Expanding the portfolio of anti-ALK weapons.

摘要: The anaplastic lymphoma kinase (ALK) is a receptor tyrosine involved in the onset of several malignancies. In particular, ALK driving oncogenic lesion small but significant fraction non-small cell lung cancer (NSCLC) patients. ALK+ NSCLCs can be treated with dual ALK/MET inhibitor crizotinib, better outcome compared to standard chemotherapy. However, relapses frequently occur, due various mechanisms, limiting overall efficacy treatment. Point mutations within catalytic domain or gene amplification account for approximately 30-40% crizotinib-resistant cases, suggesting that diseases still relies on activity and more potent inhibitors could useful this setting. Ceritinib novel selective preclinical against mutants. A recent article New England Journal Medicine reports clinical evaluation ceritinib. Response rate progression-free survival (PFS) were comparable most importantly, patients successfully treated, similar crizotinib-naive study extends array available anti-ALK drugs. Based these data, ceritinib was approved by FDA April 2014.