Mechanism of Resistance to Epidermal Growth Factor Receptor-Tyrosine Kinase Inhibitors and a Potential Treatment Strategy

Acquired resistance to EGFR targeted therapy in non-small cell lung cancer: Mechanisms and therapeutic strategies

(2018) Sun Min Lim et al.   CANCER TREATMENT REVIEWS

PPARgamma agonists sensitize PTEN-deficient resistant lung cancer cells to EGFR tyrosine kinase inhibitors by inducing autophagy

(2018) Kenneth K.W. To et al.   EUROPEAN JOURNAL OF PHARMACOLOGY

Combination Strategies Using EGFR-TKi in NSCLC Therapy: Learning from the Gap between Pre-Clinical Results and Clinical Outcomes

(2018) Zheng Yang et al.   International Journal of Biological Sciences

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

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

Frequency and clinical significance of NF1 mutation in lung adenocarcinomas from East Asian patients

(2018) Yunjian Pan et al.   INTERNATIONAL JOURNAL OF CANCER

Phase Ib/II Study of Capmatinib (INC280) Plus Gefitinib After Failure of Epidermal Growth Factor Receptor (EGFR) Inhibitor Therapy in Patients With EGFR-Mutated, MET Factor–Dysregulated Non–Small-Cell Lung Cancer

(2018) Yi-Long Wu et al.   JOURNAL OF CLINICAL ONCOLOGY

LBA51Analysis of resistance mechanisms to osimertinib in patients with EGFR T790M advanced NSCLC from the AURA3 study

(2018) V A Papadimitrakopoulou et al.   ANNALS OF ONCOLOGY

LBA50Mechanisms of acquired resistance to first-line osimertinib: Preliminary data from the phase III FLAURA study

(2018) S S Ramalingam et al.   ANNALS OF ONCOLOGY

Clonal History and Genetic Predictors of Transformation Into Small-Cell Carcinomas From Lung Adenocarcinomas

(2017) June-Koo Lee et al.   JOURNAL OF CLINICAL ONCOLOGY

Lung Adenocarcinoma Harboring EGFR T790M and In Trans C797S Responds to Combination Therapy of First- and Third-Generation EGFR TKIs and Shifts Allelic Configuration at Resistance

(2017) Zhen Wang et al.   Journal of Thoracic Oncology

Tolerable and Effective Combination of Full-Dose Crizotinib and Osimertinib Targeting MET Amplification Sequentially Emerging after T790M Positivity in EGFR- Mutant Non–Small Cell Lung Cancer

(2017) Emily R. York 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

Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer

(2017) Tony S. Mok et al.   NEW ENGLAND JOURNAL OF MEDICINE

Treatment in EGFR-mutated Non-small Cell Lung Cancer: How to Block the Receptor and overcome Resistance Mechanisms

(2017) Claudia Proto et al.   TUMORI

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

(2017) Ken Uchibori et al.   Nature Communications

Mechanisms of resistance to irreversible epidermal growth factor receptor tyrosine kinase inhibitors and therapeutic strategies in non-small cell lung cancer

(2017) Jing Xu et al.   Oncotarget

Treatment in EGFR-mutated Non-small Cell Lung Cancer: How to Block the Receptor and overcome Resistance Mechanisms

(2017) Claudia Proto et al.   TUMORI JOURNAL

A Patient With Metastatic Lung Adenocarcinoma Harboring ConcurrentEGFRL858R,EGFRGermline T790M, andPIK3CAMutations: The Challenge of Interpreting Results of Comprehensive Mutational Testing in Lung Cancer

(2017) Philip E. Lammers et al.   Journal of the National Comprehensive Cancer Network

Combined analysis of rearrangement of ALK, ROS1, somatic mutation of EGFR, KRAS, BRAF, PIK3CA, and mRNA expression of ERCC1, TYMS, RRM1, TUBB3, EGFR in patients with non-small cell lung cancer and their clinical significance

(2016) Quan Zhang et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Met gene amplification and protein hyperactivation is a mechanism of resistance to both first and third generation EGFR inhibitors in lung cancer treatment

(2016) Puyu Shi et al.   CANCER LETTERS

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

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

Lung adenocarcinoma harboring concomitant SPTBN1-ALK fusion, c-Met overexpression, and HER-2 amplification with inherent resistance to crizotinib, chemotherapy, and radiotherapy

