Are erlotinib and gefitinib interchangeable, opposite or complementary for non-small cell lung cancer treatment? Biological, pharmacological and clinical aspects.

[1]  E. Tekle,et al.  Epidermal Growth Factor (EGF)-induced Generation of Hydrogen Peroxide , 1997, The Journal of Biological Chemistry.

[2]  R. Klemke,et al.  Four Human Ras Homologs Differ in Their Abilities to Activate Raf-1, Induce Transformation, and Stimulate Cell Motility* , 1999, The Journal of Biological Chemistry.

[3]  S. Meakin,et al.  The Signaling Adapter FRS-2 Competes with Shc for Binding to the Nerve Growth Factor Receptor TrkA , 1999, The Journal of Biological Chemistry.

[4]  W. Kolch Meaningful relationships: the regulation of the Ras/Raf/MEK/ERK pathway by protein interactions. , 2000, The Biochemical journal.

[5]  Y. Yarden,et al.  Untangling the ErbB signalling network , 2001, Nature Reviews Molecular Cell Biology.

[6]  W. Gullick,et al.  The Type 1 growth factor receptors and their ligands considered as a complex system. , 2001, Endocrine-related cancer.

[7]  E. Hafen,et al.  PDK1 regulates growth through Akt and S6K in Drosophila , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[8]  C. Arteaga Overview of epidermal growth factor receptor biology and its role as a therapeutic target in human neoplasia. , 2002, Seminars in oncology.

[9]  C. Arteaga,et al.  Gefitinib in recurrent non-small-cell lung cancer: an IDEAL trial? , 2003, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[10]  Masahiro Fukuoka,et al.  Multi-institutional randomized phase II trial of gefitinib for previously treated patients with advanced non-small-cell lung cancer (The IDEAL 1 Trial) [corrected]. , 2003, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[11]  David Cella,et al.  Efficacy of gefitinib, an inhibitor of the epidermal growth factor receptor tyrosine kinase, in symptomatic patients with non-small cell lung cancer: a randomized trial. , 2003, JAMA.

[12]  Patricia L. Harris,et al.  Activating mutations in the epidermal growth factor receptor underlying responsiveness of non-small-cell lung cancer to gefitinib. , 2004, The New England journal of medicine.

[13]  M. Cantarini,et al.  Relative bioavailability and safety profile of gefitinib administered as a tablet or as a dispersion preparation via drink or nasogastric tube: results of a randomized, open-label, three-period crossover study in healthy volunteers. , 2004, Clinical therapeutics.

[14]  S. Gabriel,et al.  EGFR Mutations in Lung Cancer: Correlation with Clinical Response to Gefitinib Therapy , 2004, Science.

[15]  R. Wilson,et al.  EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib. , 2004, Proceedings of the National Academy of Sciences of the United States of America.

[16]  Roy S Herbst,et al.  Gefitinib in combination with paclitaxel and carboplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 2. , 2004, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[17]  G. Giaccone,et al.  Gefitinib in combination with gemcitabine and cisplatin in advanced non-small-cell lung cancer: a phase III trial--INTACT 1. , 2004, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[18]  Renato Martins,et al.  Erlotinib in previously treated non-small-cell lung cancer. , 2005, The New England journal of medicine.

[19]  Kevin Carroll,et al.  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, The Lancet.

[20]  György Kéri,et al.  Cellular targets of gefitinib. , 2005, Cancer research.

[21]  M. Meyerson,et al.  Epidermal growth factor-independent transformation of Ba/F3 cells with cancer-derived epidermal growth factor receptor mutants induces gefitinib-sensitive cell cycle progression. , 2005, Cancer research.

[22]  Xin Li,et al.  TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer. , 2005, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[23]  B. Lum,et al.  Evaluation of the Absolute Oral Bioavailability and Bioequivalence of Erlotinib, an Inhibitor of the Epidermal Growth Factor Receptor Tyrosine Kinase, in a Randomized, Crossover Study in Healthy Subjects , 2006, Journal of clinical pharmacology.

[24]  William Pao,et al.  Novel D761Y and Common Secondary T790M Mutations in Epidermal Growth Factor Receptor–Mutant Lung Adenocarcinomas with Acquired Resistance to Kinase Inhibitors , 2006, Clinical Cancer Research.

[25]  M. Nishimura,et al.  Clinical benefit of readministration of gefitinib for initial gefitinib-responders with non-small cell lung cancer , 2007, BMC Cancer.

[26]  G. Clark,et al.  Effects of Smoking on the Pharmacokinetics of Erlotinib , 2006, Clinical Cancer Research.

[27]  L. Seymour,et al.  Smoking history and epidermal growth factor receptor expression as predictors of survival benefit from erlotinib for patients with non-small-cell lung cancer in the National Cancer Institute of Canada Clinical Trials Group study BR.21. , 2006, Clinical lung cancer.

