Cited by 109Lung Cancer Treatments and MutationsHER2/EGFR in Cancer ResearchLung Cancer Diagnosis and Treatment

The DOI matches its Crossref record; 151 of the 153 references it cites were found in a registry or an index.

Targeting EGFR in Lung Cancer: Current Standards and Developments

Díaz-Serrano, Asunción, Gella, Pablo, Jiménez, Elisabeth, Zugazagoitia, Jon, Paz-Ares Rodríguez, Luis·2018·Drugs

Open this paper in CoChat — free account

Abstract

Lung cancer is the second most common malignant tumor and the leading cause of cancer death. Epidermal growth factor receptor (EGFR)-mutant non-small cell lung cancer (NSCLC) is a distinct subtype of lung cancer comprising approximately 15-40% of non-squamous tumors. The development of first- and second-generation EGFR tyrosine kinase inhibitors (TKIs) has been a significant step forward in the treatment of patients with EGFR-mutant tumors, and over the last few years has been the therapy of choice in the initial management of patients with activating mutations in EGFR, with some differences in efficacy and toxicity profile. Up to 50% of patients treated with first- and second-generation TKIs develop an EGFR exon 20 T790M mutation at the time of progression. In this context, osimertinib has shown a great benefit in terms of progression-free survival (PFS) in the second-line setting, including central nervous system metastasis control. The FLAURA trial, which compared osimertinib to first-generation inhibitors as first-line therapy, showed a clear PFS advantage for osimertinib and a trend towards an increased overall survival (OS) assessed by investigator review. Although T790M mutation is the most common mechanism of resistance to first- and second-generation EGFR TKIs, other EGFR-dependent and -independent mechanisms have been described, such as HER2 and MET amplifications or BRAF and MEK mutations. Some mechanisms of resistance to osimertinib and other third-generation TKIs have also been described. Several fourth-generation TKIs, targeted drug combinations and immunotherapy strategies are under investigation to overcome resistance to EGFR TKIs in order to improve EGFR-mutant NSCLC patient outcomes.

Integrity signals

Registry

Crossref · 10.1007/s40265-018-0916-4

Cites

151 of 151 references verified0 citation errors · 0 not checkable

Statistics

Recomputing p-values needs the paper’s full text.

Claims the paper makes

This paper’s full text isn’t openly available, so its claims and self-check weren’t run. The registry and citation checks still apply.

Claims other papers make about this one

Each is checked against this paper’s own text: does it say what the citing paper says it does?

