Understanding the New Genetics of Responsiveness to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors

Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to Gefitinib

2004 • 11,185 citations

EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy

2004 • 9,201 citations

Erlotinib in Previously Treated Non–Small-Cell Lung Cancer

2005 • 5,383 citations

EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib

2004 • 4,293 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

Multi-Institutional Randomized Phase II Trial of Gefitinib for Previously Treated Patients With Advanced Non–Small-Cell Lung Cancer

2003 • 2,874 citations

Epidermal growth factor-related peptides and their receptors in human malignancies

1995 • 2,689 citations

Efficacy of Gefitinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in Symptomatic Patients With Non–Small Cell Lung Cancer

2003 • 2,522 citations

Clinical and Biological Features Associated With Epidermal Growth Factor Receptor Gene Mutations in Lung Cancers

2005 • 2,285 citations

Gefitinib plus best supportive care in previously treated patients with refractory advanced non-small-cell lung cancer: results from a randomised, placebo-controlled, multicentre study (Iressa Survival Evaluation in Lung Cancer)

2005 • 2,102 citations

Erlotinib in Lung Cancer — Molecular and Clinical Predictors of Outcome

2005 • 1,834 citations

Gefitinib in Combination With Gemcitabine and Cisplatin in Advanced Non–Small-Cell Lung Cancer: A Phase III Trial—INTACT 1

2004 • 1,733 citations

Gefitinib in Combination With Paclitaxel and Carboplatin in Advanced Non–Small-Cell Lung Cancer: A Phase III Trial—INTACT 2

2004 • 1,723 citations

TRIBUTE: A Phase III Trial of Erlotinib Hydrochloride (OSI-774) Combined With Carboplatin and Paclitaxel Chemotherapy in Advanced Non–Small-Cell Lung Cancer

2005 • 1,517 citations

KRAS Mutations and Primary Resistance of Lung Adenocarcinomas to Gefitinib or Erlotinib

2005 • 1,510 citations

Mutations in the Epidermal Growth Factor Receptor and in KRAS Are Predictive and Prognostic Indicators in Patients With Non–Small-Cell Lung Cancer Treated With Chemotherapy Alone and in Combination With Erlotinib

2005 • 1,467 citations

The EGF receptor family as targets for cancer therapy

2000 • 1,339 citations

Mutations of the Epidermal Growth Factor Receptor Gene in Lung Cancer

2004 • 1,206 citations

Phase I and Pharmacologic Study of OSI-774, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, in Patients With Advanced Solid Malignancies

2001 • 995 citations

Mutations of the Epidermal Growth Factor Receptor Gene Predict Prolonged Survival After Gefitinib Treatment in Patients With Non–Small-Cell Lung Cancer With Postoperative Recurrence

2005 • 965 citations

The Epidermal Growth Factor Receptor and Its Inhibition in Cancer Therapy

1999 • 840 citations

Phase I Safety, Pharmacokinetic, and Pharmacodynamic Trial of ZD1839, a Selective Oral Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, in Patients With Five Selected Solid Tumor Types

2002 • 828 citations

EGFR Mutations in Non–Small-Cell Lung Cancer: Analysis of a Large Series of Cases and Development of a Rapid and Sensitive Method for Diagnostic Screening With Potential Implications on Pharmacologic Treatment

2005 • 792 citations

Predictive and Prognostic Impact of Epidermal Growth Factor Receptor Mutation in Non–Small-Cell Lung Cancer Patients Treated With Gefitinib

2005 • 782 citations

ZD1839, a Selective Oral Epidermal Growth Factor Receptor–Tyrosine Kinase Inhibitor, Is Well Tolerated and Active in Patients With Solid, Malignant Tumors: Results of a Phase I Trial

2002 • 764 citations

Intragenic ERBB2 kinase mutations in tumours

2004 • 753 citations

Clinical Course of Patients with Non–Small Cell Lung Cancer and Epidermal Growth Factor Receptor Exon 19 and Exon 21 Mutations Treated with Gefitinib or Erlotinib

2006 • 720 citations

Molecular Predictors of Outcome With Gefitinib in a Phase III Placebo-Controlled Study in Advanced Non–Small-Cell Lung Cancer

2006 • 710 citations

Epidermal Growth Factor Receptor Gene Mutations and Increased Copy Numbers Predict Gefitinib Sensitivity in Patients With Recurrent Non–Small-Cell Lung Cancer

2005 • 704 citations

Oncogenic Transformation by Inhibitor-Sensitive and -Resistant EGFR Mutants

2005 • 669 citations

Somatic Mutations of the HER2 Kinase Domain in Lung Adenocarcinomas

2005 • 652 citations

Somatic mutations of epidermal growth factor receptor signaling pathway in lung cancers

2005 • 640 citations

Epidermal Growth Factor Receptor Mutations and Gene Amplification in Non–Small-Cell Lung Cancer: Molecular Analysis of the IDEAL/INTACT Gefitinib Trials

