Acquired resistance to TKIs in solid tumours: learning from lung cancer

Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma

2009 • 7,749 citations

Erlotinib versus standard chemotherapy as first-line treatment for European patients with advanced EGFR mutation-positive non-small-cell lung cancer (EURTAC): a multicentre, open-label, randomised phase 3 trial

2012 • 5,195 citations

MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling

2007 • 4,320 citations

Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer

2010 • 4,281 citations

EGFRMutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib

2005 • 3,807 citations

Acquired Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib Is Associated with a Second Mutation in the EGFR Kinase Domain

2005 • 3,450 citations

Crizotinib versus Chemotherapy in AdvancedALK-Positive Lung Cancer

2013 • 3,211 citations

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

2011 • 3,196 citations

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

2013 • 2,949 citations

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

2013 • 2,195 citations

The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP

2008 • 1,886 citations

MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib

2007 • 1,571 citations

ROS1 Rearrangements Define a Unique Molecular Class of Lung Cancers

2012 • 1,480 citations

BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models

2008 • 1,368 citations

Mechanisms of Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancers

2012 • 1,248 citations

Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study

2012 • 1,220 citations

EML4-ALK Mutations in Lung Cancer That Confer Resistance to ALK Inhibitors

2010 • 1,163 citations

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

2012 • 1,126 citations

Mechanisms of Resistance to Crizotinib in Patients with ALK Gene Rearranged Non–Small Cell Lung Cancer

2012 • 1,029 citations

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

2009 • 942 citations

Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib

2005 • 941 citations

Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial

2012 • 932 citations

Effect of crizotinib on overall survival in patients with advanced non-small-cell lung cancer harbouring ALK gene rearrangement: a retrospective analysis

2011 • 877 citations

Novel D761Y and Common Secondary T790M Mutations in Epidermal Growth Factor Receptor–Mutant Lung Adenocarcinomas with Acquired Resistance to Kinase Inhibitors

2006 • 824 citations

Clinical Definition of Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small-Cell Lung Cancer

2009 • 765 citations

PF00299804, an Irreversible Pan-ERBB Inhibitor, Is Effective in Lung Cancer Models withEGFRandERBB2Mutations that Are Resistant to Gefitinib

2007 • 688 citations

HER2 Amplification: A Potential Mechanism of Acquired Resistance to EGFR Inhibition in EGFR-Mutant Lung Cancers That Lack the Second-Site EGFRT790M Mutation

2012 • 638 citations

Local Ablative Therapy of Oligoprogressive Disease Prolongs Disease Control by Tyrosine Kinase Inhibitors in Oncogene-Addicted Non–Small-Cell Lung Cancer

2012 • 628 citations

Lung Cancer That Harbors an HER2 Mutation: Epidemiologic Characteristics and Therapeutic Perspectives

2013 • 601 citations

A Novel ALK Secondary Mutation and EGFR Signaling Cause Resistance to ALK Kinase Inhibitors

2011 • 587 citations

CSF Concentration of the Anaplastic Lymphoma Kinase Inhibitor Crizotinib

2011 • 576 citations

A common BIM deletion polymorphism mediates intrinsic resistance and inferior responses to tyrosine kinase inhibitors in cancer

2012 • 542 citations

Optimization of Dosing for EGFR-Mutant Non–Small Cell Lung Cancer with Evolutionary Cancer Modeling

2011 • 504 citations

BIM Mediates EGFR Tyrosine Kinase Inhibitor-Induced Apoptosis in Lung Cancers with Oncogenic EGFR Mutations

2007 • 483 citations

Response to Cabozantinib in Patients with RET Fusion-Positive Lung Adenocarcinomas

2013 • 448 citations

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

2012 • 424 citations

Activity of Crizotinib (PF02341066), a Dual Mesenchymal-Epithelial Transition (MET) and Anaplastic Lymphoma Kinase (ALK) Inhibitor, in a Non-small Cell Lung Cancer Patient with De Novo MET Amplification

2011 • 416 citations

Neratinib, an Irreversible Pan-ErbB Receptor Tyrosine Kinase Inhibitor: Results of a Phase II Trial in Patients With Advanced Non–Small-Cell Lung Cancer

2010 • 414 citations

Disease Flare after Tyrosine Kinase Inhibitor Discontinuation in Patients with EGFR-Mutant Lung Cancer and Acquired Resistance to Erlotinib or Gefitinib: Implications for Clinical Trial Design

2011 • 397 citations

"Pulsatile" high-dose weekly erlotinib for CNS metastases from EGFR mutant non-small cell lung cancer

2011 • 329 citations

Local Therapy with Continued EGFR Tyrosine Kinase Inhibitor Therapy as a Treatment Strategy in EGFR-Mutant Advanced Lung Cancers That Have Developed Acquired Resistance to EGFR Tyrosine Kinase Inhibitors

2013 • 321 citations

Induction of BIM Is Essential for Apoptosis Triggered by EGFR Kinase Inhibitors in Mutant EGFR-Dependent Lung Adenocarcinomas

2007 • 311 citations

Effects of Smoking on the Pharmacokinetics of Erlotinib

2006 • 299 citations

Dynamics of BCR-ABL kinase domain mutations in chronic myeloid leukemia after sequential treatment with multiple tyrosine kinase inhibitors

2007 • 299 citations

Drug Absorption Interactions Between Oral Targeted Anticancer Agents and PPIs: Is pH-Dependent Solubility the Achilles Heel of Targeted Therapy?

