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Title: PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

Journal Article · · Proceedings of the National Academy of Sciences of the United States of America
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Research Organization:
Argonne National Laboratory (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Organization:
INDUSTRY
Grant/Contract Number:
AC02-06CH11357
OSTI ID:
1182329
Journal Information:
Proceedings of the National Academy of Sciences of the United States of America, Vol. 112, Issue 11; ISSN 0027-8424
Publisher:
National Academy of Sciences, Washington, DC (United States)Copyright Statement
Country of Publication:
United States
Language:
ENGLISH
Citation Metrics:
Cited by: 195 works
Citation information provided by
Web of Science

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An Orally Available Small-Molecule Inhibitor of c-Met, PF-2341066, Exhibits Cytoreductive Antitumor Efficacy through Antiproliferative and Antiangiogenic Mechanisms journal April 2007
Translational Pharmacokinetic-Pharmacodynamic Modeling for an Orally Available Novel Inhibitor of Anaplastic Lymphoma Kinase and c-Ros Oncogene 1 journal July 2014
Survey of Tyrosine Kinase Signaling Reveals ROS Kinase Fusions in Human Cholangiocarcinoma journal January 2011
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Next-Generation Sequencing Reveals a Novel NSCLC ALK F1174V Mutation and Confirms ALK G1202R Mutation Confers High-Level Resistance to Alectinib (CH5424802/RO5424802) in ALK-Rearranged NSCLC Patients Who Progressed on Crizotinib journal April 2014
A Cre/LoxP conditional luciferase reporter transgenic mouse for bioluminescence monitoring of tumorigenesis journal October 2009
Acquired Resistance to Crizotinib from a Mutation in CD74 – ROS1 journal June 2013
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Foretinib is a potent inhibitor of oncogenic ROS1 fusion proteins journal November 2013
Insight into Crizotinib Resistance Mechanisms Caused by Three Mutations in ALK Tyrosine Kinase using Free Energy Calculation Approaches journal August 2013
Acquired resistance to tyrosine kinase inhibitors during cancer therapy journal February 2008
Analysis of Receptor Tyrosine Kinase ROS1-Positive Tumors in Non-Small Cell Lung Cancer: Identification of a FIG-ROS1 Fusion journal June 2012
Classification of human lung carcinomas by mRNA expression profiling reveals distinct adenocarcinoma subclasses journal November 2001
Clinical activity of crizotinib in advanced non-small cell lung cancer (NSCLC) harboring ROS1 gene rearrangement. journal May 2012
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Kinase fusions are frequent in Spitz tumours and spitzoid melanomas journal January 2014
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Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion–Positive Cancer journal October 2014
Chaperones as thermodynamic sensors of drug-target interactions reveal kinase inhibitor specificities in living cells journal June 2013
Differential Protein Stability and ALK Inhibitor Sensitivity of EML4-ALK Fusion Variants journal August 2012
ROS1 as a ‘druggable’ receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway journal April 2012
ROS Fusion Tyrosine Kinase Activates a SH2 Domain–Containing Phosphatase-2/Phosphatidylinositol 3-Kinase/Mammalian Target of Rapamycin Signaling Axis to Form Glioblastoma in Mice journal August 2006
Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK) journal September 2011
Discovery of (10 R )-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro- 2H -8,4-(metheno)pyrazolo[4,3- h ][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations journal December 2013
Chromosome 3 Anomalies Investigated by Genome Wide SNP Analysis of Benign, Low Malignant Potential and Low Grade Ovarian Serous Tumours journal December 2011
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Molecular Changes Associated with Acquired Resistance to Crizotinib in ROS1-Rearranged Non-Small Cell Lung Cancer journal February 2015
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Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib journal February 2014
Breakpoint Analysis of Transcriptional and Genomic Profiles Uncovers Novel Gene Fusions Spanning Multiple Human Cancer Types journal April 2013
Crizotinib in ROS1-Rearranged Non–Small-Cell Lung Cancer journal February 2015
The Oncogenic Lung Cancer Fusion Kinase CD74-ROS Activates a Novel Invasiveness Pathway through E-Syt1 Phosphorylation journal July 2012

Cited By (31)

Targeted therapies in non-small cell lung cancer: a focus on ALK/ROS1 tyrosine kinase inhibitors journal December 2017
Oncogenic kinase fusions: an evolving arena with innovative clinical opportunities journal March 2016
The role of HGF/c-MET signaling pathway in lymphoma journal December 2016
Recent Advances in Targetable Therapeutics in Metastatic Non-Squamous NSCLC journal May 2016
Management of advanced non-small cell lung cancers with known mutations or rearrangements: latest evidence and treatment approaches journal November 2015
Brain Penetration of the ROS1/ALK Inhibitor Lorlatinib Confirmed by PET journal January 2017
Targeted therapies and immunotherapy in non-small-cell lung cancer journal June 2016
Consensus Recommendations for Management and Counseling of Adverse Events Associated With Lorlatinib: A Guide for Healthcare Practitioners journal May 2020
From crizotinib to lorlatinib: continuous improvement in precision treatment of ALK-positive non-small cell lung cancer journal January 2019
ALK and ROS1 as targeted therapy paradigms and clinical implications to overcome crizotinib resistance journal January 2016
Pharmacophore-based designing of putative ROS-1 targeting agents for NSCLC journal January 2020
Targeted Therapies in Non-Small Cell Lung Cancer—Beyond EGFR and ALK journal May 2015
Drug resistance mechanisms in Japanese anaplastic lymphoma kinase‐positive non–small cell lung cancer and the clinical responses based on the resistant mechanisms journal February 2020
Treatment of ALK -rearranged non-small cell lung cancer: A review of the landscape and approach to emerging patterns of treatment resistance in the Australian context journal August 2017
TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity journal July 2017
Lorlatinib in ALK- and ROS1-positive NSCLC: the future has a start journal April 2018
Anaplastic lymphoma kinase: Role in cancer and therapy perspective journal November 2015
Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR journal July 2017
Combined effect of cabozantinib and gefitinib in crizotinib-resistant lung tumors harboring ROS1 fusions journal September 2018
Tumor Resistance against ALK Targeted Therapy-Where It Comes From and Where It Goes journal February 2018
Advances in Targeted Therapy and Immunotherapy for Non-small Cell Lung Cancer Based on Accurate Molecular Typing journal March 2019
The new-generation selective ROS1/NTRK inhibitor DS-6051b overcomes crizotinib resistant ROS1-G2032R mutation in preclinical models journal August 2019
Resistance mechanisms and potent-targeted therapies of ROS1-positive lung cancer journal June 2019
Synthesis and preliminary PET imaging of 11C and 18F isotopologues of the ROS1/ALK inhibitor lorlatinib journal June 2017
Current Landscape of Targeted Therapy in Lung Cancer journal September 2017
Detection of ROS1 rearrangement in non-small cell lung cancer: current and future perspectives journal July 2017
Targeting HGF/c-MET induces cell cycle arrest, DNA damage, and apoptosis for primary effusion lymphoma journal December 2015
Can molecular profiling enhance radiotherapy? Impact of personalized targeted gold nanoparticles on radiosensitivity and imaging of adenoid cystic carcinoma journal January 2017
Conformation of the Macrocyclic Drug Lorlatinib in Polar and Nonpolar Environments: A MD Simulation and NMR Study journal December 2019
Latest perspectives of orally bioavailable 2,4-diarylaminopyrimidine analogues (DAAPalogues) as anaplastic lymphoma kinase inhibitors: discovery and clinical developments journal January 2018
Fusions in solid tumours: diagnostic strategies, targeted therapy, and acquired resistance journal August 2017

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