The next tier of EGFR resistance mutations in lung cancer

Tumor Analyses Reveal Squamous Transformation and Off-Target Alterations As Early Resistance Mechanisms to First-line Osimertinib in EGFR-Mutant Lung Cancer

(2020) Adam J Schoenfeld et al.   CLINICAL CANCER RESEARCH

Resolving Resistance to Osimertinib Therapy using Afatinib in a NSCLC Patient with an EGFR L718Q Mutation

(2020) Xue Yang et al.   Clinical Lung Cancer

Emergence of EGFR G724S After Progression on Osimertinib Responded to Afatinib Monotherapy

(2020) Wenfeng Fang et al.   Journal of Thoracic Oncology

Insight into the Therapeutic Selectivity of the Irreversible EGFR Tyrosine Kinase Inhibitor Osimertinib through Enzyme Kinetic Studies

(2020) Xiang Zhai et al.   BIOCHEMISTRY

Mutational spectrum of acquired resistance to reversible versus irreversible EGFR tyrosine kinase inhibitors

(2020) Svenja Wagener-Ryczek et al.   BMC CANCER

Genomic landscape of acquired resistance to third‐generation EGFR tyrosine kinase inhibitors in EGFR T790M‐mutant non–small cell lung cancer

(2020) Jiyun Lee et al.   CANCER

Drug Sensitivity and Allele Specificity of First-Line Osimertinib Resistance EGFR Mutations

(2020) Jacqueline H. Starrett et al.   CANCER RESEARCH

Detection of EGFR-Activating and T790M Mutations Using Liquid Biopsy in Patients With EGFR-Mutated Non–Small-Cell Lung Cancer Whose Disease Has Progressed During Treatment With First- and Second-Generation Tyrosine Kinase Inhibitors: A Multicenter Real-Life Retrospective Study

(2020) Roberta Minari et al.   Clinical Lung Cancer

Mutation Profile of Resected EGFR‐Mutated Lung Adenocarcinoma by Next‐Generation Sequencing

(2019) Ze‐Rui Zhao et al.   ONCOLOGIST

Case Report: Lung Adenocarcinoma Harboring EGFR-19del/C797S/T790M Triple Mutations Responds to Brigatinib and Anti-EGFR Antibody Combination Therapy

(2019) Xiaofei Wang et al.   Journal of Thoracic Oncology

On-target resistance to the mutant-selective EGFR inhibitor osimertinib can develop in an allele specific manner dependent on the original EGFR activating mutation

(2019) Benjamin P Brown et al.   CLINICAL CANCER RESEARCH

Single and dual targeting of mutant EGFR with an allosteric inhibitor

(2019) Ciric To et al.   Cancer Discovery

EGFR L718Q mutation occurs without T790M mutation in a lung adenocarcinoma patient with acquired resistance to osimertinib

(2019) Lei Ma et al.   Annals of Translational Medicine

Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer

(2019) Alessandro Leonetti et al.   BRITISH JOURNAL OF CANCER

Phase II Study Evaluating the Mechanisms of Resistance on Tumor Tissue and Liquid Biopsy in Patients With EGFR-mutated Non-pretreated Advanced Lung Cancer Receiving Osimertinib Until and Beyond Radiologic Progression: The MELROSE Trial

(2019) Jaafar Bennouna et al.   Clinical Lung Cancer

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

(2019) Harald Engelhardt et al.   JOURNAL OF MEDICINAL CHEMISTRY

Resistance mechanisms to osimertinib in EGFR-mutated advanced non-small-cell lung cancer: A multicentric retrospective French study

(2019) Camille Mehlman et al.   LUNG CANCER

Amplicon-based next-generation sequencing of plasma cell-free DNA for detection of driver and resistance mutations in advanced non-small cell lung cancer

(2018) N Guibert et al.   ANNALS OF ONCOLOGY

Investigating Novel Resistance Mechanisms to Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib in Non–Small Cell Lung Cancer Patients

(2018) Zhe Yang et al.   CLINICAL CANCER RESEARCH

Osimertinib As First-Line Treatment of EGFR Mutation–Positive Advanced Non–Small-Cell Lung Cancer

(2018) Suresh S. Ramalingam et al.   JOURNAL OF CLINICAL ONCOLOGY

EGFR L792H and G796R: Two Novel Mutations Mediating Resistance to the Third-Generation EGFR Tyrosine Kinase Inhibitor Osimertinib

(2018) Qi Zhang et al.   Journal of Thoracic Oncology

Acquired EGFR L718V mutation mediates resistance to osimertinib in non-small cell lung cancer but retains sensitivity to afatinib

(2018) Yutao Liu et al.   LUNG CANCER

Osimertinib in Untreated EGFR-Mutated Advanced Non–Small-Cell Lung Cancer

(2018) Jean-Charles Soria et al.   NEW ENGLAND JOURNAL OF MEDICINE

L718Q mutant EGFR escapes covalent inhibition by stabilizing a non-reactive conformation of the lung cancer drug osimertinib

(2018) D. Callegari et al.   Chemical Science

Landscape of acquired resistance to osimertinib in EGFR-mutant NSCLC and clinical validation of combined EGFR and RET inhibition with osimertinib and BLU-667 for acquired RET fusion.

