Literature DB >> 27840244

EAI045: The fourth-generation EGFR inhibitor overcoming T790M and C797S resistance.

Shuhang Wang1, Yongping Song2, Delong Liu3.   

Abstract

The third-generation tyrosine kinase inhibitors (TKI), AZD9291 (osimertinib) and CO-1686 (rociletinib) of epidermal growth factor receptor (EGFR) are highly active against T790M positive non-small cell lung cancer (NSCLC). However, resistance develops rapidly. EGFR C797S mutation was reported to be a leading mechanism of resistance to the third-generation inhibitors. The C797S mutation appears to be an ideal target for overcoming the acquired resistance to the third-generation inhibitors. This review summarizes the latest development on the discovery of a fourth-generation EGFR TKI, EAI045.3. Copyright Â
© 2016 Elsevier Ireland Ltd. All rights reserved.

Entities:  

Keywords:  AZD9291; EAI045; EGFR; NSCLC; Rociletinib; TKI; epidermal growth factor receptor; non-small cell lung cancer; tyrosine kinase inhibitor

Mesh：

Substances：

Year:  2016        PMID： 27840244     DOI： 10.1016/j.canlet.2016.11.008

Source DB:  PubMed          Journal:  Cancer Lett        ISSN： 0304-3835            Impact factor:   8.679


  61 in total

1.  Osimertinib for advanced non-small cell lung cancer harboring EGFR mutation exon 20 T790M, acquired resistant mutation for first- or second-generation EGFR-TKI.

Authors:  Yusuke Okuma; Yukio Hosomi
Journal:  J Thorac Dis       Date:  2017-03       Impact factor: 2.895

2.  Venetoclax and low-dose cytarabine induced complete remission in a patient with high-risk acute myeloid leukemia: a case report.

Authors:  Bingshan Liu; Roshni Narurkar; Madhura Hanmantgad; Wahib Zafar; Yongping Song; Delong Liu
Journal:  Front Med       Date:  2018-05-21       Impact factor: 4.592

Review 3.  Overcoming therapy resistance in EGFR-mutant lung cancer.

Authors:  Pasi A Jänne; Tony Mok; Solange Peters; Antonio Passaro
Journal:  Nat Cancer       Date:  2021-04-15

4.  Systematic analysis and molecular profiling of EGFR allosteric inhibitor cross-reactivity across the proto-oncogenic ErbB family kinases by integrating dynamics simulation, energetics calculation and biochemical assay.

Authors:  Yanli Ma; Bingli Qi; Meiying Ning; Lijuan Zhang; Zeyu An; Jing Zhao
Journal:  Eur Biophys J       Date:  2022-03-21       Impact factor: 1.733

Review 5.  Potentiating Therapeutic Effects of Epidermal Growth Factor Receptor Inhibition in Triple-Negative Breast Cancer.

Authors:  Kyu Sic You; Yong Weon Yi; Jeonghee Cho; Jeong-Soo Park; Yeon-Sun Seong
Journal:  Pharmaceuticals (Basel)       Date:  2021-06-18

6.  Discovery of Potent and Selective Epidermal Growth Factor Receptor (EGFR) Bifunctional Small-Molecule Degraders.

Authors:  Meng Cheng; Xufen Yu; Kaylene Lu; Ling Xie; Li Wang; Fanye Meng; Xiaoran Han; Xian Chen; Jing Liu; Yue Xiong; Jian Jin
Journal:  J Med Chem       Date:  2020-01-14       Impact factor: 7.446

7.  Integrin α5 promotes migration and invasion through the FAK/STAT3/AKT signaling pathway in icotinib-resistant non-small cell lung cancer cells.

Authors:  Yang Yang; Yizhe Wang; Xiaofang Che; Kezuo Hou; Jie Wu; Chunlei Zheng; Yang Cheng; Yunpeng Liu; Xuejun Hu; Jingdong Zhang
Journal:  Oncol Lett       Date:  2021-05-24       Impact factor: 2.967

Review 8.  Targeted therapy in advanced non-small cell lung cancer: current advances and future trends.

Authors:  Umair Majeed; Rami Manochakian; Yujie Zhao; Yanyan Lou
Journal:  J Hematol Oncol       Date:  2021-07-08       Impact factor: 17.388

Review 9.  Has programmed cell death ligand-1 MET an accomplice in non-small cell lung cancer?-a narrative review.

Authors:  Wolfram C M Dempke; Klaus Fenchel
Journal:  Transl Lung Cancer Res       Date:  2021-06

10.  Drug resistance and combating drug resistance in cancer.

Authors:  Xuan Wang; Haiyun Zhang; Xiaozhuo Chen
Journal:  Cancer Drug Resist       Date:  2019-06-19
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