(2016) Fei-fei Gu et al.   Journal of Hematology & Oncology

Acquired Resistance to First-Line Afatinib and the Challenges of Prearranged Progression Biopsies

(2016) Meghan Campo et al.   Journal of Thoracic Oncology

Two Cases of Small Cell Lung Cancer Transformation from EGFR Mutant Adenocarcinoma During AZD9291 Treatment

(2016) Jun Soo Ham et al.   Journal of Thoracic Oncology

Acquired C797S Mutation upon Treatment with a T790M-Specific Third-Generation EGFR Inhibitor (HM61713) in Non–Small Cell Lung Cancer

(2016) Haa-Na Song et al.   Journal of Thoracic Oncology

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

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

Dramatic Response to Combination Erlotinib and Crizotinib in a Patient with Advanced, EGFR -Mutant Lung Cancer Harboring De Novo MET Amplification

(2016) Justin F. Gainor et al.   Journal of Thoracic Oncology

Afatinib versus gefitinib as first-line treatment of patients with EGFR mutation-positive non-small-cell lung cancer (LUX-Lung 7): a phase 2B, open-label, randomised controlled trial

(2016) Keunchil Park et al.   LANCET ONCOLOGY

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

(2016) Yong Jia et al.   NATURE

Tumor cells can follow distinct evolutionary paths to become resistant to epidermal growth factor receptor inhibition

(2016) Aaron N Hata et al.   NATURE MEDICINE

Reduction in Hepatocyte Growth Factor Serum Levels is Associated with Improved Prognosis in Advanced Lung Adenocarcinoma Patients Treated with Afatinib: a Phase II Trial

(2016) Oscar Arrieta et al.   Targeted Oncology

Circulating tumour DNA profiling reveals heterogeneity of EGFR inhibitor resistance mechanisms in lung cancer patients

(2016) Jacob J. Chabon et al.   Nature Communications

Activation of the IGF1R pathway potentially mediates acquired resistance to mutant-selective 3rd-generation EGF receptor tyrosine kinase inhibitors in advanced non-small cell lung cancer

(2016) Ji Hyun Park et al.   Oncotarget

The mechanism of acquired resistance to irreversible EGFR tyrosine kinase inhibitor-afatinib in lung adenocarcinoma patients

(2016) Shang-Gin Wu et al.   Oncotarget

Targeted sequencing identifies genetic alterations that confer primary resistance to EGFR tyrosine kinase inhibitor (Korean Lung Cancer Consortium)

(2016) Sun Min Lim et al.   Oncotarget

Phenotype-genotype correlation in multiple primary lung cancer patients in China

(2016) Yang Yang et al.   Scientific Reports

Osimertinib for EGFR T790M mutation-positive non-small cell lung cancer

(2016) Kenzo Soejima et al.   Expert Review of Clinical Pharmacology

Lung cancer patients withHER2mutations treated with chemotherapy andHER2-targeted drugs: results from the European EUHER2 cohort

(2015) J. Mazières et al.   ANNALS OF ONCOLOGY

EGFR-independent mechanisms of acquired resistance to AZD9291 in EGFR T790M-positive NSCLC patients

(2015) D. Planchard et al.   ANNALS OF ONCOLOGY

Epidermal growth factor receptor exon 20 insertions in advanced lung adenocarcinomas: Clinical outcomes and response to erlotinib

(2015) Jarushka Naidoo et al.   CANCER

SMO Gene Amplification and Activation of the Hedgehog Pathway as Novel Mechanisms of Resistance to Anti-Epidermal Growth Factor Receptor Drugs in Human Lung Cancer

(2015) C. M. Della Corte et al.   CLINICAL CANCER RESEARCH

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 Exon 18 Mutations in Lung Cancer: Molecular Predictors of Augmented Sensitivity to Afatinib or Neratinib as Compared with First- or Third-Generation TKIs

(2015) Y. Kobayashi et al.   CLINICAL CANCER RESEARCH

Afatinib plus Cetuximab Delays Resistance Compared to Single-Agent Erlotinib or Afatinib in Mouse Models of TKI-Naive EGFR L858R-Induced Lung Adenocarcinoma

(2015) V. Pirazzoli et al.   CLINICAL CANCER RESEARCH

EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors

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

Phase II Study of the AKT Inhibitor MK-2206 plus Erlotinib in Patients with Advanced Non-Small Cell Lung Cancer Who Previously Progressed on Erlotinib

