Molecular mechanisms of acquired resistance to third-generation EGFR-TKIs in EGFR T790M-mutant lung cancer
Charles Ricordel,Charles Ricordel,Charles Ricordel,Luc Friboulet,Francesco Facchinetti,J-C. Soria,J-C. Soria +6 more
TLDR
The heterogeneity of the mechanisms that a tumour can develop to evade therapeutic pressure is revealed, as well as strategies currently being tested in clinical trials are discussed in light of these findings.About:
This article is published in Annals of Oncology.The article was published on 2018-01-01 and is currently open access. It has received 94 citations till now. The article focuses on the topics: EGFR inhibitors & Osimertinib.read more
Citations
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Journal ArticleDOI
Resistance mechanisms to osimertinib in EGFR-mutated non-small cell lung cancer.
Alessandro Leonetti,Sugandhi Sharma,Roberta Minari,Paola Perego,Elisa Giovannetti,Elisa Giovannetti,Marcello Tiseo +6 more
TL;DR: The molecular mechanisms of resistance to osimertinib in patients with advanced EGFR-mutated NSCLC, including MET/HER2 amplification, activation of the RAS–mitogen-activated protein kinase (MAPK) or RAS-phosphatidylinositol 3-kinase (PI3K) pathways, novel fusion events and histological/phenotypic transformation are summarized.
Journal ArticleDOI
Making the first move in EGFR-driven or ALK-driven NSCLC: first-generation or next-generation TKI?
Gonzalo Recondo,Francesco Facchinetti,Ken A. Olaussen,Benjamin Besse,Benjamin Besse,Luc Friboulet +5 more
TL;DR: Preclinical and clinical evidence supporting both treatment strategies — the ‘historical’ sequential treatment strategy and the use of next-generation TKIs — as frontline therapies are described and the suitability of both strategies for patients with EGFR-driven or ALK-driven NSCLC is discussed.
Journal ArticleDOI
Trends in kinase drug discovery: targets, indications and inhibitor design.
Misty M. Attwood,Doriano Fabbro,Aleksandr V. Sokolov,Stefan Knapp,Stefan Knapp,Helgi B. Schiöth,Helgi B. Schiöth +6 more
TL;DR: In this paper, the authors analyzed the landscape of approved and investigational therapies that target kinases and trends within it, including the most popular targets of kinase inhibitors and their expanding range of indications.
Journal ArticleDOI
Overcoming therapy resistance in EGFR-mutant lung cancer
TL;DR: The mechanisms of acquired EGFR TKI resistance, the methods for monitoring its appearance, as well as current and future efforts to define treatment strategies to overcome resistance are reviewed.
Journal ArticleDOI
Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non-Small Cell Lung Cancer
Francois Gonzalvez,Sylvie Vincent,Theresa E. Baker,Alexandra E. Gould,Shuai Li,Scott Wardwell,Sara Nadworny,Yaoyu Ning,Sen Zhang,Wei-Sheng Huang,Yongbo Hu,Feng Li,Matthew T. Greenfield,Stephan G. Zech,Biplab Das,Narayana I. Narasimhan,Tim Clackson,David C. Dalgarno,William C Shakespeare,Michael Fitzgerald,Johara Chouitar,Robert J. Griffin,Shengwu Liu,Kwok-Kin Wong,Xiaotian Zhu,Victor M. Rivera +25 more
TL;DR: Pacheco et al. as mentioned in this paper proposed a novel EGFR exon 20 insertion (EGFRex20ins) driver mutations in non-small cell lung cancer (NSCLC) to address the limitations of existing therapies targeting EGFR-mutated NSCLC.
References
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Lindsey A. Torre,Freddie Bray,Rebecca L. Siegel,Jacques Ferlay,Joannie Lortet-Tieulent,Ahmedin Jemal +5 more
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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.
Rafael Rosell,Enric Carcereny,Radj Gervais,A. Vergnenegre,Bartomeu Massuti,Enriqueta Felip,Ramon Palmero,Ramon Garcia-Gomez,Cinta Pallares,Jose Miguel Sanchez,Rut Porta,Manuel Cobo,Pilar Garrido,Flavia Longo,Teresa Moran,A. Insa,Filippo de Marinis,Romain Corre,Isabel Bover,Alfonso Illiano,Eric Dansin,Javier de Castro,Michele Milella,Noemi Reguart,Giuseppe Altavilla,Ulpiano Jimenez,Mariano Provencio,Miguel Angel Moreno,J. Terrasa,Jose Muñoz-Langa,Javier Valdivia,Dolores Isla,Manuel Domine,Olivier Molinier,Julien Mazieres,Nathalie Baize,Rosario García-Campelo,Gilles Robinet,Delvys Rodriguez-Abreu,Guillermo Lopez-Vivanco,Vittorio Gebbia,Lioba Ferrera-Delgado,Pierre Bombaron,R. Bernabé,Alessandra Bearz,Angel Artal,Enrico Cortesi,Christian Rolfo,Maria Sanchez-Ronco,Ana Drozdowskyj,Cristina Queralt,Itziar de Aguirre,Jose Luis Ramirez,Jose Javier Sanchez,Miguel Angel Molina,Miquel Taron,Luis Paz-Ares +56 more
TL;DR: Erlotinib has been shown to improve progression-free survival compared with chemotherapy when given as first-line treatment for Asian patients with non-small-cell lung cancer (NSCLC) with activating EGFR mutations as discussed by the authors.
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MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling
Jeffrey A. Engelman,Kreshnik Zejnullahu,Tetsuya Mitsudomi,Youngchul Song,Courtney Hyland,Joon Oh Park,Neal I. Lindeman,Christopher-Michael Gale,Xiaojun Zhao,James J. Christensen,Takayuki Kosaka,Alison J. Holmes,Andrew M. Rogers,Federico Cappuzzo,Tony Mok,Charles Lee,Bruce E. Johnson,Lewis C. Cantley,Pasi A. Jänne +18 more
TL;DR: It is proposed that MET amplification may promote drug resistance in other ERBB-driven cancers as well after it was found that amplification of MET causes gefitinib resistance by driving ERBB3 (HER3)–dependent activation of PI3K, a pathway thought to be specific to EGFR/ERBB family receptors.
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