X-396 Capsule in Advanced NSCLC Patients With ROS1 Gene Rearrangement

Inclusion Criteria: * Female or male, 18 years of age or older * Histologically or cytologically proven diagnosis of NSCLC that is locally advanced or metastatic * Positive for translocation or inversion events involving the ROS1 gene * Tyrosine kinase inhibitor (TKI) treatment-naive or have previously received no more than one systemic treatment regimen(s) such as chemotherapy (After a 3-week washout period) * Eastern Cooperative Oncology Group (ECOG) performance status 0 to 1 * Predicted survival ≥ 3 months * Drug related toxicities were relieved to grade 1, except for hair loss (based on NCI CTCAE v4.03) * Adequate organ function * At least 1 measurable tumor lesion as per RECIST v1.1 * Asymptomatic central nervous system (CNS) metastases do not require the use of steroids or anticonvulsants. * Signed and dated informed consent * Willingness and ability to comply with scheduled visits, treatment plans, laboratory tests, and other study procedures * Agree to use effective contraception during the study period and for at least 90 days after completion of the study treatment Exclusion Criteria: * Current treatment on another systemic anti-cancer therapy * Prior therapy specifically directed against ROS1 fusion genes (except for the exploratory arm that will enroll patients pretreated with crizotinib) * Evidence of active malignancy within last 3 years * Previous therapeutic clinical trial must have completed at least 4 week prior to initiation of study drug * Prior surgery or immunotherapy must have completed at least 4 weeks, and radiation must have been completed at least 2 weeks prior to initiation of study drug * Known interstitial fibrosis or interstitial lung disease * Presence of active gastrointestinal disease or other condition that will interfere significantly with the absorption, distribution, metabolism, or excretion of study medication * Clinically significant cardiovascular disease * Patients with a known allergy or delayed hypersensitivity reaction to study drug or its excipient * Pregnant or breast feeding * Use of drugs or foods that are known potent CYP3A4 inhibitors or inducers * Inability or unwillingness to comply with study and/or follow-up procedures outlined in the protocol * Other serious illness or medical condition potentially interfering with the study