(2018) Zofia Piotrowska et al.   Cancer Discovery

Assessment of Resistance Mechanisms and Clinical Implications in Patients With EGFR T790M–Positive Lung Cancer and Acquired Resistance to Osimertinib

(2018) Geoffrey R. Oxnard et al.   JAMA Oncology

Effects of secondary EGFR mutations on resistance against upfront osimertinib in cells with EGFR-activating mutations in vitro

(2018) Masaya Nishino et al.   LUNG CANCER

Newly emergent acquired EGFR exon 18 G724S mutation after resistance of a T790M specific EGFR inhibitor osimertinib in non-small-cell lung cancer: a case report

(2018) Yan Zhang et al.   OncoTargets and Therapy

Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

(2018) Jana Fassunke et al.   Nature Communications

Discovery of N -(5-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-4-methoxy-2-(4-methyl-1,4-diazepan-1-yl)phenyl)acrylamide (CHMFL-ALK/EGFR-050) as a potent ALK/EGFR dual kinase inhibitor capable of overcoming a variety of ALK/EGFR associated drug resistant mutants in NSCLC

(2017) Yongfei Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel Mutations on EGFR Leu792 Potentially Correlate to Acquired Resistance to Osimertinib in Advanced NSCLC

(2017) Kai Chen et al.   Journal of Thoracic Oncology

Subclonal Therapy by Two EGFR TKIs Guided by Sequential Plasma Cell-free DNA in EGFR -Mutated Lung Cancer

(2017) Nir Peled et al.   Journal of Thoracic Oncology

Acquired BRAF V600E Mutation as Resistant Mechanism after Treatment with Osimertinib

(2017) Chao-Chi Ho et al.   Journal of Thoracic Oncology

Combination Osimertinib and Gefitinib in C797S and T790M EGFR- Mutated Non–Small Cell Lung Cancer

(2017) Surein Arulananda et al.   Journal of Thoracic Oncology

Emergence of EGFR G724S mutation in EGFR-mutant lung adenocarcinoma post progression on osimertinib

(2017) A. Oztan et al.   LUNG CANCER

Emergence of novel and dominant acquired EGFR solvent-front mutations at Gly796 (G796S/R) together with C797S/R and L792F/H mutations in one EGFR (L858R/T790M) NSCLC patient who progressed on osimertinib

(2017) Sai-Hong Ignatius Ou et al.   LUNG CANCER

Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer

(2017) Ken Uchibori et al.   Nature Communications

EGFR G796D mutation mediates resistance to osimertinib

(2017) Di Zheng et al.   Oncotarget

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

(2016) Scott A. Foster et al.   CANCER CELL

Sensitivities to various epidermal growth factor receptor-tyrosine kinase inhibitors of uncommonepidermal growth factor receptormutations L861Q and S768I: What is the optimal epidermal growth factor receptor-tyrosine kinase inhibitor?

(2016) Eri Banno et al.   CANCER SCIENCE

Heterogeneous Mechanisms of Primary and Acquired Resistance to Third-Generation EGFR Inhibitors

(2016) S. Ortiz-Cuaran et al.   CLINICAL CANCER RESEARCH

L718Q Mutation as New Mechanism of Acquired Resistance to AZD9291 in EGFR -Mutated NSCLC

(2016) Melissa Bersanelli et al.   Journal of Thoracic Oncology

S768I Mutation in EGFR in Patients with Lung Cancer

(2016) Konstantinos Leventakos et al.   Journal of Thoracic Oncology

Characterization of EGFR T790M, L792F, and C797S Mutations as Mechanisms of Acquired Resistance to Afatinib in Lung Cancer

(2016) Yoshihisa Kobayashi et al.   MOLECULAR CANCER THERAPEUTICS

Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors

(2016) Yong Jia et al.   NATURE

The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies

(2015) M. J. Niederst et al.   CLINICAL CANCER RESEARCH

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors

(2015) D. Ercan et al.   CLINICAL CANCER RESEARCH

Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M

(2015) Kenneth S Thress et al.   NATURE MEDICINE

Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer

(2015)   NEW ENGLAND JOURNAL OF MEDICINE

AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer

(2015) Pasi A. Jänne et al.   NEW ENGLAND JOURNAL OF MEDICINE

AZD9291, an Irreversible EGFR TKI, Overcomes T790M-Mediated Resistance to EGFR Inhibitors in Lung Cancer

(2014) D. A. E. Cross et al.   Cancer Discovery

Effects of oncogenic mutations on the conformational free-energy landscape of EGFR kinase

(2013) L. Sutto et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Transitions to catalytically inactive conformations in EGFR kinase

(2013) Y. Shan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC

(2013) A. O. Walter et al.   Cancer Discovery

Oncogenic Mutations Counteract Intrinsic Disorder in the EGFR Kinase and Promote Receptor Dimerization

(2012) Yibing Shan et al.   CELL

HER2 Amplification: A Potential Mechanism of Acquired Resistance to EGFR Inhibition in EGFR -Mutant Lung Cancers That Lack the Second-Site EGFR T790M Mutation

(2012) Ken Takezawa et al.   Cancer Discovery

Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors

(2011) L. V. Sequist et al.   Science Translational Medicine

PTEN Loss Contributes to Erlotinib Resistance in EGFR-Mutant Lung Cancer by Activation of Akt and EGFR

(2009) M. L. Sos et al.   CANCER RESEARCH