期刊
CANCER CELL
卷 28, 期 1, 页码 70-81出版社
CELL PRESS
DOI: 10.1016/j.ccell.2015.05.010
关键词
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资金
- NIH [5R01CA164273-02]
- USA Department of Defense Breast Cancer Research Innovator Award [W81XWH-10-1-0016, P01-CA080124]
- Uniting Against Lung Cancer
- Grants-in-Aid for Scientific Research [25710015] Funding Source: KAKEN
We report the preclinical evaluation of PF-06463922, a potent and brain-penetrant ALK/ROS1 inhibitor. Compared with other clinically available ALK inhibitors, PF-06463922 displayed superior potency against all known clinically acquired ALK mutations, including the highly resistant G1202R mutant. Furthermore, PF-06463922 treatment led to regression of EML4-ALK-driven brain metastases, leading to prolonged mouse survival, in a superior manner. Finally, PF-06463922 demonstrated high selectivity and safety margins in a variety of preclinical studies. These results suggest that PF-06463922 will be highly effective for the treatment of patients with ALK-driven lung cancers, including those who relapsed on clinically available ALK inhibitors because of secondary ALK kinase domain mutations and/or brain metastases.
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