Crizotinib is a mesenchymal-epithelial transition/anaplastic largecell kinase (MET/ALK) multi-targeted receptor tyrosine kinase inhibitor and has been rapidly and successfully developed as an inhibitor in ALK-rearranged NSCLC (non-small cell lung cancer). Lung cancer is the major cause of cancer-related mortality, accounting for over one quarter of cancer deaths. Lung cancers are generally divided into two main categories: SCLC (small cell lung cancer) and NSCLC. NSCLC accounts for approximately 85% of all lung cancers. ALK gene rearrangements are identified and targeted resulting in promising response rates for NSCLC in early studies. Considering the significance of Crizotinib in the treatment of NSCLC, the synthesis, pharmacodynamics, pharmacokinetics, therapeutic trials and adverse events are briefly overviewed in order to make more scholars, medical workers and patients have a more clear and comprehensive recognition on Crizotinib.