[28]  F. Hirsch,et al.  Molecular predictors of outcome with gefitinib in a phase III placebo-controlled study in advanced non-small-cell lung cancer. , 2006, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[29]  Boris N Kholodenko,et al.  Scaffolding Protein Grb2-associated Binder 1 Sustains Epidermal Growth Factor-induced Mitogenic and Survival Signaling by Multiple Positive Feedback Loops* , 2006, Journal of Biological Chemistry.

[30]  T. Čufer,et al.  Phase II, open-label, randomized study (SIGN) of single-agent gefitinib (IRESSA) or docetaxel as second-line therapy in patients with advanced (stage IIIb or IV) non-small-cell lung cancer , 2006, Anti-cancer drugs.

[31]  D. Tenen,et al.  BIM Mediates EGFR Tyrosine Kinase Inhibitor-Induced Apoptosis in Lung Cancers with Oncogenic EGFR Mutations , 2007, PLoS medicine.

[32]  G. Giaccone,et al.  Functional analysis of cancer-associated EGFR mutants using a cellular assay with YFP-tagged EGFR intracellular domain , 2007, Molecular Cancer.

[33]  M. Hidalgo,et al.  Differential Metabolism of Gefitinib and Erlotinib by Human Cytochrome P450 Enzymes , 2007, Clinical Cancer Research.

[34]  Matthew Meyerson,et al.  Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity. , 2007, Cancer cell.

[35]  J. Milanowski,et al.  Phase III study of erlotinib in combination with cisplatin and gemcitabine in advanced non-small-cell lung cancer: the Tarceva Lung Cancer Investigation Trial. , 2007, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[36]  D. Haber,et al.  Epidermal growth factor receptor mutants from human lung cancers exhibit enhanced catalytic activity and increased sensitivity to gefitinib. , 2007, Cancer research.

[37]  T. Boggon,et al.  P2-138: Disruption of a conserved ion pair E884-R958 in EGFR differentially alters kinase inhibitor sensitivity and downstream signaling , 2007 .

[38]  Hoguen Kim,et al.  Phase II study of erlotinib in advanced non-small-cell lung cancer after failure of gefitinib. , 2007, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[39]  P. Jänne,et al.  Effects of Erlotinib in EGFR Mutated Non-Small Cell Lung Cancers with Resistance to Gefitinib , 2008, Clinical Cancer Research.

[40]  R. Soong,et al.  Evidence for Disease Control with Erlotinib after Gefitinib Failure in Typical Gefitinib-Sensitive Asian Patients with Non-small Cell Lung Cancer , 2008, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.

[41]  A. Dowlati,et al.  Randomized phase II trial of erlotinib or standard chemotherapy in patients with advanced non-small-cell lung cancer and a performance status of 2. , 2008, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[42]  M. Ladanyi,et al.  Acquired Resistance to Epidermal Growth Factor Receptor Kinase Inhibitors Associated with a Novel T854A Mutation in a Patient with EGFR-Mutant Lung Adenocarcinoma , 2008, Clinical Cancer Research.

[43]  B. Lum,et al.  Effect of food on the pharmacokinetics of erlotinib, an orally active epidermal growth factor receptor tyrosine-kinase inhibitor, in healthy individuals , 2008, Anti-cancer drugs.

[44]  Kenji Eguchi,et al.  Phase III study, V-15-32, of gefitinib versus docetaxel in previously treated Japanese patients with non-small-cell lung cancer. , 2008, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[45]  T. Mok,et al.  Better survival with EGFR exon 19 than exon 21 mutations in gefitinib-treated non-small cell lung cancer patients is due to differential inhibition of downstream signals. , 2008, Cancer letters.

[46]  M. Meyerson,et al.  The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP , 2008, Proceedings of the National Academy of Sciences.

[47]  D. Lee,et al.  Phase II study of erlotinib as a salvage treatment for non-small-cell lung cancer patients after failure of gefitinib treatment. , 2008, Annals of oncology : official journal of the European Society for Medical Oncology.

[48]  Jeremy Purvis,et al.  Role of Network Branching in Eliciting Differential Short‐Term Signaling Responses in the Hypersensitive Epidermal Growth Factor Receptor Mutants Implicated in Lung Cancer , 2008, Biotechnology progress.

[49]  Edward S. Kim,et al.  Gefitinib versus docetaxel in previously treated non-small-cell lung cancer (INTEREST): a randomised phase III trial , 2008, The Lancet.

[50]  D. Tenen,et al.  Differential responses to erlotinib in epidermal growth factor receptor (EGFR)-mutated lung cancers with acquired resistance to gefitinib carrying the L747S or T790M secondary mutations. , 2008, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[51]  W. Lam,et al.  Erlotinib as salvage treatment after failure to first-line gefitinib in non-small cell lung cancer , 2009, Cancer Chemotherapy and Pharmacology.

