Activity of crizotinib (PF02341066), a dual mesenchymal-epithelial transition (MET) and anaplastic lymphoma kinase (ALK) inhibitor, in a non-small cell lung cancer patient with de novo MET amplification.
Sai-Hong Ignatius Ou,Eunice L. Kwak,Christina Siwak-Tapp,Joni Dy,Kristin Bergethon,Jeffrey W. Clark,D. Ross Camidge,Benjamin Solomon,Robert G. Maki,Yung-Jue Bang,Dong Wan Kim,James G. Christensen,Weiwei Tan,Keith D. Wilner,Ravi Salgia,A. John Iafrate +15 more
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TLDR
An NSCLC patient with de novo MET amplification but no ALK rearrangement who achieved a rapid and durable response to crizotinib indicating is also a bona fide MET inhibitor.About:
This article is published in Journal of Thoracic Oncology.The article was published on 2011-05-01 and is currently open access. It has received 418 citations till now. The article focuses on the topics: ALK inhibitor & Crizotinib.read more
Citations
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Journal ArticleDOI
Crizotinib versus Chemotherapy in Advanced ALK-Positive Lung Cancer
Alice T. Shaw,Dong Wan Kim,Kazuhiko Nakagawa,Takashi Seto,Lucio Crinò,Myung-Ju Ahn,Tommaso De Pas,Benjamin Besse,Benjamin Solomon,Fiona H Blackhall,Yi-Long Wu,Michael Thomas,Kenneth J. O'Byrne,Denis Moro-Sibilot,D. Ross Camidge,Tony Mok,Vera Hirsh,Gregory J. Riely,Shrividya Iyer,V. Tassell,Anna Polli,Keith D. Wilner,Pasi A. Jänne +22 more
TL;DR: Crizotinib is superior to standard chemotherapy in patients with previously treated, advanced non-small-cell lung cancer with ALK rearrangement and greater improvement in global quality of life with crizotinIB than with chemotherapy.
Journal ArticleDOI
Structure Based Drug Design of Crizotinib (PF-02341066), a Potent and Selective Dual Inhibitor of Mesenchymal–Epithelial Transition Factor (c-MET) Kinase and Anaplastic Lymphoma Kinase (ALK)
J. Jean Cui,Michelle Tran-Dubé,Hong Shen,Nambu Mitchell David,Pei-Pei Kung,Pairish Mason Alan,Jia Lei,Jerry Meng,Funk Lee Andrew,Botrous Iriny,Michele McTigue,Neil Grodsky,Kevin Ryan,Ellen Padrique,Gordon Alton,Sergei Timofeevski,Shinji Yamazaki,Qiuhua Li,Helen Y. Zou,James G. Christensen,Barbara Mroczkowski,Steve Bender,Robert Steven Kania,Martin Paul Edwards +23 more
TL;DR: A novel 2-amino-5-aryl-3-benzyloxypyridine series was created to more effectively make the key interactions achieved with 3, which demonstrated potent in vitro and in vivo c-MET kinase and ALK inhibition, effective tumor growth inhibition, and good pharmaceutical properties.
Journal ArticleDOI
Acquired resistance to TKIs in solid tumours: learning from lung cancer
TL;DR: This Review explores breakthroughs in the understanding and treatment of acquired resistance in NSCLC, focusing on EGFR mutant and ALK rearrangement-positive disease, which may be relevant across multiple different solid malignancies with oncogene-addicted subtypes.
Journal ArticleDOI
Updated Molecular Testing Guideline for the Selection of Lung Cancer Patients for Treatment With Targeted Tyrosine Kinase Inhibitors: Guideline From the College of American Pathologists, the International Association for the Study of Lung Cancer, and the Association for Molecular Pathology
Neal I. Lindeman,Philip T. Cagle,Dara L. Aisner,Maria E. Arcila,Mary Beth Beasley,Eric H. Bernicker,Carol Colasacco,Sanja Dacic,Fred R. Hirsch,Keith M. Kerr,David J. Kwiatkowski,Marc Ladanyi,Jan A. Nowak,Lynette M. Sholl,Robyn Temple-Smolkin,Benjamin Solomon,Lesley Souter,Erik Thunnissen,Ming-Sound Tsao,Christina B. Ventura,Murry W. Wynes,Yasushi Yatabe +21 more
TL;DR: The 2013 guideline for molecular analysis of lung cancers was largely reaffirmed with updated recommendations to allow testing of cytology samples, require improved assay sensitivity, and recommend against the use of immunohistochemistry for EGFR testing.