PD-1 and PD-L1 Immune Checkpoint Blockade to Treat Breast Cancer
Hartkopf, A. D., Taran, F., Wallwiener, M., Walter, C. B., Krämer, B., Grischke, E., & Brucker, S. Y. (2016) · Breast Care · doi:10.1159/000453569 · Cited by 30,989
Adverse Renal Effects of Immune Checkpoint Inhibitors: A Narrative Review
Wanchoo, R., Karam, S., Uppal, N. N., Barta, V. S., Deray, G., Devoe, C., Launay‐Vacher, V., Jhaveri, K. D., & on behalf of Cancer and Kidney International Network Workgroup on Immune Checkpoint Inhibitors (2017) · American Journal of Nephrology · doi:10.1159/000455014 · Cited by 15,320
Cancer Statistics, 2017.
Siegel, R. L., Miller, K. D., & Jemal, A. (2017) · CA: A Cancer Journal for Clinicians · doi:10.3322/caac.21387 · Cited by 14,712
Nivolumab versus docetaxel in advanced nonsquamous non-small-cell lung cancer
Borghaei, H., Paz-Ares, L., Horn, L., Spigel, D. R., Steins, M., Ready, N. E., Chow, L. Q., Vokes, E. E., Felip, E., Holgado, E., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1507643 · Cited by 9,335
Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma
Mok, T. S., Wu, Y.-L., Thongprasert, S., Yang, C.-H., Chu, D.-T., Saijo, N., Sunpaweravong, P., Han, B., Margono, B., Ichinose, Y., et al. (2009) · New England Journal of Medicine · doi:10.1056/nejmoa0810699 · Cited by 8,261 · cited 2×
“After molecular studies identified EGFR mutations as predictive biomarkers for EGFR TKIs therapy response [28, 29], several preclinical and clinical trials showed enhanced activity of EGFR TKIs in EGFR-mutant NSCLC.”
Cell Signaling by Receptor Tyrosine Kinases
Lemmon, M. A., & Schlessinger, J. (2010) · Cell · doi:10.1016/j.cell.2010.06.011 · Cited by 7,929
Pembrolizumab versus docetaxel for previously treated, PD-L1-positive, advanced non-small-cell lung cancer (KEYNOTE-010): a randomised controlled trial
Herbst, R. S., Baas, P., Kim, D.-W., Felip, E., Pérez-Gracia, J. L., Han, J.-Y., Molina, J., Kim, J.-H., Arvis, C. D., Ahn, M.-J., et al. (2016) · The Lancet · doi:10.1016/s0140-6736(15)01281-7 · Cited by 6,449
Comprehensive molecular profiling of lung adenocarcinoma
The Cancer Genome Atlas Research Network (2014) · Nature · doi:10.1038/nature13385 · Cited by 5,732
Gefitinib or Chemotherapy for Non–Small-Cell Lung Cancer with Mutated EGFR
Maemondo, M., Inoue, A., Kobayashi, K., Sugawara, S., Oizumi, S., Isobe, H., Gemma, A., Harada, M., Yoshizawa, H., Kinoshita, I., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa0909530 · Cited by 5,525
Osimertinib in Untreated EGFR -Mutated Advanced Non–Small-Cell Lung Cancer
Soria, J.-C., Ohe, Y., Vansteenkiste, J., Reungwetwattana, T., Chewaskulyong, B., Lee, K. H., Dechaphunkul, A., Imamura, F., Nogami, N., Kurata, T., et al. (2018) · New England Journal of Medicine · doi:10.1056/nejmoa1713137 · Cited by 5,508
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
Rosell, R., Carcereny, E., Gervais, R., Vergnenegre, A., Massuti, B., Felip, E., Palmero, R., Garcia-Gomez, R., Pallares, C., Sanchez, J. M., et al. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(11)70393-x · Cited by 5,489
Erlotinib in Previously Treated Non–Small-Cell Lung Cancer
Shepherd, F. A., Rodrigues Pereira, J., Ciuleanu, T., Tan, E. H., Hirsh, V., Thongprasert, S., Campos, D., Maoleekoonpiroj, S., Smylie, M., Martins, R., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050753 · Cited by 5,419
Comparison of Four Chemotherapy Regimens for Advanced Non–Small-Cell Lung Cancer
Schiller, J. H., Harrington, D., Belani, C. P., Langer, C., Sandler, A., Krook, J., Zhu, J., & Johnson, D. H. (2002) · New England Journal of Medicine · doi:10.1056/nejmoa011954 · Cited by 4,955
MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
Engelman, J. A., Zejnullahu, K., Mitsudomi, T., Song, Y., Hyland, C., Park, J. O., Lindeman, N., Gale, C.-M., Zhao, X., Christensen, J., et al. (2007) · Science · doi:10.1126/science.1141478 · Cited by 4,496
EGF receptor gene mutations are common in lung cancers from “never smokers” and are associated with sensitivity of tumors to gefitinib and erlotinib
Pao, W., Miller, V., Zakowski, M., Doherty, J., Politi, K., Sarkaria, I., Singh, B., Heelan, R., Rusch, V., Fulton, L., et al. (2004) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0405220101 · Cited by 4,338
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
Mitsudomi, T., Morita, S., Yatabe, Y., Negoro, S., Okamoto, I., Tsurutani, J., Seto, T., Satouchi, M., Tada, H., Hirashima, T., et al. (2010) · The Lancet Oncology · doi:10.1016/s1470-2045(09)70364-x · Cited by 4,090
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
Zhou, C., Wu, Y.-L., Chen, G., Feng, J., Liu, X.-Q., Wang, C., Zhang, S., Wang, J., Zhou, S., Ren, S., et al. (2011) · The Lancet Oncology · doi:10.1016/s1470-2045(11)70184-x · Cited by 4,081
EGFR Mutation and Resistance of Non–Small-Cell Lung Cancer to Gefitinib
Kobayashi, S., Boggon, T. J., Dayaram, T., Jänne, P. A., Kocher, O., Meyerson, M., Johnson, B. E., Eck, M. J., Tenen, D. G., & Halmos, B. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa044238 · Cited by 3,964
COMPARISON OF FOUR CHEMOTHERAPY REGIMENS FOR ADVANCED NON-SMALL-CELL LUNG CANCER
Chiller, J. O. H. S., Arrington, D. A. H., Elani, C. H. P. B., Anger, C., Andler, A. L. S., Rook, J. A. K., Hu, J., & Ohnson, D. A. H. J. (2002) · Cited by 3,730
Genotypic and Histological Evolution of Lung Cancers Acquiring Resistance to EGFR Inhibitors
Sequist, L. V., Waltman, B. A., Dias-Santagata, D., Digumarthy, S., Turke, A. B., Fidias, P., Bergethon, K., Shaw, A. T., Gettinger, S., Cosper, A. K., et al. (2011) · Science Translational Medicine · doi:10.1126/scitranslmed.3002003 · Cited by 3,499
Osimertinib or Platinum–Pemetrexed in EGFR T790M–Positive Lung Cancer
Mok, T. S., Wu, Y.-L., Ahn, M.-J., Garassino, M. C., Kim, H. R., Ramalingam, S. S., Shepherd, F. A., He, Y., Akamatsu, H., Theelen, W. S. M. E., et al. (2017) · New England Journal of Medicine · doi:10.1056/nejmoa1612674 · Cited by 3,379
Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma With EGFR Mutations
Sequist, L. V., Yang, J. C.-H., Yamamoto, N., O'Byrne, K., Hirsh, V., Mok, T., Geater, S. L., Orlov, S., Tsai, C.-M., Boyer, M., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.44.2806 · Cited by 3,228
Analysis of Tumor Specimens at the Time of Acquired Resistance to EGFR-TKI Therapy in 155 Patients with EGFR -Mutant Lung Cancers
Yu, H. A., Arcila, M. E., Rekhtman, N., Sima, C. S., Zakowski, M. F., Pao, W., Kris, M. G., Miller, V. A., Ladanyi, M., & Riely, G. J. (2013) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-12-2246 · Cited by 2,454
Lung Cancer
Herbst, R. S., Heymach, J. V., & Lippman, S. M. (2008) · New England Journal of Medicine · doi:10.1056/nejmra0802714 · Cited by 2,435
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP
Yun, C.-H., Mengwasser, K. E., Toms, A. V., Woo, M. S., Greulich, H., Wong, K.-K., Meyerson, M., & Eck, M. J. (2008) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0709662105 · Cited by 2,118 · cited 1×
“T790M mutation increases the kinase affinity for ATP, reducing the inhibitory efficacy of EGFR ATP-competitive inhibitors such as gefitinib and erlotinib [66, 67].”
AZD9291 in EGFR Inhibitor–Resistant Non–Small-Cell Lung Cancer
Jänne, P. A., Yang, J. C.-H., Kim, D.-W., Planchard, D., Ohe, Y., Ramalingam, S. S., Ahn, M.-J., Kim, S.-W., Su, W.-C., Horn, L., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1411817 · Cited by 2,116
EGFR Antagonists in Cancer Treatment
Ciardiello, F., & Tortora, G. (2008) · New England Journal of Medicine · doi:10.1056/nejmra0707704 · Cited by 2,095
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)