[52]  Edward S. Kim,et al.  Comparison of gefitinib and docetaxel in patients with pretreated advanced non-small cell lung cancer (NSCLC): Meta-analysis from four clinical trials. , 2009, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[53]  Y. Bang,et al.  Erlotinib after Gefitinib failure in female never-smoker Asian patients with pulmonary adenocarcinoma. , 2009, Lung cancer.

[54]  T. Mok,et al.  Gefitinib or carboplatin-paclitaxel in pulmonary adenocarcinoma. , 2009, The New England journal of medicine.

[55]  J. Ahn,et al.  Randomized Phase III Trial of Gefitinib versus Docetaxel in Non–Small Cell Lung Cancer Patients Who Have Previously Received Platinum-Based Chemotherapy , 2010, Clinical Cancer Research.

[56]  A. Gemma,et al.  F1000 highlights , 2010 .

[57]  J. Ahn,et al.  Comparison of gefitinib versus erlotinib in patients with nonsmall cell lung cancer who failed previous chemotherapy , 2010, Cancer.

[58]  S. Agelaki,et al.  Pemetrexed (MTA) compared with erlotinib (ERL) in pretreated patients with advanced non-small cell lung cancer (NSCLC): Results of a randomized phase III Hellenic Oncology Research Group trial. , 2010 .

[59]  P. Schnabel,et al.  Erlotinib versus carboplatin/vinorelbine in elderly patients (age 70 or older) with advanced non-small cell lung carcinoma (NSCLC): A randomized phase II study of the German Thoracic Oncology Working Group. , 2010 .

[60]  Yukiko Nakamura,et al.  Pooled analysis of the reports of erlotinib after failure of gefitinib for non-small cell lung cancer. , 2010, Lung cancer.

[61]  E. Giovannetti,et al.  Molecular Cancer Therapeutics Association of Polymorphisms in AKT 1 and EGFR with Clinical Outcome and Toxicity in Non – Small Cell Lung Cancer Patients Treated with Gefitinib , 2010 .

[62]  Bruce E. Johnson,et al.  Overall survival (OS) in ATLAS, a phase IIIb trial comparing bevacizumab (B) therapy with or without erlotinib (E) after completion of chemotherapy (chemo) with B for first-line treatment of locally advanced, recurrent, or metastatic non-small cell lung cancer (NSCLC). , 2010 .

[63]  G. Giaccone,et al.  Erlotinib as maintenance treatment in advanced non-small-cell lung cancer: a multicentre, randomised, placebo-controlled phase 3 study. , 2010, The Lancet. Oncology.

[64]  Edward S. Kim,et al.  Molecular predictors of outcome with gefitinib and docetaxel in previously treated non-small-cell lung cancer: data from the randomized phase III INTEREST trial. , 2010, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[65]  J. Schlessinger,et al.  Cell Signaling by Receptor Tyrosine Kinases , 2000, Cell.

[66]  Sang-We Kim,et al.  Phase II study of erlotinib for chemotherapy-naïve patients with advanced or metastatic non-small cell lung cancer who are ineligible for platinum doublets , 2010, Cancer Chemotherapy and Pharmacology.

[67]  Laura La Paglia,et al.  Driver mutations and differential sensitivity to targeted therapies: a new approach to the treatment of lung adenocarcinoma. , 2010, Cancer treatment reviews.

[68]  S. Toyooka,et al.  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. , 2010, The Lancet. Oncology.

[69]  Masahiro Fukuoka,et al.  Biomarker analyses and final overall survival results from a phase III, randomized, open-label, first-line study of gefitinib versus carboplatin/paclitaxel in clinically selected patients with advanced non-small-cell lung cancer in Asia (IPASS). , 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[70]  L. Trusolino,et al.  Oncogene addiction as a foundational rationale for targeted anti-cancer therapy: promises and perils , 2011, EMBO molecular medicine.

[71]  Jun Ma,et al.  Erlotinib versus chemotherapy as first-line treatment for patients with advanced EGFR mutation-positive non-small-cell lung cancer (OPTIMAL, CTONG-0802): a multicentre, open-label, randomised, phase 3 study. , 2011, The Lancet. Oncology.

[72]  G. Ku,et al.  Gefitinib vs. chemotherapy as first-line therapy in advanced non-small cell lung cancer: meta-analysis of phase III trials. , 2011, Lung cancer.

[73]  Yeun-Chung Chang,et al.  Comparison of gefitinib and erlotinib in advanced NSCLC and the effect of EGFR mutations. , 2011, Lung cancer.

[74]  C. Ficorella,et al.  EGFR genomic alterations in cancer: prognostic and predictive values. , 2011, Frontiers in bioscience.

