.9 months, entrectinib showed durable response in these patients, with a median duration of response (mDOR) of 28.6 months. In the subpopulation analysis, the ORR of patients with CNS metastases was 83.3%. These results revealed that entrectinib has the potential to provide clinical benefit for patients with ROS1 fusion and CNS metastases NSCLC.