Update on third-generation EGFR tyrosine kinase inhibitors.

作者: Eric Haura , Jhanelle Gray

DOI: 10.3978/J.ISSN.2218-6751.2014.09.08

关键词:

摘要: Among patients with non-small cell lung cancer (NSCLC), EGFR mutations, 90% of which present as an exon 19 deletion or 21 point mutation L858R, have been detected in Western and Asian populations at a rate ~15% ~40%, respectively. To date, numerous trials established the efficacy toxicity profile singleagent oral EGFR-tyrosine kinase inhibitor (TKI) therapies for EGFR-TKI-naive NSCLC harboring mutations. These include IPASS gefitinib (1), Optimal erlotinib (2), LUX-Lung 3 afatinib (3). Still, majority will eventually develop resistance.

参考文章(12)
Lecia V. Sequist, James Chih-Hsin Yang, Nobuyuki Yamamoto, Kenneth O'Byrne, Vera Hirsh, Tony Mok, Sarayut Lucien Geater, Sergey Orlov, Chun-Ming Tsai, Michael Boyer, Wu-Chou Su, Jaafar Bennouna, Terufumi Kato, Vera Gorbunova, Ki Hyeong Lee, Riyaz Shah, Dan Massey, Victoria Zazulina, Mehdi Shahidi, Martin Schuler, Phase III Study of Afatinib or Cisplatin Plus Pemetrexed in Patients With Metastatic Lung Adenocarcinoma With EGFR Mutations Journal of Clinical Oncology. ,vol. 31, pp. 3327- 3334 ,(2013) , 10.1200/JCO.2012.44.2806
David Jackman, William Pao, Gregory J. Riely, Jeffrey A. Engelman, Mark G. Kris, Pasi A. Jänne, Thomas Lynch, Bruce E. Johnson, Vincent A. Miller, Clinical Definition of Acquired Resistance to Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Non–Small-Cell Lung Cancer Journal of Clinical Oncology. ,vol. 28, pp. 357- 360 ,(2010) , 10.1200/JCO.2009.24.7049
Nobuyuki Katakami, Shinji Atagi, Koichi Goto, Toyoaki Hida, Takeshi Horai, Akira Inoue, Yukito Ichinose, Kunihiko Koboyashi, Koji Takeda, Katsuyuki Kiura, Kazuto Nishio, Yoko Seki, Ryuichi Ebisawa, Mehdi Shahidi, Nobuyuki Yamamoto, LUX-Lung 4: A Phase II Trial of Afatinib in Patients With Advanced Non–Small-Cell Lung Cancer Who Progressed During Prior Treatment With Erlotinib, Gefitinib, or Both Journal of Clinical Oncology. ,vol. 31, pp. 3335- 3341 ,(2013) , 10.1200/JCO.2012.45.0981
Yelena Y. Janjigian, Christopher G. Azzoli, Lee M. Krug, Leanne K. Pereira, Naiyer A. Rizvi, M Catherine Pietanza, Mark G. Kris, Michelle S. Ginsberg, William Pao, Vincent A. Miller, Gregory J. Riely, Phase I/II Trial of Cetuximab and Erlotinib in Patients with Lung Adenocarcinoma and Acquired Resistance to Erlotinib Clinical Cancer Research. ,vol. 17, pp. 2521- 2527 ,(2011) , 10.1158/1078-0432.CCR-10-2662
Caicun Zhou, Yi-Long Wu, Gongyan Chen, Jifeng Feng, Xiao-Qing Liu, Changli Wang, Shucai Zhang, Jie Wang, Songwen Zhou, Shengxiang Ren, Shun Lu, Li Zhang, Chengping Hu, Chunhong Hu, Yi Luo, Lei Chen, Ming Ye, Jianan Huang, Xiuyi Zhi, Yiping Zhang, Qingyu Xiu, Jun Ma, Li Zhang, Changxuan You, 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 Lancet Oncology. ,vol. 12, pp. 735- 742 ,(2011) , 10.1016/S1470-2045(11)70184-X
Tony S. Mok, Yi-Long Wu, Sumitra Thongprasert, Chih-Hsin Yang, Da-Tong Chu, Nagahiro Saijo, Patrapim Sunpaweravong, Baohui Han, Benjamin Margono, Yukito Ichinose, Yutaka Nishiwaki, Yuichiro Ohe, Jin-Ji Yang, Busyamas Chewaskulyong, Haiyi Jiang, Emma L. Duffield, Claire L. Watkins, Alison A. Armour, Masahiro Fukuoka, Gefitinib or Carboplatin–Paclitaxel in Pulmonary Adenocarcinoma The New England Journal of Medicine. ,vol. 361, pp. 947- 957 ,(2009) , 10.1056/NEJMOA0810699
YY Janjigian, HJ Groen, L Horn, EF Smit, Yali Fu, F Wang, M Shahidi, LJ Denis, W Pao, VA Miller, None, Activity and tolerability of afatinib (BIBW 2992) and cetuximab in NSCLC patients with acquired resistance to erlotinib or gefitinib Journal of Clinical Oncology. ,vol. 29, pp. 7525- 7525 ,(2011) , 10.1200/JCO.2011.29.15_SUPPL.7525
Shirish M. Gadgeel, Heather A. Wakelee, D. Ross Camidge, Andrea Varga, Benjamin J. Solomon, Vassiliki Papadimitrakopoulou, Sarah S. Jaw-Tsai, Lisa Caunt, Paramjit Kaur, Lindsey Rolfe, Andrew R. Allen, Jonathan Wade Goldman, Lecia V. Sequist, Jean-Charles Soria, First-in-human evaluation of CO-1686, an irreversible, highly selective tyrosine kinase inhibitor of mutations of EGFR (activating and T790M). Journal of Clinical Oncology. ,vol. 32, pp. 8010- 8010 ,(2014) , 10.1200/JCO.2014.32.15_SUPPL.8010
Dong-Wan Kim, Dae Ho Lee, Jin Hyoung Kang, Keunchil Park, Ji-Youn Han, Jong-Seok Lee, In-Jin Jang, Hyo-Yeon Kim, Jeewoong Son, Joo-Hang Kim, Clinical activity and safety of HM61713, an EGFR-mutant selective inhibitor, in advanced non-small cell lung cancer (NSCLC) patients (pts) with EGFR mutations who had received EGFR tyrosine kinase inhibitors (TKIs). Journal of Clinical Oncology. ,vol. 32, pp. 8011- 8011 ,(2014) , 10.1200/JCO.2014.32.15_SUPPL.8011
Martin H Schuler, Chih-Hsin Yang, Keunchil Park, Jaafar Bennouna, Yuh-Min Chen, Christos Chouaid, Filippo De Marinis, Ji Feng Feng, Francesco Grossi, Dong-Wan Kim, Xiaoqing Liu, Shun Lu, Janos Strausz, Yurii Vinnyk, Rainer Wiewrodt, Caicun Zhou, Vikram K Chand, Bushi Wang, Joo-Hang Kim, David Planchard, LUX-Lung 5 Investigators, None, Continuation of afatinib beyond progression: Results of a randomized, open-label, phase III trial of afatanib plus paclitaxel (P) versus investigator’s choice chemotherapy (CT) in patients (pts) with metastatic non-small cell lung cancer (NSCLC) progressed on erlotinib/gefitinib (E/G) and afatanib—LUX-Lung 5 (LL5). Journal of Clinical Oncology. ,vol. 32, pp. 8019- 8019 ,(2014) , 10.1200/JCO.2014.32.15_SUPPL.8019