PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

doi:10.1016/j.ccell.2015.05.010

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PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Cancer cell - 13 Jul 2015

Zou Helen Y, Friboulet Luc, Kodack David P, Engstrom Lars D, Li Qiuhua, West Melissa, Tang Ruth W, Wang Hui, Tsaparikos Konstantinos, Wang Jinwei, Timofeevski Sergei, Katayama Ryohei, Dinh Dac M, Lam Hieu, Lam Justine L, Yamazaki Shinji, Hu Wenyue, Patel Bhushankumar, Bezwada Divya, Frias Rosa L, Lifshits Eugene, Mahmood Sidra, Gainor Justin F, Affolter Timothy, Lappin Patrick B, Gukasyan Hovhannes, Lee Nathan, Deng Shibing, Jain Rakesh K, Johnson Ted W, Shaw Alice T, Fantin Valeria R, Smeal Tod

Abstract excerpt

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...

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Identifiers

PMID: 26144315
DOI: 10.1016/j.ccell.2015.05.010
PMCID: PMC4504786

Genes

ALK
ROS1
EML4

Variants

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-08.1.

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