Rearrangements in ALK gene and EML4 gene were first described in 2007. This 
genomic aberration is found in about 2%-8% of non-small-cell lung cancer (NSCLC) 
patients. Crizotinib was the first ALK tyrosine kinase inhibitor licensed for 
the treatment of metastatic ALK-positive NSCLC based on a randomized Phase III 
trial. Despite the initial treatment response of crizotinib, disease progression 
inevitably develops after approximately 10 months of therapy. Different 
resistance mechanisms have recently been described. One relevant mechanism of 
resistance is the development of mutations in ALK. Novel ALK tyrosine kinase 
inhibitors have been developed to overcome these mutations. Ceritinib is an oral 
second-generation ALK inhibitor showing clinical activity not only in 
crizotinib-resistant ALK-positive NSCLC but also in treatment-naïve ALK-positive 
disease. In this paper, preclinical and clinical data of ceritinib are reviewed, 
and its role in the clinical setting is put into perspective.