Journal ArticleDOI
Non–Small Cell Lung Cancer
David S. Ettinger,Wallace Akerley,Gerold Bepler,Andrew C. Chang,Richard T. Cheney,Lucian R. Chirieac,Thomas A. D'Amico,Todd L. Demmy,Steven J. Feigenberg,Robert A. Figlin,Ramaswamy Govindan,Frederic W. Grannis,Thierry Jahan,Mohammad Jahanzeb,Anne Kessinger,Ritsuko Komaki,Mark G. Kris,Corey J. Langer,Quynh-Thu Le,Renato G. Martins,Gregory A. Otterson,Jyoti D. Patel,Francisco Robert,David J. Sugarbaker,Douglas E. Wood +24 more
TL;DR: In 2010, approximately 222,520 new cases of lung or bronchial cancer will be diagnosed in the USA, and 157,300 patients are expected to die of this disease as discussed by the authors.
References
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Journal ArticleDOI
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.
Journal ArticleDOI
Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer
Eunice L. Kwak,Yung-Jue Bang,D. Ross Camidge,Alice T. Shaw,Benjamin Solomon,Robert G. Maki,Sai-Hong Ignatius Ou,Bruce J. Dezube,Pasi A. Jänne,Daniel B. Costa,Marileila Varella-Garcia,Woo-Ho Kim,Thomas J. Lynch,Panos Fidias,Hannah Stubbs,Jeffrey A. Engelman,Lecia V. Sequist,Weiwei Tan,Leena Gandhi,Mari Mino-Kenudson,Greg C. Wei,S. Martin Shreeve,Mark J. Ratain,Jeffrey Settleman,James G. Christensen,Daniel A. Haber,Keith D. Wilner,Ravi Salgia,Geoffrey I. Shapiro,Jeffrey W. Clark,A. John Iafrate +30 more
TL;DR: The inhibition of ALK in lung tumors with the ALK rearrangement resulted in tumor shrinkage or stable disease in most patients, and the drug resulted in grade 1 or 2 gastrointestinal side effects.
Journal ArticleDOI
MET amplification occurs with or without T790M mutations in EGFR mutant lung tumors with acquired resistance to gefitinib or erlotinib
Jonathan F. Bean,Cameron Brennan,Jin-Yuan Shih,Gregory J. Riely,Gregory J. Riely,Agnes Viale,Lu Wang,Dhananjay Chitale,Noriko Motoi,Noriko Motoi,Janos Szoke,Stephen Broderick,Marissa Balak,Wen Cheng Chang,Chong-Jen Yu,Adi F. Gazdar,Harvey I. Pass,Valerie W. Rusch,William L. Gerald,Shiu Feng Huang,Pan-Chyr Yang,Vincent Miller,Vincent Miller,Marc Ladanyi,Chih-Hsin Yang,William Pao,William Pao +26 more
TL;DR: Analysis of tumor samples from multiple independent patient cohorts and array-based comparative genomic hybridization suggest that MET amplification occurs independently of EGFRT790M mutations and that MET may be a clinically relevant therapeutic target for some patients with acquired resistance to gefitinib or erlotinib.
Journal ArticleDOI
An orally available small-molecule inhibitor of c-met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms
Helen Y. Zou,Qiuhua Li,Joseph H. Lee,Maria E. Arango,Scott Rp McDonnell,Shinji Yamazaki,Tatiana B. Koudriakova,Gordon Alton,Jingrong Jean Cui,Pei Pei Kung,Nambu Mitchell David,Gerrit Los,Bender Steven Lee,Barbara Mroczkowski,James G. Christensen +14 more
TL;DR: The antitumor activity of PF-2341066 may be mediated by direct effects on tumor cell growth or survival as well as antiangiogenic mechanisms, and the therapeutic potential of targeting c-Met with selective small-molecule inhibitors for the treatment of human cancers is shown.
Journal ArticleDOI
Increased MET Gene Copy Number Negatively Affects Survival of Surgically Resected Non–Small-Cell Lung Cancer Patients
Federico Cappuzzo,Antonio Marchetti,Margaret Skokan,Elisa Rossi,Sujatha Gajapathy,Lara Felicioni,Maela Del Grammastro,Maria Grazia Sciarrotta,F Buttitta,Matteo Incarbone,Luca Toschi,Giovanna Finocchiaro,Annarita Destro,Luigi Terracciano,Massimo Roncalli,Marco Alloisio,Armando Santoro,M. Varella-Garcia +17 more
TL;DR: MET increased gene copy number is an independent negative prognostic factor in surgically resected NSCLC and EGFR gene gain does not impact survival after resection.
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Anaplastic Lymphoma Kinase Inhibition in Non–Small-Cell Lung Cancer
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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
Identification of the transforming EML4–ALK fusion gene in non-small-cell lung cancer
Crizotinib versus Chemotherapy in Advanced ALK-Positive Lung Cancer
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Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma
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