Thatcher, N., Chang, A., Parikh, P., Rodrigues Pereira, J., Ciuleanu, T., von Pawel, J., Thongprasert, S., Tan, E. H., Pemberton, K., Archer, V., et al. (2005) · The Lancet · doi:10.1016/s0140-6736(05)67625-8 · Cited by 2,079
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
Wu, Y.-L., Zhou, C., Hu, C.-P., Feng, J., Lu, S., Huang, Y., Li, W., Hou, M., Shi, J. H., Lee, K. Y., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(13)70604-1 · Cited by 1,978
Erlotinib in Lung Cancer — Molecular and Clinical Predictors of Outcome
Tsao, M., Sakurada, A., Cutz, J.-C., Zhu, C., Kamel‐Reid, S., Squire, J. A., Lorimer, I. A. J., Zhang, T., Liu, G., Daneshmand, M., et al. (2005) · New England Journal of Medicine · doi:10.1056/nejmoa050736 · Cited by 1,815
Principles of cancer therapy: oncogene and non-oncogene addiction
Luo, J., Solimini, N. L., & Elledge, S. J. (2009) · Cell · doi:10.1016/j.cell.2009.02.024 · Cited by 1,765
Gefitinib in Combination With Gemcitabine and Cisplatin in Advanced Non–Small-Cell Lung Cancer: A Phase III Trial—INTACT 1
Giaccone, G., Herbst, R. S., Manegold, C., Scagliotti, G. V., Rosell, R., Miller, V. A., Natale, R. B., Schiller, J. H., von Pawel, J., Pluzanska, A., et al. (2004) · Journal of Clinical Oncology · doi:10.1200/jco.2004.08.001 · Cited by 1,712
Gefitinib in Combination With Paclitaxel and Carboplatin in Advanced Non–Small-Cell Lung Cancer: A Phase III Trial—INTACT 2
Herbst, R. S., Giaccone, G., Schiller, J. H., Natale, R. B., Miller, V. A., Manegold, C., Scagliotti, G. V., Rosell, R., Oliff, I. A., Reeves, J. A., et al. (2004) · Journal of Clinical Oncology · doi:10.1200/jco.2004.07.215 · Cited by 1,701
An allosteric mechanism for activation of the kinase domain of epidermal growth factor receptor
Zhang, X., Gureasko, J., Shen, K., Cole, P. A., & Kuriyan, J. (2006) · Cell · doi:10.1016/j.cell.2006.05.013 · Cited by 1,650
The EGFR family and its ligands in human cancer
Yarden, Y. (2001) · European Journal of Cancer · doi:10.1016/s0959-8049(01)00230-1 · Cited by 1,605
MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib
Bean, J., Brennan, C., Shih, J.-Y., Riely, G., Viale, A., Wang, L., Chitale, D., Motoi, N., Szoke, J., Broderick, S., et al. (2007) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.0710370104 · Cited by 1,598
Acquired EGFR C797S mutation mediates resistance to AZD9291 in non–small cell lung cancer harboring EGFR T790M
Thress, K. S., Paweletz, C. P., Felip, E., Cho, B. C., Stetson, D., Dougherty, B., Lai, Z., Markovets, A., Vivancos, A., Kuang, Y., et al. (2015) · Nature Medicine · doi:10.1038/nm.3854 · Cited by 1,589
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)
Fukuoka, M., Wu, Y.-L., Thongprasert, S., Sunpaweravong, P., Leong, S.-S., Sriuranpong, V., Chao, T.-Y., Nakagawa, K., Chu, D.-T., Saijo, N., et al. (2011) · Journal of Clinical Oncology · doi:10.1200/jco.2010.33.4235 · Cited by 1,581
Afatinib versus cisplatin-based chemotherapy for EGFR mutation-positive lung adenocarcinoma (LUX-Lung 3 and LUX-Lung 6): analysis of overall survival data from two randomised, phase 3 trials
Yang, J. C.-H., Wu, Y.-L., Schuler, M., Sebastian, M., Popat, S., Yamamoto, N., Zhou, C., Hu, C.-P., O'Byrne, K., Feng, J., et al. (2015) · The Lancet Oncology · doi:10.1016/s1470-2045(14)71173-8 · Cited by 1,574 · cited 2×
“A post hoc analysis combining OS results from LUX-Lung 3 and LUX-Lung 6 studies (N = 709) did not show differences in overall population [44].”
TRIBUTE: a phase III trial of erlotinib hydrochloride (OSI-774) combined with carboplatin and paclitaxel chemotherapy in advanced non-small-cell lung cancer
Herbst, R. S., Prager, D., Hermann, R., Fehrenbacher, L., Johnson, B. E., Sandler, A., Kris, M. G., Tran, H. T., Klein, P., Li, X., et al. (2005) · Journal of Clinical Oncology · doi:10.1200/jco.2005.02.840 · Cited by 1,490
Dacomitinib versus gefitinib as first-line treatment for patients with EGFR-mutation-positive non-small-cell lung cancer (ARCHER 1050): a randomised, open-label, phase 3 trial
Wu, Y.-L., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Linke, R., Rosell, R., Corral, J., et al. (2017) · The Lancet Oncology · doi:10.1016/s1470-2045(17)30608-3 · Cited by 1,216
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
Park, K., Tan, E.-H., O'Byrne, K., Zhang, L., Boyer, M., Mok, T., Hirsh, V., Yang, J. C.-H., Lee, K. H., Lu, S., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30033-x · Cited by 1,183
Activating and resistance mutations of EGFR in non-small-cell lung cancer: role in clinical response to EGFR tyrosine kinase inhibitors
Gazdar, A. F. (2009) · Oncogene · doi:10.1038/onc.2009.198 · Cited by 991
Overcoming EGFR(T790M) and EGFR(C797S) resistance with mutant-selective allosteric inhibitors
Jia, Y., Yun, C., Park, E., Ercan, D., Manuia, M., Juarez, J., Xu, C., Rhee, K., Chen, T., Zhang, H., et al. (2016) · Nature · doi:10.1038/nature17960 · Cited by 954
Non-Small Cell Lung Cancer
(2016) · Elsevier eBooks · doi:10.1016/b978-0-323-37753-9.50111-0 · Cited by 859
First-Line Gefitinib in Patients With Advanced Non–Small-Cell Lung Cancer Harboring Somatic EGFR Mutations
Sequist, L. V., Martins, R. G., Spigel, D., Grunberg, S. M., Spira, A., Jänne, P. A., Joshi, V. A., McCollum, D., Evans, T. L., Muzikansky, A., et al. (2008) · Journal of Clinical Oncology · doi:10.1200/jco.2007.14.8494 · Cited by 820
Erlotinib alone or with bevacizumab as first-line therapy in patients with advanced non-squamous non-small-cell lung cancer harbouring EGFR mutations (JO25567): an open-label, randomised, multicentre, phase 2 study
Seto, T., Kato, T., Nishio, M., Goto, K., Atagi, S., Hosomi, Y., Yamamoto, N., Hida, T., Maemondo, M., Nakagawa, K., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(14)70381-x · Cited by 750
First-line erlotinib versus gemcitabine/cisplatin in patients with advanced EGFR mutation-positive non-small-cell lung cancer: analyses from the phase III, randomized, open-label, ENSURE study
Wu, Y.-L., Zhou, C., Liam, C.-K., Wu, G., Liu, X., Zhong, Z., Lu, S., Cheng, Y., Han, B., Chen, L., et al. (2015) · Annals of Oncology · doi:10.1093/annonc/mdv270 · Cited by 738
Non–Small Cell Lung Cancer
_, _. (2008) · Journal of the National Comprehensive Cancer Network · doi:10.6004/jnccn.2008.0021 · Cited by 737
Preclinical Comparison of Osimertinib with Other EGFR-TKIs in EGFR-Mutant NSCLC Brain Metastases Models, and Early Evidence of Clinical Brain Metastases Activity
Ballard, P., Yates, J. W. T., Yang, Z., Kim, D.-W., Yang, J. C.-H., Cantarini, M., Pickup, K., Jordan, A., Hickey, M., Grist, M., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-0399 · Cited by 718
HER2 Amplification: A Potential Mechanism of Acquired Resistance to EGFR Inhibition in EGFR -Mutant Lung Cancers That Lack the Second-Site EGFR T790M Mutation
Takezawa, K., Pirazzoli, V., Arcila, M. E., Nebhan, C. A., Song, X., de Stanchina, E., Ohashi, K., Janjigian, Y. Y., Spitzler, P. J., Melnick, M. A., et al. (2012) · Cancer Discovery · doi:10.1158/2159-8290.cd-12-0108 · Cited by 710
Upregulation of PD-L1 by EGFR Activation Mediates the Immune Escape in EGFR-Driven NSCLC: Implication for Optional Immune Targeted Therapy for NSCLC Patients with EGFR Mutation
Chen, N., Fang, W., Zhan, J., Hong, S., Tang, Y., Kang, S., Zhang, Y., He, X., Zhou, T., Qin, T., et al. (2015) · Journal of Thoracic Oncology · doi:10.1097/jto.0000000000000500 · Cited by 681
Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer
Sequist, L. V., Soria, J.-C., Goldman, J. W., Wakelee, H. A., Gadgeel, S. M., Varga, A., Papadimitrakopoulou, V., Solomon, B. J., Oxnard, G. R., Dziadziuszko, R., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1413654 · Cited by 665
