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Ceritinib is a second-generation, orally active small molecule tyrosine kinase inhibitor developed for the treatment of anaplastic lymphoma kinase (ALK)-positive metastatic non-small cell lung cancer (NSCLC). It selectively and potently inhibits ALK by blocking its autophosphorylation and downstream signaling pathways, thereby preventing proliferation of ALK-dependent cancer cells. Ceritinib also inhibits other kinases to a lesser extent, including insulin-like growth factor 1 receptor (IGF-1R), insulin receptor, and ROS1. It is particularly effective in patients who have developed resistance to crizotinib or as a first-line therapy for ALK-positive NSCLC. Ceritinib was developed by Novartis and received FDA approval in April 2014.
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