PURPOSE: Published data on the clinical efficacy, safety, dosage and 
administration, and costs of the anaplastic lymphoma kinase (ALK) inhibitors 
crizotinib and ceritinib in the treatment of non-small-cell lung cancer (NSCLC) 
are reviewed and compared.
SUMMARY: The ALK protein functions as a transmembrane receptor tyrosine kinase; 
rearrangements of the ALK gene are associated with the development of NSCLC with 
adenocarcinoma histology. Crizotinib is an oral tyrosine kinase inhibitor 
approved in 2011 as a first-line therapy for patients with metastatic ALK 
mutation-driven NSCLC. Significantly improved response rates and 
progression-free survival (PFS) have been reported with the use of crizotinib 
therapy versus standard chemotherapy, but mutations conferring resistance to 
treatment develop in most cases. The second-generation ALK inhibitor ceritinib 
was approved in 2014 for the treatment of ALK-mutated NSCLC in patients who are 
intolerant or develop resistance to crizotinib. In a clinical trial of ceritinib 
involving 130 patients with ALK-positive NSCLC, the majority of whom had 
experienced disease progression during crizotinib use, patients receiving at 
least 400 mg of ceritinib daily had an overall response rate of 56% and median 
PFS of seven months. Adverse effects commonly reported with the use of either 
drug include visual disturbances, gastrointestinal disorders (e.g., diarrhea), 
and liver enzyme abnormalities.
CONCLUSION: The tyrosine kinase inhibitors crizotinib and ceritinib provide an 
effective treatment approach for patients with ALK-mutated NSCLC. Efficacy data 
for both crizotinib and ceritinib indicate improved response rates and PFS with 
the use of either drug as an alternative to standard chemotherapy.