Circulating tumour DNA profiling reveals heterogeneity of EGFR inhibitor resistance mechanisms in lung cancer patients
Chabon, J. J., Simmons, A. D., Lovejoy, A. F., Esfahani, M. S., Newman, A. M., Haringsma, H. J., Kurtz, D. M., Stehr, H., Scherer, F., Karlovich, C., et al. (2016) · Nature Communications · doi:10.1038/ncomms11815 · Cited by 657
Osimertinib for pretreated EGFR Thr790Met-positive advanced non-small-cell lung cancer (AURA2): a multicentre, open-label, single-arm, phase 2 study
Goss, G. D., Tsai, C., Shepherd, F. A., Bazhenova, L. A., Lee, J. S., Chang, G., Crinò, L., Satouchi, M., Chu, Q. S.-C., Hida, T., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30508-3 · Cited by 654
Hepatocyte growth factor induces gefitinib resistance of lung adenocarcinoma with epidermal growth factor receptor-activating mutations
Yano, S., Wang, W., Li, Q., Matsumoto, K., Sakurama, H., Nakamura, T., Ogino, H., Kakiuchi, S., Hanibuchi, M., Nishioka, Y., et al. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1643 · Cited by 643
Analysis of Epidermal Growth Factor Receptor Gene Mutation in Patients with Non–Small Cell Lung Cancer and Acquired Resistance to Gefitinib
Kosaka, T., Yatabe, Y., Endoh, H., Yoshida, K., Hida, T., Tsuboi, M., Tada, H., Kuwano, H., & Mitsudomi, T. (2006) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-0714 · Cited by 598
Brigatinib in Patients With Crizotinib-Refractory Anaplastic Lymphoma Kinase–Positive Non–Small-Cell Lung Cancer: A Randomized, Multicenter Phase II Trial
Kim, D., Tiseo, M., Ahn, M., Reckamp, K. L., Hansen, K. H., Kim, S., Huber, R. M., West, H., Groen, H. J. M., Hochmair, M. J., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2016.71.5904 · Cited by 591
The Allelic Context of the C797S Mutation Acquired upon Treatment with Third-Generation EGFR Inhibitors Impacts Sensitivity to Subsequent Treatment Strategies
Niederst, M. J., Hu, H., Mulvey, H. E., Lockerman, E. L., Garcia, A. R., Piotrowska, Z., Sequist, L. V., & Engelman, J. A. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-0560 · Cited by 583
Updated overall survival results from a randomized phase III trial comparing gefitinib with carboplatin–paclitaxel for chemo-naïve non-small cell lung cancer with sensitive EGFR gene mutations (NEJ002)
Inoue, A., Kobayashi, K., Maemondo, M., Sugawara, S., Oizumi, S., Isobe, H., Gemma, A., Harada, M., Yoshizawa, H., Kinoshita, I., et al. (2013) · Annals of Oncology · doi:10.1093/annonc/mds214 · Cited by 540
Afatinib versus gefitinib in patients with EGFR mutation-positive advanced non-small-cell lung cancer: overall survival data from the phase IIb LUX-Lung 7 trial
Paz-Ares, L., Tan, E.-H., O’Byrne, K., Zhang, L., Hirsh, V., Boyer, M., Yang, J. C.-H., Mok, T., Lee, K. H., Lu, S., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdw611 · Cited by 524
Heterogeneity Underlies the Emergence of EGFR T790 Wild-Type Clones Following Treatment of T790M-Positive Cancers with a Third-Generation EGFR Inhibitor
Piotrowska, Z., Niederst, M. J., Karlovich, C., Wakelee, H. A., Neal, J. W., Mino-Kenudson, M. A., Fulton, L. E., Hata, A. N., Lockerman, E. L., Kalsy, A., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0399 · Cited by 467
Management of Brain Metastases in Tyrosine Kinase Inhibitor–Naïve Epidermal Growth Factor Receptor–Mutant Non–Small-Cell Lung Cancer: A Retrospective Multi-Institutional Analysis
Magnuson, W. J., Lester-Coll, N. H., Wu, A. J.-C., Yang, J. T., Lockney, N. A., Gerber, N. K., Beal, K. P., Amini, A., Patil, T., Kavanagh, B. D., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2016.69.7144 · Cited by 462
Allelic dilution obscures detection of a biologically significant resistance mutation in EGFR-amplified lung cancer
Engelman, J. A., Mukohara, T., Zejnullahu, K., Lifshits, E., Borras, A. M., Gale, C.-M., Naumov, G. N., Yeap, B. Y., Jarrell, E., Sun, J., et al. (2006) · Journal of Clinical Investigation · doi:10.1172/jci28656 · Cited by 457
Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small-Cell Lung Cancers Dependent on the Epidermal Growth Factor Receptor Pathway
Nguyen, K.-S. H., Kobayashi, S., & Costa, D. B. (2009) · Clinical Lung Cancer · doi:10.3816/clc.2009.n.039 · Cited by 437
Afatinib versus erlotinib as second-line treatment of patients with advanced squamous cell carcinoma of the lung (LUX-Lung 8): an open-label randomised controlled phase 3 trial
Soria, J.-C., Felip, E., Cobo, M., Lu, S., Syrigos, K., Lee, K. H., Göker, E., Georgoulias, V., Li, W., Isla, D., et al. (2015) · The Lancet Oncology · doi:10.1016/s1470-2045(15)00006-6 · Cited by 433
Brigatinib combined with anti-EGFR antibody overcomes osimertinib resistance in EGFR-mutated non-small-cell lung cancer
Uchibori, K., Inase, N., Araki, M., Kamada, M., Sato, S., Okuno, Y., Fujita, N., & Katayama, R. (2017) · Nature Communications · doi:10.1038/ncomms14768 · Cited by 432
Icotinib versus gefitinib in previously treated advanced non-small-cell lung cancer (ICOGEN): a randomised, double-blind phase 3 non-inferiority trial
Shi, Y., Zhang, L., Liu, X., Zhou, C., Zhang, L., Zhang, S., Wang, D., Li, Q., Qin, S., Hu, C., et al. (2013) · The Lancet Oncology · doi:10.1016/s1470-2045(13)70355-3 · Cited by 425
Gefitinib plus chemotherapy versus placebo plus chemotherapy in EGFR-mutation-positive non-small-cell lung cancer after progression on first-line gefitinib (IMPRESS): a phase 3 randomised trial
Soria, J.-C., Wu, Y.-L., Nakagawa, K., Kim, S.-W., Yang, J.-J., Ahn, M.-J., Wang, J., Yang, J. C.-H., Lu, Y., Atagi, S., et al. (2015) · The Lancet Oncology · doi:10.1016/s1470-2045(15)00121-7 · Cited by 413 · cited 1×
“This explored gefitinib treatment beyond progression in addition to platinum-based doublet chemotherapy versus chemotherapy alone after disease progression to gefitinib in 265 patients not previously exposed to chemotherapy [119].”
First-line gefitinib in Caucasian EGFR mutation-positive NSCLC patients: a phase-IV, open-label, single-arm study
Douillard, J.-Y., Ostoros, G., Cobo, M., Ciuleanu, T., McCormack, R., Webster, A., & Milenkova, T. (2014) · British Journal of Cancer · doi:10.1038/bjc.2013.721 · Cited by 412
FAS and NF-κB signalling modulate dependence of lung cancers on mutant EGFR
Bivona, T. G., Hieronymus, H., Parker, J., Chang, K., Taron, M., Rosell, R., Moonsamy, P., Dahlman, K., Miller, V. A., Costa, C., et al. (2011) · Nature · doi:10.1038/nature09870 · Cited by 396
Phase II trial of erlotinib plus concurrent whole-brain radiation therapy for patients with brain metastases from non-small-cell lung cancer
Welsh, J. W., Komaki, R., Amini, A., Munsell, M. F., Unger, W., Allen, P. K., Chang, J. Y., Wefel, J. S., McGovern, S. L., Garland, L. L., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2011.40.1174 · Cited by 395
Implementing multiplexed genotyping of non-small-cell lung cancers into routine clinical practice
Sequist, L. V., Heist, R. S., Shaw, A. T., Fidias, P., Rosovsky, R., Temel, J. S., Lennes, I. T., Digumarthy, S., Waltman, B. A., Bast, E., et al. (2011) · Annals of Oncology · doi:10.1093/annonc/mdr489 · Cited by 370
EGFR Mutations and Resistance to Irreversible Pyrimidine-Based EGFR Inhibitors
Ercan, D., Choi, H. G., Yun, C.-H., Capelletti, M., Xie, T., Eck, M. J., Gray, N. S., & Jänne, P. A. (2015) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-14-2789 · Cited by 368
First-Line Afatinib versus Chemotherapy in Patients with Non–Small Cell Lung Cancer and Common Epidermal Growth Factor Receptor Gene Mutations and Brain Metastases
Schuler, M., Wu, Y.-L., Hirsh, V., O’Byrne, K., Yamamoto, N., Mok, T., Popat, S., Sequist, L. V., Massey, D., Zazulina, V., et al. (2016) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2015.11.014 · Cited by 361