2005 • 609 citations

Increased Epidermal Growth Factor Receptor Gene Copy Number Detected by Fluorescence In Situ Hybridization Associates With Increased Sensitivity to Gefitinib in Patients With Bronchioloalveolar Carcinoma Subtypes: A Southwest Oncology Group Study

2005 • 590 citations

Selective Oral Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor ZD1839 Is Generally Well-Tolerated and Has Activity in Non–Small-Cell Lung Cancer and Other Solid Tumors: Results of a Phase I Trial

2002 • 583 citations

Exon 19 Deletion Mutations of Epidermal Growth Factor Receptor Are Associated with Prolonged Survival in Non–Small Cell Lung Cancer Patients Treated with Gefitinib or Erlotinib

2006 • 568 citations

Detection of p53 Gene Mutations in Human Brain Tumors by Single-strand Conformation Polymorphism Analysis of Polymerase Chain Reaction Products

1991 • 556 citations

Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo.

2001 • 550 citations

The tyrosine kinase inhibitor ZD1839 ("Iressa") inhibits HER2-driven signaling and suppresses the growth of HER2-overexpressing tumor cells.

2001 • 516 citations

Inherited susceptibility to lung cancer may be associated with the T790M drug resistance mutation in EGFR

2005 • 508 citations

Prospective Phase II Study of Gefitinib for Chemotherapy-Naïve Patients With Advanced Non–Small-Cell Lung Cancer With Epidermal Growth Factor Receptor Gene Mutations

2006 • 507 citations

Incidence and possible clinical significance of K-ras oncogene activation in adenocarcinoma of the human lung.

1988 • 458 citations

HER2 kinase domain mutation results in constitutive phosphorylation and activation of HER2 and EGFR and resistance to EGFR tyrosine kinase inhibitors

2006 • 449 citations

Cigarette smoking is strongly associated with mutation of the K-ras gene in patients with primary adenocarcinoma of the lung

2001 • 443 citations

Differential endocytic routing of homo- and hetero-dimeric ErbB tyrosine kinases confers signaling superiority to receptor heterodimers

1998 • 400 citations

IncreasedHER2Gene Copy Number Is Associated With Response to Gefitinib Therapy in Epidermal Growth Factor Receptor–Positive Non–Small-Cell Lung Cancer Patients

2005 • 365 citations

Activating Mutations in the Tyrosine Kinase Domain of the Epidermal Growth Factor Receptor Are Associated with Improved Survival in Gefitinib-Treated Chemorefractory Lung Adenocarcinomas

2005 • 338 citations

Mutation in the Tyrosine Kinase Domain of Epidermal Growth Factor Receptor Is a Predictive and Prognostic Factor for Gefitinib Treatment in Patients with Non–Small Cell Lung Cancer

2005 • 315 citations

Overview of epidermal growth factor receptor biology and its role as a therapeutic target in human neoplasia

2002 • 306 citations

Results of a phase III trial of erlotinib (OSI-774) combined with cisplatin and gemcitabine (GC) chemotherapy in advanced non-small cell lung cancer (NSCLC)

2004 • 301 citations

Cooperative inhibitory effect of ZD1839 (Iressa) in combination with trastuzumab (Herceptin) on human breast cancer cell growth

2002 • 276 citations

Phase I pharmacokinetic trial of the selective oral epidermal growth factor receptor tyrosine kinase inhibitor gefitinib (‘Iressa’, ZD1839) in Japanese patients with solid malignant tumors

2003 • 271 citations

Optimization of Patient Selection for Gefitinib in Non–Small Cell Lung Cancer by Combined Analysis of Epidermal Growth Factor Receptor Mutation, K-ras Mutation, and Akt Phosphorylation

2006 • 257 citations

ZD1839, a specific epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, induces the formation of inactive EGFR/HER2 and EGFR/HER3 heterodimers and prevents heregulin signaling in HER2-overexpressing breast cancer cells.

2003 • 245 citations

Epidermal growth factor receptor activating mutations in Spanish gefitinib-treated non-small-cell lung cancer patients

2005 • 233 citations

Implications and Prognostic Value of K-ras Mutation for Early-Stage Lung Cancer in Women

1999 • 229 citations

Detection of ras gene mutations in human lung cancers by single-strand conformation polymorphism analysis of polymerase chain reaction products.

