LDK378 is an orally available ALK inhibitor. LDK378 is an approximately 20-fold more potent ALK inhibitor than crizotinib, it is more selective for ALK and does not inhibit MET. The inhibition leads to disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-overexpressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development. ALK dysregulation and gene rearrangements are associated with a series of tumors.
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