Activity and safety of brigatinib in ALK-rearranged non-small-cell lung cancer and other malignancies: a single-arm, open-label, phase 1/2 trial
Gettinger, S. N., Bazhenova, L. A., Langer, C. J., Salgia, R., Gold, K. A., Rosell, R., Shaw, A. T., Weiss, G. J., Tugnait, M., Narasimhan, N. I., et al. (2016) · The Lancet Oncology · doi:10.1016/s1470-2045(16)30392-8 · Cited by 359
Non–Small Cell Lung Cancer
Ettinger, D. S., Akerley, W., Borghaei, H., Chang, A. C., Cheney, R. T., Chirieac, L. R., D’Amico, T. A., Demmy, T. L., Ganti, A. K., Govindan, R., et al. (2012) · Journal of the National Comprehensive Cancer Network · doi:10.6004/jnccn.2012.0130 · Cited by 352
Gefitinib in patients with brain metastases from non-small-cell lung cancer: a prospective trial
Ceresoli, G. L., Cappuzzo, F., Gregorc, V., Bartolini, S., Crinò, L., & Villa, E. (2004) · Annals of Oncology · doi:10.1093/annonc/mdh276 · Cited by 351
EGF receptor ligands: recent advances
Singh, B., Carpenter, G. F., & Coffey, R. J. (2016) · F1000Research · doi:10.12688/f1000research.9025.1 · Cited by 330
Symptom Control and Quality of Life in LUX-Lung 3: A Phase III Study of Afatinib or Cisplatin/Pemetrexed in Patients With Advanced Lung Adenocarcinoma With EGFR Mutations
Yang, J. C., Hirsh, V., Schüler, M., Yamamoto, N., O'Byrne, K. J., Mok, T. S. K., Zazulina, V., Shahidi, M., Lungershausen, J., Massey, D., et al. (2013) · Journal of Clinical Oncology · doi:10.1200/jco.2012.46.1764 · Cited by 330
Efficacy of epidermal growth factor receptor tyrosine kinase inhibitors for brain metastasis in non-small cell lung cancer patients harboring either exon 19 or 21 mutation
Park, S. J., Kim, H. T., Lee, D., Kim, K. P., Kim, S.-W., Suh, C. H., & Lee, J. S. (2012) · Lung Cancer · doi:10.1016/j.lungcan.2012.05.092 · Cited by 324
Brain metastases from lung cancer responding to erlotinib: the importance of EGFR mutation
Porta, R., Sánchez-Torres, J. M., Paz-Ares, L., Massutí, B., Reguart, N., Mayo, C., Lianes, P., Queralt, C., Guillem, V., Salinas, P., et al. (2011) · European Respiratory Journal · doi:10.1183/09031936.00195609 · Cited by 316
Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer
Wang, S., Cang, S., & Liu, D. (2016) · Journal of Hematology & Oncology · doi:10.1186/s13045-016-0268-z · Cited by 312
Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models
Eberlein, C. A., Stetson, D., Markovets, A. A., Al-Kadhimi, K. J., Lai, Z., Fisher, P. R., Meador, C. B., Spitzler, P. J., Ichihara, E., Ross, S. J., et al. (2015) · Cancer Research · doi:10.1158/0008-5472.can-14-3167 · Cited by 310
Intercalated combination of chemotherapy and erlotinib for patients with advanced stage non-small-cell lung cancer (FASTACT-2): a randomised, double-blind trial
Wu, Y.-L. L. C., Lee, J. S., Thongprasert, S., Yu, C., Zhang, L., Ladrera, G., Srimuninnimit, V., Sriuranpong, V., Sandoval-Tan, J., Zhu, Y., et al. (2013) · The Lancet Oncology · doi:10.1016/s1470-2045(13)70254-7 · Cited by 302
First-line icotinib versus cisplatin/pemetrexed plus pemetrexed maintenance therapy for patients with advancedEGFR mutation-positive lung adenocarcinoma (CONVINCE): a phase 3, open-label, randomized study
Shi, Y. K., Wang, L., Han, B. H., Li, W., Yu, P., Liu, Y. P., Ding, C. M., Song, X., Ma, Z. Y., Ren, X. L., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx359 · Cited by 287
Structure- and Reactivity-Based Development of Covalent Inhibitors of the Activating and Gatekeeper Mutant Forms of the Epidermal Growth Factor Receptor (EGFR)
Ward, R. A., Anderton, M. J., Ashton, S., Bethel, P. A., Box, M., Butterworth, S., Colclough, N., Chorley, C. G., Chuaqui, C., Cross, D. A. E., et al. (2013) · Journal of Medicinal Chemistry · doi:10.1021/jm400822z · Cited by 279
A phase 3 trial of whole brain radiation therapy and stereotactic radiosurgery alone versus WBRT and SRS with temozolomide or erlotinib for non-small cell lung cancer and 1 to 3 brain metastases: Radiation Therapy Oncology Group 0320
Sperduto, P. W., Wang, M., Robins, H. I., Schell, M. C., Werner-Wasik, M., Komaki, R., Souhami, L., Buyyounouski, M. K., Khuntia, D., Demas, W., et al. (2013) · International Journal of Radiation Oncology*Biology*Physics · doi:10.1016/j.ijrobp.2012.11.042 · Cited by 274
Randomized Phase II Study of Dacomitinib (PF-00299804), an Irreversible Pan–Human Epidermal Growth Factor Receptor Inhibitor, Versus Erlotinib in Patients With Advanced Non–Small-Cell Lung Cancer
Ramalingam, S. S., Blackhall, F. H., Krzakowski, M. J., Barrios, C. H., Park, K., Bover, I., Heo, D. S., Rosell, R., Talbot, D. C., Frank, R. C., et al. (2012) · Journal of Clinical Oncology · doi:10.1200/jco.2011.40.9433 · Cited by 263
First-line treatment of advanced epidermal growth factor receptor (EGFR) mutation positive non-squamous non-small cell lung cancer
Greenhalgh, J., Dwan, K. M., Boland, A., Bates, V., Vecchio, F., Dundar, Y., Jain, P., & Green, J. A. (2016) · Cochrane Database of Systematic Reviews · doi:10.1002/14651858.cd010383.pub2 · Cited by 248
Erlotinib as second-line treatment in patients with advanced non-small-cell lung cancer and asymptomatic brain metastases: a phase II study (CTONG–0803)
Wu, Y.-L. L. C., Zhou, C., Cheng, Y., Lü, S., Chen, G.-Y., Huang, C., Huang, Y., Yan, H., Ren, S., Liu, Y.-B., et al. (2012) · Annals of Oncology · doi:10.1093/annonc/mds529 · Cited by 236
Combined EGFR/MEK Inhibition Prevents the Emergence of Resistance in EGFR -Mutant Lung Cancer
Tricker, E. M., Xu, C., Uddin, S., Capelletti, M., Ercan, D., Ogino, A., Pratilas, C. A., Rosen, N. X., Gray, N. S., Wong, K., et al. (2015) · Cancer Discovery · doi:10.1158/2159-8290.cd-15-0063 · Cited by 220
Hostile, Hypoxia–A2-Adenosinergic Tumor Biology as the Next Barrier to Overcome for Tumor Immunologists
Sitkovsky, M. V., Hatfield, S., Abbott, R., Belikoff, B., Lukashev, D., & Ohta, A. (2014) · Cancer Immunology Research · doi:10.1158/2326-6066.cir-14-0075 · Cited by 215
Schedule-Dependent Cytotoxic Synergism of Pemetrexed and Erlotinib in Human Non–Small Cell Lung Cancer Cells
Li, T., Ling, Y., Goldman, I. D., & Perez-Soler, R. (2007) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-06-2923 · Cited by 214
Poor response to erlotinib in patients with tumors containing baseline EGFR T790M mutations found by routine clinical molecular testing
Yu, H. A., Arcila, M. E., Hellmann, M. D., Kris, M. G., Ladanyi, M., & Riely, G. J. (2014) · Annals of Oncology · doi:10.1093/annonc/mdt573 · Cited by 206
Third-generation epidermal growth factor receptor-tyrosine kinase inhibitors in T790M-positive non-small cell lung cancer: review on emerged mechanisms of resistance
Minari, R., Bordi, P., & Tiseo, M. (2016) · Translational Lung Cancer Research · doi:10.21037/tlcr.2016.12.02 · Cited by 186
Clinical and molecular evidences of epithelial to mesenchymal transition in acquired resistance to EGFR-TKIs
Chung, J.-H., Rho, J. K., Xu, X., Lee, J. S., Yoon, H. I., Lee, C. T., Choi, Y. J., Kim, H.-R., Kim, C. H., & Lee, J. C. (2010) · Lung Cancer · doi:10.1016/j.lungcan.2010.11.011 · Cited by 186
Pooled safety analysis of EGFR-TKI treatment for EGFR mutation-positive non-small cell lung cancer
Takeda, M., Okamoto, I., & Nakagawa, K. (2015) · Lung Cancer · doi:10.1016/j.lungcan.2015.01.026 · Cited by 182
Randomized Phase II Trial of Gefitinib With and Without Pemetrexed as First-Line Therapy in Patients With Advanced Nonsquamous Non–Small-Cell Lung Cancer With Activating Epidermal Growth Factor Receptor Mutations
Cheng, Y., Murakami, H., Yang, P., He, J., Nakagawa, K., Kang, J. H., Kim, J.-H., Wang, X., Enatsu, S., Puri, T., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.66.9218 · Cited by 182
