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The Potent ALK Inhibitor Brigatinib (AP26113) Overcomes Mechanisms of Resistance to First- and Second-Generation ALK Inhibitors in Preclinical Models.
Sen Zhang
1 ,
Rana Anjum
1 ,
Rachel Squillace
1 ,
Sara Nadworny
1 ,
Tianjun Zhou
1 ,
Jeff Keats
1 ,
Yaoyu Ning
1 ,
Scott D Wardwell
1 ,
David Miller
1 ,
Youngchul Song
1 ,
Lindsey Eichinger
1 ,
Lauren Moran
1 ,
Wei-Sheng Huang
1 ,
Shuangying Liu
1 ,
Dong Zou
1 ,
Yihan Wang
1 ,
Qurish Mohemmad
1 ,
Hyun Gyung Jang
1 ,
Emily Ye
1 ,
Narayana Narasimhan
1 ,
Frank Wang
1 ,
Juan Miret
1 ,
Xiaotian Zhu
1 ,
Tim Clackson
1 ,
David Dalgarno
1 ,
William C Shakespeare
1 ,
Victor M Rivera
2
Nov 15 2016
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Abstract
Non-small cell lung cancers (NSCLCs) harboring ALK gene rearrangements (ALK(+)) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) crizotinib through development of secondary resistance mutations in ALK or disease progression in the brain. Mutations that confer resistance to second-generation ALK TKIs ceritinib and alectinib have also been identified. Here, we report the structure and first comprehensive preclinical evaluation of the next-generation ALK TKI brigatinib.