Discovery of rociletinib (CO-1686), a mutant-selective covalent inhibitor of EGFR

被引：0
|
作者：
Niu, Deqiang [1 ]
机构：
[1] Celgene Avil Res, Med Chem, Lexington, MA USA
来源：
ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY | 2015年 / 250卷
关键词：
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
337
引用
收藏
页数：1
相关论文
共 50 条
  • [1] Identification of Effective Drug Combinations to Prevent or Delay Resistance to the EGFR Mutant Selective Inhibitor Rociletinib (CO-1686)
    Simmons, Andrew
    Haringsma, Henry J.
    Minh Nguyen
    Robillard, Liliane
    Allen, Andrew
    Harding, Thomas C.
    [J]. JOURNAL OF THORACIC ONCOLOGY, 2015, 10 (09) : S295 - S295
  • [2] In vivo acquired resistance to the mutant EGFR inhibitor Rociletinib (CO-1686) is associated with activation of the c-MET pathway
    Haringsma, Henry J.
    Allen, Andrew
    Harding, Thomas C.
    Simmons, Andrew D.
    [J]. CANCER RESEARCH, 2015, 75
  • [3] Design of a novel covalent EGFR mutant-selective inhibitor
    Sjin, R. Tjin Tham
    Lee, K.
    Sheets, M.
    Martin, T. St.
    Niu, D.
    Chaturvedi, P.
    Westlin, W.
    Petter, R.
    Nacht, M.
    Singh, J.
    [J]. EJC SUPPLEMENTS, 2010, 8 (07): : 31 - 31
  • [4] Pretreatment and serial plasma assessments of EGFR mutations in NSCLC patients treated with rociletinib (CO-1686)
    Goldman, Jonathan W.
    Karlovich, Chris
    Mann, Elaina
    Rolfe, Lindsey
    Matheny, Shannon
    Despain, Darrin
    Angenendt, Philipp
    Stamm, Claudia
    Wakelee, Heather A.
    Soria, Jean-Charles
    Solomon, Benjamin
    Camidge, D. R.
    Dziadziuszko, Rafal
    Horn, Leora
    Gadgeel, Shirish
    Raponi, Mitch
    Allen, Andrew R.
    Sequist, Lecia V.
    [J]. CANCER RESEARCH, 2015, 75
  • [5] In vitro acquired resistance to the mutant selective EGFR inhibitor CO-1686 is associated with epithelial-mesenchymal transition (EMT).
    Haringsma, Henry
    Walter, Annette O.
    Sjin, Robert Tjin Tham
    Allen, Andrew
    Harding, Thomas C.
    Simmons, Andrew D.
    [J]. MOLECULAR CANCER THERAPEUTICS, 2013, 12 (11)
  • [6] Interim phase 2 results of study CO-1686-008: A phase 1/2 study of the irreversible, mutant selective, EGFR inhibitor rociletinib (CO-1686) in patients with advanced non small cell lung cancer
    Soria, J.
    Sequist, L. V.
    Goldman, J. W.
    Wakelee, H. A.
    Gadgeel, S. M.
    Varga, A.
    Yu, H. A.
    Solomon, B. J.
    Ou, S. H.
    Papadimitrakopoulou, V.
    Oxnard, G. R.
    Horn, L.
    Dziadziuszko, R.
    Chao, B.
    Spira, A. I.
    Liu, S.
    Mekhail, T.
    Matheny, S.
    Litten, J.
    Camidge, R. D.
    [J]. EUROPEAN JOURNAL OF CANCER, 2014, 50 : 199 - 199
  • [7] Discovery of a Mutant-Selective Covalent Inhibitor of EGFR that Overcomes T790M-Mediated Resistance in NSCLC
    Walter, Annette O.
    Sjin, Robert Tjin Tham
    Haringsma, Henry J.
    Ohashi, Kadoaki
    Sun, Jing
    Lee, Kwangho
    Dubrovskiy, Aleksandr
    Labenski, Matthew
    Zhu, Zhendong
    Wang, Zhigang
    Sheets, Michael
    St Martin, Thia
    Karp, Russell
    van Kalken, Dan
    Chaturvedi, Prasoon
    Niu, Deqiang
    Nacht, Mariana
    Petter, Russell C.
    Westlin, William
    Lin, Kevin
    Jaw-Tsai, Sarah
    Raponi, Mitch
    Van Dyke, Terry
    Etter, Jeff
    Weaver, Zoe
    Pao, William
    Singh, Juswinder
    Simmons, Andrew D.
    Harding, Thomas C.
    Allen, Andrew
    [J]. CANCER DISCOVERY, 2013, 3 (12) : 1404 - 1415
  • [8] Efficacy of rociletinib (co-1686) in EGFR-mutant non-small cell lung cancer (NSCLC) patients (pts) assessed with a plasma EGFR test
    Gadgeel, S.
    Soria, J. C.
    Goldman, J. W.
    Wakelee, H.
    Camidge, D. R.
    Yu, H.
    Varga, A.
    Solomon, B.
    Oxnard, G. R.
    Ou, S. H.
    Papadimitrakopoulou, V.
    Liu, S. V.
    Reckamp, K.
    Spira, A.
    Piotrowska, Z.
    Despain, D.
    Karlovich, C.
    Yurasov, S.
    Sequist, L. V.
    [J]. EUROPEAN JOURNAL OF CANCER, 2015, 51 : S628 - S628
  • [9] Discovery of a potent covalent mutant-selective EGFR inhibitor - the journey from high throughput screening to EGF816
    Lelais, Gerald
    Epple, Robert
    Michellys, Pierre-Yves
    Marsilje, Thomas H.
    Long, Yun
    McNeill, Matthew
    Chen, Bei
    Lu, Wenshuo
    Bursulaya, Badry
    DiDonato, Michael
    Jia, Yong
    Kasibhatla, Shailaja
    Li, Chun
    Matushansky, Igor
    Bender, Steven
    [J]. CANCER RESEARCH, 2015, 75
  • [10] Discovery and Optimization of Dibenzodiazepinones as Allosteric Mutant-Selective EGFR Inhibitors
    De Clercq, Dries J. H.
    Heppner, David E.
    To, Ciric
    Jang, Jaebong
    Park, Eunyoung
    Yun, Cai-Hong
    Mushajiang, Mierzhati
    Shin, Bo Hee
    Gero, Thomas W.
    Scott, David A.
    Janne, Pasi A.
    Eck, Michael J.
    Gray, Nathanael S.
    [J]. ACS MEDICINAL CHEMISTRY LETTERS, 2019, 10 (11): : 1549 - 1553
12345