Gefitinib Plus Chemotherapy Versus Chemotherapy in Epidermal Growth Factor Receptor Mutation–Positive Non–Small-Cell Lung Cancer Resistant to First-Line Gefitinib (IMPRESS): Overall Survival and Biomarker Analyses
Mok, T. S. K., Kim, S., Wu, Y.-L. L. C., Nakagawa, K., Yang, J., Ahn, M., Wang, J., Yang, J. C., Lü, Y., Atagi, S., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.73.9250 · Cited by 179
Evaluation of Biologic End Points and Pharmacokinetics in Patients With Metastatic Breast Cancer After Treatment With Erlotinib, an Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor
Tan, A. R., Yang, X., Hewitt, S. M., Berman, A. W., Lepper, E. R., Sparreboom, A., Parr, A. L., Figg, W. D., Chow, C., Steinberg, S. M., et al. (2004) · Journal of Clinical Oncology · doi:10.1200/jco.2004.08.189 · Cited by 176
A phase III randomised controlled trial of erlotinib vs gefitinib in advanced non-small cell lung cancer with EGFR mutations
Yang, J. J., Zhou, Q., Yan, H. H., Zhang, X. C., Chen, H. J., Tu, H. Y., Wang, Z., Xu, C. R., Su, J., Wang, B. C., et al. (2017) · British Journal of Cancer · doi:10.1038/bjc.2016.456 · Cited by 175
Prognostic impact of CD73 and A2A adenosine receptor expression in non-small-cell lung cancer
Inoue, Y., Yoshimura, K., Kurabe, N., Kahyo, T., Kawase, A., Tanahashi, M., Ogawa, H., Inui, N., Funai, K., Shinmura, K., et al. (2017) · Oncotarget · doi:10.18632/oncotarget.14434 · Cited by 172
Olmutinib: First Global Approval
Kim, E. S. (2016) · Drugs · doi:10.1007/s40265-016-0606-z · Cited by 170
Recent updates on third generation EGFR inhibitors and emergence of fourth generation EGFR inhibitors to combat C797S resistance
Patel, H., Pawara, R., Ansari, A., & Surana, S. (2017) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2017.05.027 · Cited by 170
EGFR TKI combination with immunotherapy in non-small cell lung cancer
Ahn, M., Sun, J., Lee, S., Ahn, J. S., & Park, K. (2017) · Expert Opinion on Drug Safety · doi:10.1080/14740338.2017.1300656 · Cited by 170
Osimertinib benefit inEGFR-mutant NSCLC patients withT790M-mutation detected by circulating tumour DNA
Remón, J., Caramella, C., Jovelet, C., Lacroix, L., Lawson, A. R. J., Smalley, S., Howarth, K., Gale, D. G., Green, E., Plagnol, V., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx017 · Cited by 167
EGFR Mutation Heterogeneity and the Mixed Response to EGFR Tyrosine Kinase Inhibitors of Lung Adenocarcinomas
Chen, Z.-Y., Zhong, W.-Z., Zhang, X.-C., Su, J., Yang, X.-N., Chen, Z.-H., Yang, J.-J., Zhou, Q., Yan, H.-H., An, S.-J., et al. (2012) · The Oncologist · doi:10.1634/theoncologist.2011-0385 · Cited by 165
Randomized Phase III Study Comparing Gefitinib With Erlotinib in Patients With Previously Treated Advanced Lung Adenocarcinoma: WJOG 5108L
Urata, Y., Katakami, N., Morita, S., Kaji, R., Yoshioka, H., Seto, T., Satouchi, M., Iwamoto, Y., Kanehara, M., Fujimoto, D., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2015.63.4154 · Cited by 159
Oncogenic Activity of Epidermal Growth Factor Receptor Kinase Mutant Alleles Is Enhanced by the T790M Drug Resistance Mutation
Godin-Heymann, N., Bryant, I., Rivera, M. N., Ulkus, L., Bell, D. W., Riese, D. J., Settleman, J. E., & Haber, D. A. (2007) · Cancer Research · doi:10.1158/0008-5472.can-06-4625 · Cited by 157
Binding mode of the breakthrough inhibitor AZD9291 to epidermal growth factor receptor revealed
Yosaatmadja, Y., Silva, S., Dickson, J. M. J. J., Patterson, A. V., Smaill, J. B., Flanagan, J. U., McKeage, M. J., & Squire, C. J. (2015) · Journal of Structural Biology · doi:10.1016/j.jsb.2015.10.018 · Cited by 150
Gefitinib as palliative therapy for lung adenocarcinoma metastatic to the brain
Wu, C., Li, Y. L., Wang, Z. M., Li, Z., Zhang, T. X., & Wei, Z. (2007) · Lung Cancer · doi:10.1016/j.lungcan.2007.03.011 · Cited by 149
Dacomitinib versus erlotinib in patients with advanced-stage, previously treated non-small-cell lung cancer (ARCHER 1009): a randomised, double-blind, phase 3 trial
Ramalingam, S. S., Janne, P. A., Mok, T. S. K., O'Byrne, K. J., Boyer, M. J., von Pawel, J., Płużański, A., Shtivelband, M. I., Docampo, L. I., Bennouna, J., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(14)70452-8 · Cited by 143
Dacomitinib compared with placebo in pretreated patients with advanced or metastatic non-small-cell lung cancer (NCIC CTG BR.26): a double-blind, randomised, phase 3 trial
Ellis, P. M., Shepherd, F. A., Millward, M. J., Perrone, F., Seymour, L., Liu, G., Sun, S. B., Cho, B. C., Morabito, A., Leighl, N. B., et al. (2014) · The Lancet Oncology · doi:10.1016/s1470-2045(14)70472-3 · Cited by 135
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are effective for leptomeningeal metastasis from non-small cell lung cancer patients with sensitive EGFR mutation or other predictive factors of good response for EGFR TKI
Yi, H. G., Kim, H. J., Kim, Y. J., Han, S., Oh, D., Lee, S., Kim, D., Im, S., Kim, T., Kim, C. S., et al. (2008) · Lung Cancer · doi:10.1016/j.lungcan.2008.10.016 · Cited by 125
The Role of Erlotinib (Tarceva, OSI 774) in the Treatment of Non-Small Cell Lung Cancer
Perez-Soler, R. (2004) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-040017 · Cited by 110
Uncommon Epidermal Growth Factor Receptor mutations in non-small cell lung cancer and their mechanisms of EGFR tyrosine kinase inhibitors sensitivity and resistance
Massarelli, E., Johnson, F. M., Erickson, H. S., Wistuba, I. I., & Papadimitrakopoulou, V. (2013) · Lung Cancer · doi:10.1016/j.lungcan.2013.01.018 · Cited by 110
CYP3A Phenotyping Approach to Predict Systemic Exposure to EGFR Tyrosine Kinase Inhibitors
Li, J., Karlsson, M. O., Brahmer, J. R., Spitz, A. N., Zhao, M., Hidalgo, M. M., & Baker, S. D. (2006) · JNCI Journal of the National Cancer Institute · doi:10.1093/jnci/djj466 · Cited by 106
CD73 Promotes Resistance to HER2/ErbB2 Antibody Therapy
Turcotte, M., Allard, D., Mittal, D., Barèche, Y., Buisseret, L., José, V., Pommey, S., Delisle, V., Loi, S., Joensuu, H., et al. (2017) · Cancer Research · doi:10.1158/0008-5472.can-17-0707 · Cited by 106
Impact of Deferring Radiation Therapy in Patients With Epidermal Growth Factor Receptor–Mutant Non-Small Cell Lung Cancer Who Develop Brain Metastases
Magnuson, W. J., Yeung, J. T., Guillod, P., Gettinger, S. N., Yu, J. B., & Chiang, V. (2016) · International Journal of Radiation Oncology*Biology*Physics · doi:10.1016/j.ijrobp.2016.01.037 · Cited by 100
Metastatic brain tumors from non-small cell lung cancer with EGFR mutations: Distinguishing influence of exon 19 deletion on radiographic features
Sekine, A., Kato, T., Hagiwara, E., Shinohara, T., Komagata, T., Iwasawa, T., Satoh, H., Tamura, K., Kasamatsu, T., Hayashihara, K., et al. (2012) · Lung Cancer · doi:10.1016/j.lungcan.2011.12.017 · Cited by 97
Erlotinib versus radiation therapy for brain metastases in patients with EGFR-mutant lung adenocarcinoma
Gerber, N. K., Yamada, Y., Rimner, A., Shi, W., Riely, G. J., Beal, K., Yu, H. A., Chan, T. A., Zhang, Z., & Wu, A. J. (2014) · International Journal of Radiation Oncology*Biology*Physics · doi:10.1016/j.ijrobp.2014.02.022 · Cited by 96
Determining EGFR-TKI sensitivity of G719X and other uncommon EGFR mutations in non-small cell lung cancer: Perplexity and solution
Li, K., Yang, M., Liang, N., & Li, S. (2017) · Oncology Reports · doi:10.3892/or.2017.5409 · Cited by 95
Osimertinib (AZD9291)—a science-driven, collaborative approach to rapid drug design and development
Yver, A. (2016) · Annals of Oncology · doi:10.1093/annonc/mdw129 · Cited by 94
Deregulated EGFR Signaling during Lung Cancer Progression: Mutations, Amplicons, and Autocrine Loops
