Description: Ceritinib (formerly known as LDK378; trade name: Zykadia) is novel, potent and selective inhibitor against ALK (anaplastic lymphoma kinase positive) with potential anticancer activity. It inhibits ALK with IC50 of 0.2 nM in cell-free assays, and shows 40- and 35-fold selectivity for ALK over IGF-1R and InsR, respectively. Ceritinib was approved by FDA in April 2014 for the treatment non-small cell lung cancer (NSCLC). In Phase I trials, Ceritinib showed a marked clinical response in 78 patients with anaplastic ALK+ metastatic non-small cell lung cancer who had progressed during or after crizotinib therapy or had not been previously treated with crizotinib.
References: J Med Chem. 2013 Jul 25;56(14):5675-90.
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