[75]  Yu-Quan Wei,et al.  Systems Biology Modeling Reveals a Possible Mechanism of the Tumor Cell Death upon Oncogene Inactivation in EGFR Addicted Cancers , 2011, PloS one.

[76]  S. Barni,et al.  Erlotinib as maintenance therapy in patients with advanced non-small cell lung cancer: a pooled analysis of three randomized trials , 2011, Anti-cancer drugs.

[77]  Hyae-Young Kim,et al.  First-SIGNAL: first-line single-agent iressa versus gemcitabine and cisplatin trial in never-smokers with adenocarcinoma of the lung. , 2012, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[78]  J. Whang‐Peng,et al.  Erlotinib has better efficacy than gefitinib in adenocarcinoma patients without EGFR-activating mutations, but similar efficacy in patients with EGFR-activating mutations. , 2012, Experimental and therapeutic medicine.

[79]  L. Seymour,et al.  Pharmacogenetic Analysis of BR.21, a Placebo-Controlled Randomized Phase III Clinical Trial of Erlotinib in Advanced Non-small Cell Lung Cancer , 2012, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.

[80]  A. Awada,et al.  Milestones in the use of chemotherapy for the management of non-small cell lung cancer (NSCLC). , 2011, Critical reviews in oncology/hematology.

[81]  E. Giovannetti,et al.  EGF receptor-targeted therapy in non-small-cell lung cancer: role of germline polymorphisms in outcome and toxicity. , 2012, Future oncology.

[82]  A. Custodio,et al.  Strategies for maintenance therapy in advanced non-small cell lung cancer: current status, unanswered questions and future directions. , 2012, Critical reviews in oncology/hematology.

[83]  T. Bivona,et al.  Mechanisms of Resistance to Epidermal Growth Factor Receptor Inhibitors and Novel Therapeutic Strategies to Overcome Resistance in NSCLC Patients , 2012, Chemotherapy research and practice.

[84]  S. Barni,et al.  Relationship between skin rash and outcome in non-small-cell lung cancer patients treated with anti-EGFR tyrosine kinase inhibitors: a literature-based meta-analysis of 24 trials. , 2012, Lung cancer.

[85]  Ying Cheng,et al.  Gefitinib versus placebo as maintenance therapy in patients with locally advanced or metastatic non-small-cell lung cancer (INFORM; C-TONG 0804): a multicentre, double-blind randomised phase 3 trial. , 2012, The Lancet. Oncology.

[86]  T. Ciuleanu,et al.  Efficacy and safety of erlotinib versus chemotherapy in second-line treatment of patients with advanced, non-small-cell lung cancer with poor prognosis (TITAN): a randomised multicentre, open-label, phase 3 study. , 2012, The Lancet. Oncology.

[87]  W. Zhou,et al.  Maintenance erlotinib improves clinical outcomes of unresectable advanced non-small cell lung cancer: A meta-analysis of randomized controlled trials , 2012, Experimental and therapeutic medicine.

[88]  C. Mermel,et al.  Concomitant Actionable Mutations and Overall Survival (OS) in Egfr-Mutant Non-Small-Cell Lung Cancer (NSCLC) Patients (P) Included in The Eurtac Trial: EGFR L858R, EGFR T790M, TP53 R273H and EML4-ALK (V3) , 2012 .

[89]  C. Langer Individualized therapy for patients with non-small cell lung cancer: emerging trends and challenges. , 2012, Critical reviews in oncology/hematology.

[90]  H. Sasaki,et al.  Polymorphisms in intron 1 of the EGFR gene in non-small cell lung cancer patients , 2012, Experimental and therapeutic medicine.

[91]  J. Whang‐Peng,et al.  Phase II Randomized Trial of Erlotinib or Vinorelbine in Chemonaive, Advanced, Non-small Cell Lung Cancer Patients Aged 70 Years or Older , 2012, Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer.

[92]  I. Sohn,et al.  Randomized phase II study of gefitinib versus erlotinib in patients with advanced non-small cell lung cancer who failed previous chemotherapy. , 2010, Lung cancer.

[93]  E. Felip,et al.  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, The Lancet. Oncology.

[94]  M. Lai,et al.  Comparison of gefitinib and erlotinib efficacies as third-line therapy for advanced non-small-cell lung cancer. , 2013, European journal of cancer.

[95]  Yongmei Yin,et al.  Gefitinib or Erlotinib as Maintenance Therapy in Patients with Advanced Stage Non-Small Cell Lung Cancer: A Systematic Review , 2013, PloS one.

[96]  G. Giaccone,et al.  Sensitivity and kinase activity of epidermal growth factor receptor (EGFR) exon 19 and others to EGFR‐tyrosine kinase inhibitors , 2013, Cancer science.