Literature DB >> 30108799

The structure-guided discovery of osimertinib: the first U.S. FDA approved mutant selective inhibitor of EGFR T790M.

Sam Butterworth1, Darren A E Cross1, M Raymond V Finlay1, Richard A Ward1, Michael J Waring1.   

Abstract

The winners of the Malcolm Campbell Memorial Prize for 2017 discuss the structure-guided discovery of Osimertinib and the difficulties associated with discovering a new drug.

Entities:  

Year:  2017        PMID： 30108799      PMCID： PMC6072417          DOI： 10.1039/c7md90012k

Source DB:  PubMed          Journal:  Medchemcomm        ISSN： 2040-2503            Impact factor:   3.597


  4 in total

1.  Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).

Authors:  Richard A Ward; Mark J Anderton; Susan Ashton; Paul A Bethel; Matthew Box; Sam Butterworth; Nicola Colclough; Christopher G Chorley; Claudio Chuaqui; Darren A E Cross; Les A Dakin; Judit É Debreczeni; Cath Eberlein; M Raymond V Finlay; George B Hill; Matthew Grist; Teresa C M Klinowska; Clare Lane; Scott Martin; Jonathon P Orme; Peter Smith; Fengjiang Wang; Michael J Waring
Journal:  J Med Chem       Date:  2013-08-30       Impact factor: 7.446

2.  Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.

Authors:  M Raymond V Finlay; Mark Anderton; Susan Ashton; Peter Ballard; Paul A Bethel; Matthew R Box; Robert H Bradbury; Simon J Brown; Sam Butterworth; Andrew Campbell; Christopher Chorley; Nicola Colclough; Darren A E Cross; Gordon S Currie; Matthew Grist; Lorraine Hassall; George B Hill; Daniel James; Michael James; Paul Kemmitt; Teresa Klinowska; Gillian Lamont; Scott G Lamont; Nathaniel Martin; Heather L McFarland; Martine J Mellor; Jonathon P Orme; David Perkins; Paula Perkins; Graham Richmond; Peter Smith; Richard A Ward; Michael J Waring; David Whittaker; Stuart Wells; Gail L Wrigley
Journal:  J Med Chem       Date:  2014-10-01       Impact factor: 7.446

3.  Osimertinib or Platinum-Pemetrexed in EGFR T790M-Positive Lung Cancer.

Authors:  Tony S Mok; Yi-Long Wu; Myung-Ju Ahn; Marina C Garassino; Hye R Kim; Suresh S Ramalingam; Frances A Shepherd; Yong He; Hiroaki Akamatsu; Willemijn S M E Theelen; Chee K Lee; Martin Sebastian; Alison Templeton; Helen Mann; Marcelo Marotti; Serban Ghiorghiu; Vassiliki A Papadimitrakopoulou
Journal:  N Engl J Med       Date:  2016-12-06       Impact factor: 91.245

4.  AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

Authors:  Darren A E Cross; Susan E Ashton; Serban Ghiorghiu; Cath Eberlein; Caroline A Nebhan; Paula J Spitzler; Jonathon P Orme; M Raymond V Finlay; Richard A Ward; Martine J Mellor; Gareth Hughes; Amar Rahi; Vivien N Jacobs; Monica Red Brewer; Eiki Ichihara; Jing Sun; Hailing Jin; Peter Ballard; Katherine Al-Kadhimi; Rachel Rowlinson; Teresa Klinowska; Graham H P Richmond; Mireille Cantarini; Dong-Wan Kim; Malcolm R Ranson; William Pao
Journal:  Cancer Discov       Date:  2014-06-03       Impact factor: 39.397
  4 in total
  7 in total

1.  Acrylamide fragment inhibitors that induce unprecedented conformational distortions in enterovirus 71 3C and SARS-CoV-2 main protease.

Authors:  Bo Qin; Gregory B Craven; Pengjiao Hou; Julian Chesti; Xinran Lu; Emma S Child; Rhodri M L Morgan; Wenchao Niu; Lina Zhao; Alan Armstrong; David J Mann; Sheng Cui
Journal:  Acta Pharm Sin B       Date:  2022-06-09       Impact factor: 14.903

2.  The third-generation EGFR inhibitor AZD9291 overcomes primary resistance by continuously blocking ERK signaling in glioblastoma.

Authors:  Xuejiao Liu; Xiangyu Chen; Lin Shi; Qianqian Shan; Qiyu Cao; Chenglong Yue; Huan Li; Shengsheng Li; Jie Wang; Shangfeng Gao; Mingshan Niu; Rutong Yu
Journal:  J Exp Clin Cancer Res       Date:  2019-05-23

Review 3.  Tackling Drug Resistance in EGFR Exon 20 Insertion Mutant Lung Cancer.

Authors:  Laura Pacini; Andrew D Jenks; Simon Vyse; Christopher P Wilding; Amani Arthur; Paul H Huang
Journal:  Pharmgenomics Pers Med       Date:  2021-03-09

4.  Comparison of Gefitinib in the treatment of patients with non-small cell lung cancer and clinical effects of Osimertinib and EGFR Gene mutation.

Authors:  Xiaofeng Li; Zhanqiang Zhai; Youcai Zhu; Haiou Zhou
Journal:  Pak J Med Sci       Date:  2022 Jul-Aug       Impact factor: 2.340

Review 5.  Advances in covalent drug discovery.

Authors:  Lydia Boike; Nathaniel J Henning; Daniel K Nomura
Journal:  Nat Rev Drug Discov       Date:  2022-08-25       Impact factor: 112.288

Review 6.  Targeting RTK-PI3K-mTOR Axis in Gliomas: An Update.

Authors:  Mayra Colardo; Marco Segatto; Sabrina Di Bartolomeo
Journal:  Int J Mol Sci       Date:  2021-05-05       Impact factor: 5.923

7.  Multi-scale Predictions of Drug Resistance Epidemiology Identify Design Principles for Rational Drug Design.

Authors:  Scott M Leighow; Chuan Liu; Haider Inam; Boyang Zhao; Justin R Pritchard
Journal:  Cell Rep       Date:  2020-03-24       Impact factor: 9.423
  7 in total

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