Description
Crizotinib is an inhibitor of anaplastic lymphoma kinase (ALK), c-ros oncogene 1 (ROS1), and c-MET, binding competitively to the ATP-binding pocket of kinases. Crizotinib exhibits anticancer chemotherapeutic benefit in the treatment of non-small cell lung cancer (NSCLC) and is currently in clinical trials as a potential treatment for neuroblastoma and other advanced solid tumors. In cellular models, this compound upregulates expression of pro-apoptotic BIM and downregulates expression of anti-apoptotic survivin to induce apoptosis and inhibit cell proliferation.
References
Timm A, Kolesar JM. Crizotinib for the treatment of non-small-cell lung cancer. Am J Health Syst Pharm. 2013 Jun 1;70(11):943-7. PMID: 23686600.
Okamoto W, Okamoto I, Arao T, et al. Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification. Mol Cancer Ther. 2012 Jul;11(7):1557-64. PMID: 22729845.
Tanizaki J, Okamoto I, Okamoto K, et al. MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations. J Thorac Oncol. 2011 Oct;6(10):1624-31. PMID: 21716144.
