SAF-189s, a potent new-generation ROS1 inhibitor, is active against crizotinib-resistant ROS1 mutant-driven tumors

[1]  A. Hui,et al.  SAF-189s in previously treated patients with advanced ALK-rearranged non-small cell lung cancer (NSCLC): Results from the dose-finding portion in a single-arm, first-in-human phase I/II study. , 2020 .

[2]  Kengo Watanabe,et al.  The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models , 2019, Nature Communications.

[3]  A. Drilon,et al.  Repotrectinib (TPX-0005) Is a Next-Generation ROS1/TRK/ALK Inhibitor That Potently Inhibits ROS1/TRK/ALK Solvent- Front Mutations. , 2018, Cancer discovery.

[4]  A. Shaw,et al.  Recent Advances in Targeting ROS1 in Lung Cancer , 2017, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.

[5]  T. Bivona,et al.  Understanding and targeting resistance mechanisms in NSCLC , 2017, Nature Reviews Cancer.

[6]  A. Drilon,et al.  Fusions in solid tumours: diagnostic strategies, targeted therapy, and acquired resistance , 2017, Nature Reviews Clinical Oncology.

[7]  C. Luo,et al.  Discovery of 3-(5'-Substituted)-Benzimidazole-5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazoles as Potent Fibroblast Growth Factor Receptor Inhibitors: Design, Synthesis, and Biological Evaluation. , 2016, Journal of medicinal chemistry.

[8]  A. Uguen,et al.  ROS1 fusions in cancer: a review. , 2016, Future oncology.

[9]  M. McTigue,et al.  PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations , 2015, Proceedings of the National Academy of Sciences.

[10]  Jeffrey W. Clark,et al.  Crizotinib in ROS1-rearranged non-small-cell lung cancer. , 2014, The New England journal of medicine.

[11]  Mari Mino-Kenudson,et al.  Acquired resistance to crizotinib from a mutation in CD74-ROS1. , 2013, The New England journal of medicine.

[12]  F. Cappuzzo,et al.  Identifying and Targeting ROS1 Gene Fusions in Non–Small Cell Lung Cancer , 2012, Clinical Cancer Research.

[13]  S. Ou,et al.  ROS1 as a ‘druggable’ receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway , 2012, Expert review of anticancer therapy.

[14]  Young Lim Choi,et al.  EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors. , 2010, The New England journal of medicine.

[15]  Sungjoon Kim,et al.  Ba/F3 cells and their use in kinase drug discovery , 2007, Current opinion in oncology.

[16]  Andrew I Su,et al.  An efficient rapid system for profiling the cellular activities of molecular libraries. , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[17]  M. Meyerson,et al.  EGFR mutation and resistance of non-small-cell lung cancer to gefitinib. , 2005, The New England journal of medicine.

[18]  A. Tsao,et al.  ROS1 Rearrangements Define a Unique Molecular Class of Lung Cancers , 2012 .