Hope and Disappointment: Covalent Inhibitors to Overcome Drug Resistance in Non-Small Cell Lung Cancer

被引:76
作者
Engel, Julian [1 ]
Lategahn, Jonas [1 ]
Rauh, Daniel [1 ]
机构
[1] TU Dortmund Univ, Fac Chem & Chem Biol, Otto Hahn Str 4a, D-44227 Dortmund, Germany
来源
ACS MEDICINAL CHEMISTRY LETTERS | 2016年 / 7卷 / 01期
关键词
EGFR; MUTATIONS; GEFITINIB; ERLOTINIB; AZD9291;
D O I
10.1021/acsmedchemlett.5b00475
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
In the last five years, the detailed understanding of how to overcome T790M drug resistance in non-small cell lung cancer (NSCLC) has culminated in the development of a third-generation of covalent EGFR inhibitors with excellent clinical outcomes. However, the emergence of a newly discovered acquired drug resistance challenges the concept of small molecule targeted cancer therapy in NSCLC.
引用
收藏
页码:2 / 5
页数:4
相关论文
共 12 条
[1]   Irreversible Protein Kinase Inhibitors: Balancing the Benefits and Risks [J].
Barf, Tjeerd ;
Kaptein, Allard .
JOURNAL OF MEDICINAL CHEMISTRY, 2012, 55 (14) :6243-6262
[2]   AZD9291 in EGFR Inhibitor-Resistant Non-Small-Cell Lung Cancer [J].
Jaenne, Pasi A. ;
Yang, James Chih-Hsin ;
Kim, Dong-Wan ;
Planchard, David ;
Ohe, Yuichiro ;
Ramalingam, Suresh S. ;
Ahn, Myung-Ju ;
Kim, Sang-We ;
Su, Wu-Chou ;
Horn, Leora ;
Haggstrom, Daniel ;
Felip, Enriqueta ;
Kim, Joo-Hang ;
Frewer, Paul ;
Cantarini, Mireille ;
Brown, Kathryn H. ;
Dickinson, Paul A. ;
Ghiorghiu, Serban ;
Ranson, Malcolm .
NEW ENGLAND JOURNAL OF MEDICINE, 2015, 372 (18) :1689-1699
[3]   BIBW2992, an irreversible EGFR/HER2 inhibitor highly effective in preclinical lung cancer models [J].
Li, D. ;
Ambrogio, L. ;
Shimamura, T. ;
Kubo, S. ;
Takahashi, M. ;
Chirieac, L. R. ;
Padera, R. F. ;
Shapiro, G. I. ;
Baum, A. ;
Himmelsbach, F. ;
Rettig, W. J. ;
Meyerson, M. ;
Solca, F. ;
Greulich, H. ;
Wong, K-K .
ONCOGENE, 2008, 27 (34) :4702-4711
[4]   Structural insights into how irreversible inhibitors can overcome drug resistance in EGFR [J].
Michalczyk, Anja ;
Klueter, Sabine ;
Rode, Haridas B. ;
Simard, Jeffrey R. ;
Gruetter, Christian ;
Rabiller, Matthias ;
Rauh, Daniel .
BIOORGANIC & MEDICINAL CHEMISTRY, 2008, 16 (07) :3482-3488
[5]   Afatinib versus placebo for patients with advanced, metastatic non-small-cell lung cancer after failure of erlotinib, gefitinib, or both, and one or two lines of chemotherapy (LUX-Lung 1): a phase 2b/3 randomised trial [J].
Miller, Vincent A. ;
Hirsh, Vera ;
Cadranel, Jacques ;
Chen, Yuh-Min ;
Park, Keunchil ;
Kim, Sang-We ;
Zhou, Caicun ;
Su, Wu-Chou ;
Wang, Mengzhao ;
Sun, Yan ;
Heo, Dae Seog ;
Crino, Lucio ;
Tan, Eng-Huat ;
Chao, Tsu-Yi ;
Shahidi, Mehdi ;
Cong, Xiuyu Julie ;
Lorence, Robert M. ;
Yang, James Chih-Hsin .
LANCET ONCOLOGY, 2012, 13 (05) :528-538
[6]   EGF receptor gene mutations are common in lung cancers from "never smokers" and are associated with sensitivity of tumors to gefitinib and erlotinib [J].
Pao, W ;
Miller, V ;
Zakowski, M ;
Doherty, J ;
Politi, K ;
Sarkaria, I ;
Singh, B ;
Heelan, R ;
Rusch, V ;
Fulton, L ;
Mardis, E ;
Kupfer, D ;
Wilson, R ;
Kris, M ;
Varmus, H .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 2004, 101 (36) :13306-13311
[7]   Rociletinib in EGFR-Mutated Non-Small-Cell Lung Cancer [J].
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. ;
Aisner, D. L. ;
Doebele, R. C. ;
Galasso, C. ;
Garon, E. B. ;
Heist, R. S. ;
Logan, J. ;
Neal, J. W. ;
Mendenhall, M. A. ;
Nichols, S. ;
Piotrowska, Z. ;
Wozniak, A. J. ;
Raponi, M. ;
Karlovich, C. A. ;
Jaw-Tsai, S. ;
Isaacson, J. ;
Despain, D. ;
Matheny, S. L. ;
Rolfe, L. ;
Allen, A. R. ;
Camidge, D. R. .
NEW ENGLAND JOURNAL OF MEDICINE, 2015, 372 (18) :1700-1709
[8]   Epidermal growth factor receptor mutations in lung cancer [J].
Sharma, Sreenath V. ;
Bell, Daphne W. ;
Settleman, Jeffrey ;
Haber, Daniel A. .
NATURE REVIEWS CANCER, 2007, 7 (03) :169-181
[9]   Insulin-like growth factor 1 (IGF1R)/insulin receptor (INSR) inhibitory activity of rociletinib (CO-1686) and its metabolites in nonclinical models [J].
Simmons, Andrew D. ;
Jaw-Tsai, Sarah ;
Haringsma, Henry J. ;
Allen, Andrew ;
Harding, Thomas C. .
CANCER RESEARCH, 2015, 75
[10]   Acquired EGFR C797S mutation mediates resistance to AZD9291 in non-small cell lung cancer harboring EGFR T790M [J].
Thress, Kenneth S. ;
Paweletz, Cloud P. ;
Felip, Enriqueta ;
Cho, Byoung Chul ;
Stetsonl, Daniel ;
Dougherty, Brian ;
Lai, Zhongwu ;
Markovets, Aleksandra ;
Vivancos, Ana ;
Kuang, Yanan ;
Ercan, Dalia ;
Matthews, Sarah E. ;
Cantarini, Mireille ;
Barrett, J. Carl ;
Jaenne, Pasi A. ;
Oxnard, Geoffrey R. .
NATURE MEDICINE, 2015, 21 (06) :560-562