Gazdar, A. F., & Minna, J. D. (2008) · Cancer Prevention Research · doi:10.1158/1940-6207.capr-08-0080 · Cited by 88
Expression of selected gene for acquired drug resistance to EGFR-TKI in lung adenocarcinoma
Uramoto, H., Shimokawa, H., Hanagiri, T., Kuwano, M., & Ono, M. (2011) · Lung Cancer · doi:10.1016/j.lungcan.2011.01.008 · Cited by 83
Update to Rociletinib Data with the RECIST Confirmed Response Rate
Sequist, L. V. D., Soria, J., & Camidge, D. R. (2016) · New England Journal of Medicine · doi:10.1056/nejmc1602688 · Cited by 77
LBA1_PR: Osimertinib as first-line treatment for EGFR mutation-positive advanced NSCLC: updated efficacy and safety results from two Phase I expansion cohorts
Ramalingam, S. S., Yang, J. C.-H., Lee, C. K., Kurata, T., Kim, D.-W., John, T., Nogami, N., Ohe, Y., & Janne, P. A. (2016) · Journal of Thoracic Oncology · doi:10.1016/s1556-0864(16)30324-0 · Cited by 68
CNS response to osimertinib in patients (pts) with T790M-positive advanced NSCLC: Data from a randomized phase III trial (AURA3).
Mok, T. S. K., Ahn, M., Han, J., Kang, J. H., Katakami, N., Kim, H. R., Hodge, R. A., Ghiorghiu, D. C., Cantarini, M., Wu, Y.-L. L. C., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.9005 · Cited by 63
Third-Generation Tyrosine Kinase Inhibitors Targeting Epidermal Growth Factor Receptor Mutations in Non-Small Cell Lung Cancer
Barnes, T. A., O'Kane, G. M., Vincent, M. D., & Leighl, N. B. (2017) · Frontiers in Oncology · doi:10.3389/fonc.2017.00113 · Cited by 61
Rociletinib in EGFR-Mutated Non–Small-Cell Lung Cancer
(2015) · New England Journal of Medicine · doi:10.1056/nejmc1506831 · Cited by 61
Polymorphisms of CYP2D6 Gene and Gefitinib-Induced Hepatotoxicity
Takimoto, T., Kijima, T., Otani, Y., Nonen, S., Namba, Y., Mori, M., Yokota, S., Minami, S., Komuta, K., Uchida, J., et al. (2013) · Clinical Lung Cancer · doi:10.1016/j.cllc.2013.03.003 · Cited by 59
Is There a Common Etiology for the Rising Incidence of and Decreasing Survival with Adenocarcinoma of the Lung?
Janssen-Heijnen, M. L. G., Coebergh, J. W. W., Klinkhamer, P. J. J. M., Schipper, R. M., Splinter, T. A. W., & Mooi, A. W. J. (2001) · Epidemiology · doi:10.1097/00001648-200103000-00020 · Cited by 57
Dacomitinib versus erlotinib in patients with EGFR-mutated advanced nonsmall-cell lung cancer (NSCLC): pooled subset analyses from two randomized trials
Ramalingam, S. S., O'Byrne, K. J., Boyer, M. J., Mok, T. S. K., Janne, P. A., Zhang, H., Liang, J. J., Taylor, I. W., Sbar, E. I., & Paz-Ares, L. (2016) · Annals of Oncology · doi:10.1093/annonc/mdv593 · Cited by 57
Potential prognostic biomarker CD73 regulates epidermal growth factor receptor expression in human breast cancer
Zhi, X., Wang, Y., Yu, J., Yu, J., Zhang, L., Yin, L., & Zhou, P. (2012) · IUBMB Life · doi:10.1002/iub.1086 · Cited by 54
Optimal management of EGFR -mutant non-small cell lung cancer with disease progression on first-line tyrosine kinase inhibitor therapy
Liao, B.-C., Lin, C., Lee, J., & Yang, J. C. (2017) · Lung Cancer · doi:10.1016/j.lungcan.2017.05.009 · Cited by 48
Anti-CD73 immunotherapy: A viable way to reprogram the tumor microenvironment
Antonioli, L., Blandizzi, C., Malavasi, F., Ferrari, D., & Haskó, G. (2016) · OncoImmunology · doi:10.1080/2162402x.2016.1216292 · Cited by 47
Carcinomatous meningitis from non-small-cell lung cancer responding to gefitinib
Sakai, M., Ishikawa, S., Ito, H., Ozawa, Y., Yamamoto, T., Onizuka, M., & Sakakibara, Y. (2006) · International Journal of Clinical Oncology · doi:10.1007/s10147-005-0558-x · Cited by 46
BI 1482694 (HM61713), an EGFR mutant-specific inhibitor, in T790M+ NSCLC: Efficacy and safety at the RP2D.
Park, K., Lee, J.-S., Lee, K. H., Kim, J.-H., Cho, B. C., Min, Y. J., Choi, Y., Han, J., Kim, B.-S., Kim, J.-S., et al. (2016) · Journal of Clinical Oncology · doi:10.1200/jco.2016.34.15_suppl.9055 · Cited by 43
PD-1 Axis Inhibitors in EGFR- and ALK-Driven Lung Cancer: Lost Cause?
Gettinger, S. N., & Politi, K. A. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-16-1401 · Cited by 40
Complete clearance of plasma EGFR mutations as a predictor of outcome on osimertinib in the AURA trial.
Thress, K. S., Markovets, A. A., Barrett, J. C., Chmielecki, J., Goldberg, S. B., Shepherd, F. A., Vowler, S. L., & Oxnard, G. R. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.9018 · Cited by 40
EGFR Mutation Status and First-Line Treatment in Patients with Stage III/IV Non–Small Cell Lung Cancer in Germany: An Observational Study
Schuette, W., Schirmacher, P., Eberhardt, W., Fischer, J. R., von der Schulenburg, J.-M. G., Mezger, J., Schumann, C., Serke, M. H., Zaun, S., Dietel, M., et al. (2015) · Cancer Epidemiology Biomarkers & Prevention · doi:10.1158/1055-9965.epi-14-1149 · Cited by 38
Lower gefitinib dose led to earlier resistance acquisition before emergence of T790M mutation in epidermal growth factor receptor‐mutated lung cancer model
Hayakawa, H., Ichihara, E., Ohashi, K., Ninomiya, T., Yasugi, M., Takata, S., Sakai, K., Matsumoto, K., Takigawa, N., Tanimoto, M., et al. (2013) · Cancer Science · doi:10.1111/cas.12284 · Cited by 36
Osimertinib vs standard of care (SoC) EGFR-TKI as first-line therapy in patients (pts) with EGFRm advanced NSCLC: FLAURA
Ramalingam, S., Reungwetwattana, T., Chewaskulyong, B., Dechaphunkul, A., Lee, K. H., Imamura, F., Nogami, N., Ohe, Y., Cheng, Y., Cho, B. C., et al. (2017) · Annals of Oncology · doi:10.1093/annonc/mdx440.050 · Cited by 36
Dacomitinib versus gefitinib for the first-line treatment of advanced EGFR mutation positive non-small cell lung cancer (ARCHER 1050): A randomized, open-label phase III trial.
Mok, T. S. K., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Rosell, R., Jaime, J. C., Migliorino, M. R., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.18_suppl.lba9007 · Cited by 33
EGFR mutations in circulating tumour DNA
Rosell, R., Molina‐Vila, M. Á., & Serrano, M. J. (2012) · The Lancet Oncology · doi:10.1016/s1470-2045(12)70369-8 · Cited by 29
Toxicity profile of epidermal growth factor receptor tyrosine kinase inhibitors in patients with epidermal growth factor receptor gene mutation-positive lung cancer
Takeda, M., & Nakagawa, K. (2016) · Molecular and Clinical Oncology · doi:10.3892/mco.2016.1099 · Cited by 29
Second-line Treatment of Non-Small Cell Lung Cancer: Focus on the Clinical Development of Dacomitinib
Zugazagoitia, J., Díaz, A., Jiménez, E., Nuñez, J. A., Iglesias, L., Ponce-Aix, S., & Paz-Ares, L. G. (2017) · Frontiers in Medicine · doi:10.3389/fmed.2017.00036 · Cited by 12
Self-citation
P1.04-001 Osimertinib with Ramucirumab or Necitumumab in Advanced T790M-positive EGFR-Mutant NSCLC: Preliminary Ph1 Study Results
Yu, H. A., Planchard, D., Yang, J. C.-H., Lee, K. H., Garrido, P., Park, K., Kim, J. H., Lee, D., He, S., Wolff, K., et al. (2017) · Journal of Thoracic Oncology · doi:10.1016/j.jtho.2017.09.860 · Cited by 8
Dacomitinib versus gefitinib for the first-line treatment of advanced EGFR mutation positive non-small cell lung cancer (ARCHER 1050): A randomized, open-label phase III trial.
Mok, T. S. K., Cheng, Y., Zhou, X., Lee, K. H., Nakagawa, K., Niho, S., Tsuji, F., Rosell, R., Jaime, J. C., Migliorino, M. R., et al. (2017) · Journal of Clinical Oncology · doi:10.1200/jco.2017.35.15_suppl.lba9007 · Cited by 7
Abstract 4112: Overgrowth of competing resistance mechanisms, such as an acquired KRAS mutation, underlies a poor prognosis subtype of acquired resistance to osimertinib in T790M-positive NSCLC
Oxnard, G. R., Hu, Y., Tracy, P. D., Feeney, N. B., Paweletz, C. P., Thress, K. S., & Janne, P. A. (2017) · Cancer Research · doi:10.1158/1538-7445.am2017-4112 · Cited by 4