2012 • 298 citations

Prospective Assessment of Discontinuation and Reinitiation of Erlotinib or Gefitinib in Patients with Acquired Resistance to Erlotinib or Gefitinib Followed by the Addition of Everolimus

2007 • 286 citations

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

2011 • 274 citations

Cerebrospinal fluid concentration of gefitinib and erlotinib in patients with non-small cell lung cancer

2012 • 273 citations

Reactivation of ERK Signaling Causes Resistance to EGFR Kinase Inhibitors

2012 • 271 citations

Response and Resistance in a Non–Small-Cell Lung Cancer Patient With an Epidermal Growth Factor Receptor Mutation and Leptomeningeal Metastases Treated With High-Dose Gefitinib

2006 • 255 citations

Epithelial to Mesenchymal Transition in an Epidermal Growth Factor Receptor-Mutant Lung Cancer Cell Line with Acquired Resistance to Erlotinib

2011 • 244 citations

A mechanism of resistance to gefitinib mediated by cellular reprogramming and the acquisition of an FGF2-FGFR1 autocrine growth loop

2013 • 231 citations

Amplification of EGFR T790M causes resistance to an irreversible EGFR inhibitor

2010 • 223 citations

Pharmacogenomic and Pharmacokinetic Determinants of Erlotinib Toxicity

2008 • 217 citations

Development of Central Nervous System Metastases in Patients with Advanced Non–Small Cell Lung Cancer and Somatic EGFR Mutations Treated with Gefitinib or Erlotinib

2010 • 207 citations

Spectrum of Oncogenic Driver Mutations in Lung Adenocarcinomas from East Asian Never Smokers

2011 • 204 citations

The T790M “gatekeeper” mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor

2008 • 196 citations

Poor response to erlotinib in patients with tumors containing baseline EGFR T790M mutations found by routine clinical molecular testing

2014 • 186 citations

Heterogeneity of Genetic Changes Associated with Acquired Crizotinib Resistance in ALK-Rearranged Lung Cancer

2013 • 153 citations

A Patient With BRAF V600E Lung Adenocarcinoma Responding to Vemurafenib

2012 • 148 citations

Challenges relating to solid tumour brain metastases in clinical trials, part 1: patient population, response, and progression. A report from the RANO group

2013 • 120 citations

Activity of Pemetrexed on brain metastases from Non-Small Cell Lung Cancer

2009 • 114 citations

Effects of Pharmacokinetic Processes and Varied Dosing Schedules on the Dynamics of Acquired Resistance to Erlotinib in EGFR-Mutant Lung Cancer

2012 • 83 citations

First-in-human dose-finding study of the ALK/EGFR inhibitor AP26113 in patients with advanced malignancies: Updated results.

2013 • 81 citations

Erlotinib at a Dose of 25 mg Daily for Non-small Cell Lung Cancers with EGFR Mutations

2010 • 81 citations

Ligand‐triggered resistance to molecular targeted drugs in lung cancer: Roles of hepatocyte growth factor and epidermal growth factor receptor ligands

2012 • 65 citations

Activity of Afatinib/Cetuximab in Patients (PTS) with EGFR Mutant Non-Small Cell Lung Cancer (Nsclc) and Acquired Resistance (Ar) To EGFR Inhibitors

2012 • 50 citations

Twelve-Month Frequency of Drug-Metabolizing Enzyme and Transporter-Based Drug-Drug Interaction Potential in Patients Receiving Oral Enzyme-Targeted Kinase Inhibitor Antineoplastic Agents

2013 • 43 citations

Timing of Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor Therapy in Patients With Lung Cancer With EGFR Mutations

2012 • 43 citations

Efficacy and safety of PF-00299804 (PF299) in patients (pt) with advanced NSCLC after failure of at least one prior chemotherapy regimen and prior treatment with erlotinib (E): A two-arm, phase II trial

2009 • 43 citations

First-in-human evaluation of CO-1686, an irreversible, selective, and potent tyrosine kinase inhibitor of EGFR T790M.

2013 • 42 citations

Response to Crizotinib Rechallenge after Initial Progression and Intervening Chemotherapy in ALK Lung Cancer

2013 • 34 citations

Treatment of Leptomeningeal Spread of NSCLC: A Continuing Challenge

2012 • 28 citations