(2015) P. N. Lara et al.   CLINICAL CANCER RESEARCH

Mechanisms of Acquired Resistance to AZD9291

(2015) Tae Min Kim et al.   Journal of Thoracic Oncology

Inhibition of IGF1R signaling abrogates resistance to afatinib (BIBW2992) in EGFR T790M mutant lung cancer cells

(2015) Yongik Lee et al.   MOLECULAR CARCINOGENESIS

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

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

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

Anaplastic Lymphoma Kinase Rearrangement in Digestive Tract Cancer: Implication for Targeted Therapy in Chinese Population

(2015) Jianming Ying et al.   PLoS One

NVP-BEZ235 overcomes gefitinib-acquired resistance by down-regulating PI3K/AKT/ mTOR phosphorylation

(2015) Gang Wu et al.   OncoTargets and Therapy

RB loss in resistant EGFR mutant lung adenocarcinomas that transform to small-cell lung cancer

(2015) Matthew J. Niederst et al.   Nature Communications

In vitro modeling to determine mutation specificity of EGFR tyrosine kinase inhibitors against clinically relevant EGFR mutants in non-small-cell lung cancer

(2015) Toshiyuki Hirano et al.   Oncotarget

Acquired Resistance ofEGFR-Mutant Lung Cancer to a T790M-Specific EGFR Inhibitor

(2015) Helena A. Yu et al.   JAMA Oncology

Coexistence of EGFR with KRAS, or BRAF, or PIK3CA somatic mutations in lung cancer: a comprehensive mutation profiling from 5125 Chinese cohorts

(2014) S Li et al.   BRITISH JOURNAL OF CANCER

The Impact of EGFR T790M Mutations and BIM mRNA Expression on Outcome in Patients with EGFR-Mutant NSCLC Treated with Erlotinib or Chemotherapy in the Randomized Phase III EURTAC Trial

(2014) C. Costa et al.   CLINICAL CANCER RESEARCH

Afatinib versus cisplatin plus gemcitabine for first-line treatment of Asian patients with advanced non-small-cell lung cancer harbouring EGFR mutations (LUX-Lung 6): an open-label, randomised phase 3 trial

(2014) Yi-Long Wu et al.   LANCET ONCOLOGY

Combining Onartuzumab with Erlotinib Inhibits Growth of Non-Small Cell Lung Cancer with Activating EGFR Mutations and HGF Overexpression

(2014) Y. Sano et al.   MOLECULAR CANCER THERAPEUTICS

PIK3CA Mutations Frequently Coexist with EGFR/KRAS Mutations in Non-Small Cell Lung Cancer and Suggest Poor Prognosis in EGFR/KRAS Wildtype Subgroup

(2014) Lei Wang et al.   PLoS One

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

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

Reduced NF1 Expression Confers Resistance to EGFR Inhibition in Lung Cancer

(2014) E. C. de Bruin et al.   Cancer Discovery

Cetuximab Response of Lung Cancer-Derived EGF Receptor Mutants Is Associated with Asymmetric Dimerization

(2013) J. Cho et al.   CANCER RESEARCH

Analysis of Tumor Specimens at the Time of Acquired Resistance to EGFR-TKI Therapy in 155 Patients with EGFR-Mutant Lung Cancers

(2013) H. A. Yu et al.   CLINICAL CANCER RESEARCH

LUX-Lung 4: A Phase II Trial of Afatinib in Patients With Advanced Non–Small-Cell Lung Cancer Who Progressed During Prior Treatment With Erlotinib, Gefitinib, or Both

(2013) Nobuyuki Katakami et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma WithEGFRMutations

(2013) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

The ErbB/HER family of protein-tyrosine kinases and cancer

(2013) Robert Roskoski   PHARMACOLOGICAL RESEARCH

In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction

(2013) F. Shima 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

Activation of the AXL kinase causes resistance to EGFR-targeted therapy in lung cancer

(2012) Zhenfeng Zhang et al.   NATURE GENETICS

Lung cancers with acquired resistance to EGFR inhibitors occasionally harbor BRAF gene mutations but lack mutations in KRAS, NRAS, or MEK1

(2012) K. Ohashi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Epithelial Mesenchymal Transition in Drug Resistance and Metastasis of Lung Cancer

(2012) Fariz Nurwidya et al.   Cancer Research and Treatment

Paracrine and Autocrine Signals Induce and Maintain Mesenchymal and Stem Cell States in the Breast

