Development of anaplastic lymphoma kinase (ALK) inhibitors and molecular diagnosis in ALK rearrangement-positive lung cancer.

摘要: The fusion of echinoderm microtubule-associated protein-like 4 with anaplastic lymphoma kinase (ALK) was identified as a transforming gene for lung cancer in 2007. This genetic rearrangement accounts 2%–5% non-small-cell (NSCLC) cases, occurring predominantly younger individuals adenocarcinoma who are never- or light smokers. A small-molecule tyrosine-kinase inhibitor ALK, crizotinib, rapidly approved by the US Food and Drug Administration on basis its pronounced clinical activity patients ALK rearrangement-positive NSCLC. Next-generation inhibitors, such alectinib, LDK378, AP26113, also being developed ongoing trials. In addition, improvement validation methods detection NSCLC will be key to optimal use inhibitors. We here summarize recent progress development new inhibitors molecular diagnosis