[HTML][HTML] PF-06463922, an ALK/ROS1 inhibitor, overcomes resistance to first and second generation ALK inhibitors in preclinical models

HY Zou, L Friboulet, DP Kodack, LD Engstrom, Q Li… - Cancer cell, 2015 - cell.com
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 …

The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN

J Guan, ER Tucker, H Wan, D Chand… - Disease models & …, 2016 - journals.biologists.com
The first-in-class inhibitor of ALK, c-MET and ROS1, crizotinib (Xalkori), has shown
remarkable clinical efficacy in treatment of ALK-positive non-small cell lung cancer …

[HTML][HTML] ALK inhibition for non-small cell lung cancer: from discovery to therapy in record time

DE Gerber, JD Minna - Cancer cell, 2010 - cell.com
It was only 3 years ago that an acquired translocation of EML4 with ALK leading to the
expression of an EML4-ALK oncoprotein in non-small cell lung cancer (NSCLC) was …

Crizotinib‐resistant mutants of EML4‐ALK identified through an accelerated mutagenesis screen

S Zhang, F Wang, J Keats, X Zhu, Y Ning… - Chemical biology & …, 2011 - Wiley Online Library
Activating gene rearrangements of anaplastic lymphoma kinase (ALK) have been identified
as driver mutations in non‐small‐cell lung cancer, inflammatory myofibroblastic tumors, and …

A mouse model for EML4-ALK-positive lung cancer

M Soda, S Takada, K Takeuchi… - Proceedings of the …, 2008 - National Acad Sciences
EML4-ALK is a fusion-type protein tyrosine kinase that is generated in human non-small-cell
lung cancer (NSCLC) as a result of a recurrent chromosome inversion, inv (p21p23) …

TPX-0131, a potent CNS-penetrant, next-generation inhibitor of wild-type ALK and ALK-resistant mutations

BW Murray, D Zhai, W Deng, X Zhang, J Ung… - Molecular cancer …, 2021 - AACR
Since 2011, with the approval of crizotinib and subsequent approval of four additional
targeted therapies, anaplastic lymphoma kinase (ALK) inhibitors have become important …

Targeted therapies in non-small cell lung cancer: a focus on ALK/ROS1 tyrosine kinase inhibitors

A Sgambato, F Casaluce, P Maione… - Expert review of …, 2018 - Taylor & Francis
Introduction: Anaplastic lymphoma kinase (ALK) and ROS1 rearrangements define
important molecular subgroups of advanced non-small cell lung cancer (NSCLC). The …

EML4‐ALK biology and drug resistance in non‐small cell lung cancer: a new phase of discoveries

M Elshatlawy, J Sampson, K Clarke… - Molecular …, 2023 - Wiley Online Library
Anaplastic lymphoma kinase (ALK) can be driven to oncogenic activity by different types of
mutational events such as point‐mutations, for example F1174L in neuroblastoma, and …

ALK inhibitors in non-small cell lung cancer: the latest evidence and developments

I Sullivan, D Planchard - Therapeutic advances in medical …, 2016 - journals.sagepub.com
The treatment of patients with advanced non-small cell lung cancer (NSCLC) harbouring
chromosomal rearrangements of ALK (anaplastic lymphoma kinase) was revolutionized by …

The potent ALK inhibitor brigatinib (AP26113) overcomes mechanisms of resistance to first-and second-generation ALK inhibitors in preclinical models

S Zhang, R Anjum, R Squillace, S Nadworny… - Clinical Cancer …, 2016 - AACR
Purpose: Non–small cell lung cancers (NSCLCs) harboring ALK gene rearrangements
(ALK+) typically become resistant to the first-generation anaplastic lymphoma kinase (ALK) …