Sorted by citations

Non‐small cell lung cancer in China
Chen, P., Liu, Y., Wen, Y., & Zhou, C. (2022) · 癌症：英文版 · doi:10.1002/cac2.12359 · Cited by 694
Adverse effects of tyrosine kinase inhibitors in cancer therapy: pathophysiology, mechanisms and clinical management
Sunder, S. S., Sharma, U. C., & Pokharel, S. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01469-6 · Cited by 572
“The AURA3 Randomized Phase III Study (Osimertinib vs PlatinumPemetrexed) and the FLAURA trial (osimertinib vs first-generation EGFR-TKI) in EGFR-Mutated Advanced non-small cell lung cancers (NSCLC) reported the frequency of LVD at 5% and 10%, respectively.(43) Paradoxically, a larger population study with a 2-year fol…”
BackgroundInfluential
EGFR Blockade Reverts Resistance to KRASG12C Inhibition in Colorectal Cancer.
Amodio, V., Yaeger, R., Arcella, P., Cancelliere, C., Lamba, S., Lorenzato, A., Arena, S., Montone, M., Mussolin, B., Bian, Y., et al. (2020) · Cancer Discovery · doi:10.1158/2159-8290.cd-20-0187 · Cited by 504
“The anti-EGFR antibodies cetuximab and panitumumab are approved for the treatment of RAS/RAF wild type CRC(34, 35), while EGFR tyrosine kinase inhibitors (TKI) are approved for the treatment of EGFR mutant lung cancer(36).”
Background
Receptor Tyrosine Kinase-Targeted Cancer Therapy
Yamaoka, T., Kusumoto, S., Ando, K., Ohba, M., & Ohmori, T. (2018) · International Journal of Molecular Sciences · doi:10.3390/ijms19113491 · Cited by 297
“Several EGFR TKIs are currently available for cancer treatment [85].”
Background
Therapeutic advances of targeting receptor tyrosine kinases in cancer
Tomuleasa, C., Tigu, A.-B., Munteanu, R. A., Moldovan, C. S., Kegyes, D., Onaciu, A., Gulei, D., Ghiaur, G., Einsele, H., & Croce, C. M. (2024) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-024-01899-w · Cited by 307

See all 109

Authors: Díaz-Serrano, A., Gella, P., Jiménez, E., Zugazagoitia, J., & Paz-Ares Rodríguez, L.
Affiliations: Research Institute Hospital 12 de Octubre (ES)
Yale Cancer Center (US)
ORCID: Díaz-Serrano, Asunción
Venue: Drugs
Publisher: Springer Science and Business Media LLC
Published: 2018-06
Volume: 78
Issue: 9
Pages: 893-911
ISSN: 0012-6667 (ISSN-L)
1179-1950
DOI: 10.1007/s40265-018-0916-4
OpenAlex: W2809285875
Semantic Scholar: 3bfe42a82922c9b186444aa869784e8c1be89711
Cited by: 108
References: 153
Citations by year: 2026: 9 · 2025: 12 · 2024: 19 · 2023: 9 · 2022: 17 · 2021: 12 · 2020: 10 · 2019: 15 · 2018: 4
FWCI: 1.82
Type: journal article
Language: en
Open access: closed
Licence: www.springer.com/tdm (tdm)
Locations: Drugs (publishedVersion)
PubMed (publishedVersion)
BURJC Digital (King Juan Carlos University) (submittedVersion)
Hispana (submittedVersion)
Funders: Consejería de Educación, Juventud y Deporte, Comunidad de Madrid (ES) and European Social Fund (PEJD16/2016/BMD-2715)
Instituto de Salud Carlos III (CM15/00196)
Sistema Nacional de Salud
Universidad Complutense de Madrid
Topics: Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Treatments and Mutations
Health Sciences › Medicine › Oncology › HER2/EGFR in Cancer Research
Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Lung Cancer Diagnosis and Treatment
Keywords: EGFR-mutant non-small cell lung cancer, EGFR tyrosine kinase inhibitors, osimertinib, T790M mutation, acquired drug resistance, MET amplification, HER2 amplification, immunotherapy, FLAURA trial, central nervous system metastasis
MeSH terms: Acrylamides, Aniline Compounds, Antineoplastic Agents, Carcinoma, Non-Small-Cell Lung, Humans, Indoles, Lung Neoplasms, Piperazines, Pyrimidines, Disease Progression, Disease-Free Survival, Drug Resistance, Neoplasm, Protein Kinase Inhibitors, Molecular Targeted Therapy, ErbB Receptors

About these checks

Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.

Statistics and arithmetic are recomputed, not judged.

Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.

What counts as a claim ›How we measure confidence ›How we check this ›

Are you an author, or do you see a problem with this page? Request a review

Targeting EGFR in Lung Cancer: Current Standards and Developments

Abstract

Overview

Integrity signals

Verification

Claims the paper makes

Claims other papers make about this one

Citations

Cites

Cited by

Related

Metadata

Record

About these checks