1990 • 213 citations

Gefitinib in Pretreated Non–Small-Cell Lung Cancer (NSCLC): Analysis of Efficacy and Correlation With HER2 and Epidermal Growth Factor Receptor Expression in Locally Advanced or Metastatic NSCLC

2003 • 213 citations

Use of Cigarette-Smoking History to Estimate the Likelihood of Mutations in Epidermal Growth Factor Receptor Gene Exons 19 and 21 in Lung Adenocarcinomas

2006 • 209 citations

K-ras oncogene mutation as a prognostic marker in non-small cell lung cancer: a combined analysis of 881 cases

1999 • 175 citations

Predictors of the Response to Gefitinib in Refractory Non–Small Cell Lung Cancer

2005 • 175 citations

A prospective phase II trial of erlotinib in advanced non-small cell lung cancer (NSCLC) patients (p) with mutations in the tyrosine kinase (TK) domain of the epidermal growth factor receptor (EGFR)

2006 • 164 citations

Epidermal growth factor receptor expression, signal pathway, and inhibitors in non–small cell lung cancer

2002 • 142 citations

Exclusive mutation in epidermal growth factor receptor gene, HER‐2, and KRAS, and synchronous methylation of nonsmall cell lung cancer

2006 • 126 citations

Gefitinib as a First-Line Therapy of Advanced or Metastatic Adenocarcinoma of the Lung in Never-Smokers

2005 • 126 citations

Gefitinib-Sensitive Mutations of the Epidermal Growth Factor Receptor Tyrosine Kinase Domain in Chinese Patients with Non–Small Cell Lung Cancer

2005 • 120 citations

Epidermal growth factor receptor expression, signal pathway, and inhibitors in non[ndash ]small cell lung cancer

2002 • 116 citations

Molecular Context of theEGFRMutations: Evidence for the Activation of mTOR/S6K Signaling

2006 • 114 citations

HER2 Overexpression Increases Sensitivity to Gefitinib, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor, through Inhibition of HER2/HER3 Heterodimer Formation in Lung Cancer Cells

2005 • 109 citations

The EGFR mutation and its correlation with response of gefitinib in previously treated Chinese patients with advanced non-small-cell lung cancer

2005 • 96 citations

O-242 Gefitinib (‘Iressa’, ZD1839) monotherapy for pretreated advanced non-small-cell lung cancer in IDEAL 1 and 2: tumor response is not clinically relevantly predictable from tumor EGFR membrane staining alone

2003 • 96 citations

Epidermal Growth Factor Receptor Messenger RNA Expression, Gene Dosage, and Gefitinib Sensitivity in Non–Small Cell Lung Cancer

2006 • 96 citations

Prognostic significance of K-ras, p53, bcl-2, PCNA, CD34 in radically resected non-small cell lung cancers

2003 • 77 citations

EGFR point mutation in non‐small cell lung cancer is occasionally accompanied by a second mutation or amplification

2006 • 74 citations

The in vitroeffect of gefitinib ('Iressa') alone and in combination with cytotoxic chemotherapy on human solid tumours

2004 • 62 citations

Trimodality treatment in Stage III nonsmall cell lung carcinoma

2002 • 55 citations

An analysis of the prognostic and predictive importance of K-ras mutation status in the National Cancer Institute of Canada Clinical Trials Group BR.21 study of erlotinib versus placebo in the treatment of non-small cell lung cancer

2006 • 50 citations

HER1/EGFR-targeted agents: predicting the future for patients with unpredictable outcomes to therapy

2005 • 49 citations

A phase I study of oral ZD 1839 given daily in patients with solid tumors: IND.122, a study of the Investigational New Drug Program of the National Cancer Institute of Canada Clinical Trials Group

2005 • 46 citations

EGFR mutation and copy number, EGFR protein expression and KRAS mutation as predictors of outcome with erlotinib in bronchioloalveolar cell carcinoma (BAC): Results of a prospective phase II trial

2006 • 43 citations

Exploratory analyses EGFR, kRAS mutations and other molecular markers in tumors of NSCLC patients (pts) treated with chemotherapy +/- erlotinib (TALENT)

2005 • 41 citations

P-611 Final results from a phase II study of erlotinib (TarcevaTM) monotherapy in patients with advanced non-small cell lung cancer following failure of platinum-based chemotherapy

2003 • 29 citations

Predicting clinical benefit from EGFR TKIs: Not all EGFR mutations are equal

2006 • 25 citations

Phase II study of gefitinib for non-small cell lung cancer (NSCLC) patients with epidermal growth factor receptor (EGFR) gene mutations detected by PNA-LNA PCR clamp

2006 • 23 citations

Phase II study of the efficacy of gefitinib in patients with non-small cell lung cancer with the EGFR mutations

2006 • 22 citations

EGFR mutation-based phase II multicenter trial of gefitinib in advanced non-small cell lung cancer (NSCLC) patients (pts): Results of West Japan Thoracic Oncology Group trial (WJTOG0403)

2006 • 17 citations

EGFR mutations and pAKT expression as potential predictors of gefitinib efficacy in non-small cell lung cancer (NSCLC) patients (pts)

2005 • 12 citations

Biologically Targeted Treatment of Non–Small-Cell Lung Cancer: Focus on Epidermal Growth Factor Receptor

2003 • 10 citations

EGFR mutations (muts), IHC and FISH status, and chromosome 7 gene copy number combined with pAkt expression as potential predictors of survival in non-small cell lung cancer (NSCLC) patients (pts) treated with gefitinib (GEF)

2006 • 8 citations

A phase II study of gefitinib as a first-line therapy for advanced non-small cell lung cancers with epidermal growth factor receptor (EGFR) gene mutations

2006 • 6 citations