The ALK/ROS1 inhibitor PF-06463922 overcomes primary resistance to crizotinib in ALK-driven neuroblastoma
作者： Nicole R. Infarinato , Jin H. Park , Kateryna Krytska , Hannah T. Ryles , Renata Sano
DOI: 10.1158/2159-8290.CD-15-1056
关键词:
摘要: Neuroblastomas (NBs) harboring activating point mutations in Anaplastic Lymphoma Kinase (ALK) are differentially sensitive to the ALK inhibitor crizotinib, with certain conferring intrinsic crizotinib resistance. To overcome this clinical obstacle, our goal was identify inhibitors improved potency that can target intractable variants such as F1174L. We find PF-06463922 has high across variants, and inhibits more effectively than vitro. Most importantly, induces complete tumor regression both crizotinib-resistant xenograft mouse models of NB, well PDXs F1174L or F1245C mutations. These studies demonstrate potential resistance, exerts unprecedented activity a single targeted agent against ALK-mutated tumors, while also inducing responses R1275Q model. Taken together, these results provide rationale move into trials for treatment patients NB.
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