(2011) Christina Scheel et al.   CELL

Hepatocyte Growth Factor Expression in EGFR Mutant Lung Cancer with Intrinsic and Acquired Resistance to Tyrosine Kinase Inhibitors in a Japanese Cohort

(2011) Seiji Yano et al.   Journal of Thoracic Oncology

Association between plasma hepatocyte growth factor and gefitinib resistance in patients with advanced non-small cell lung cancer

(2011) Ji-Youn Han et al.   LUNG CANCER

Clinical significance of serum hepatocyte growth factor and epidermal growth factor gene somatic mutations in patients with non-squamous non-small cell lung cancer receiving gefitinib or erlotinib

(2011) Katsuhiro Masago et al.   MEDICAL ONCOLOGY

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

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

BIM Expression in Treatment-Naive Cancers Predicts Responsiveness to Kinase Inhibitors

(2011) A. C. Faber et al.   Cancer Discovery

Amplification of CRKL Induces Transformation and Epidermal Growth Factor Receptor Inhibitor Resistance in Human Non-Small Cell Lung Cancers

(2011) H. W. Cheung et al.   Cancer Discovery

Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs

(2010) Jin-Haeng Chung et al.   LUNG CANCER

The emerging mechanisms of isoform-specific PI3K signalling

(2010) Bart Vanhaesebroeck et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Gefitinib or Chemotherapy for Non–Small-Cell Lung Cancer with Mutated EGFR

(2010) Makoto Maemondo et al.   NEW ENGLAND JOURNAL OF MEDICINE

Insulin-like growth factor receptor 1 (IGF1R) expression and survival in surgically resected non-small-cell lung cancer (NSCLC) patients

(2009) F. Cappuzzo et al.   ANNALS OF ONCOLOGY

Structural and mechanistic underpinnings of the differential drug sensitivity of EGFR mutations in non-small cell lung cancer

(2009) Michael J. Eck et al.   BIOCHIMICA ET BIOPHYSICA ACTA-PROTEINS AND PROTEOMICS

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

Epithelial-Mesenchymal Transitions in Development and Disease

(2009) Jean Paul Thiery et al.   CELL

Hepatocyte Growth Factor Reduces Susceptibility to an Irreversible Epidermal Growth Factor Receptor Inhibitor in EGFR-T790M Mutant Lung Cancer

(2009) T. Yamada et al.   CLINICAL CANCER RESEARCH

Erlotinib resistance in mouse models of epidermal growth factor receptor-induced lung adenocarcinoma

(2009) K. Politi et al.   Disease Models & Mechanisms

Expression of Signaling Mediators Downstream of EGF-Receptor Predict Sensitivity to Small Molecule Inhibitors Directed Against the EGF-Receptor Pathway

(2009) Martin L. Sos et al.   Journal of Thoracic Oncology

Gefitinib versus cisplatin plus docetaxel in patients with non-small-cell lung cancer harbouring mutations of the epidermal growth factor receptor (WJTOG3405): an open label, randomised phase 3 trial

(2009) Tetsuya Mitsudomi et al.   LANCET ONCOLOGY

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

(2009) Wenjun Zhou et al.   NATURE

Screening for Epidermal Growth Factor Receptor Mutations in Lung Cancer

(2009) Rafael Rosell et al.   NEW ENGLAND JOURNAL OF MEDICINE

Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma

(2009) Tony S. Mok et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hepatocyte Growth Factor Induces Gefitinib Resistance of Lung Adenocarcinoma with Epidermal Growth Factor Receptor-Activating Mutations

(2008) S. Yano et al.   CANCER RESEARCH

Kinase switching in mesenchymal-like non-small cell lung cancer lines contributes to EGFR inhibitor resistance through pathway redundancy

(2008) Stuart Thomson et al.   CLINICAL & EXPERIMENTAL METASTASIS

First-Line Gefitinib in Patients With Advanced Non–Small-Cell Lung Cancer Harboring SomaticEGFRMutations

(2008) Lecia V. Sequist et al.   JOURNAL OF CLINICAL ONCOLOGY

Epithelial to mesenchymal transition derived from repeated exposure to gefitinib determines the sensitivity to EGFR inhibitors in A549, a non-small cell lung cancer cell line

(2008) Jin Kyung Rho et al.   LUNG CANCER