生物活性

• 描述EGF816 is a covalent, irreversible, mutant-selective EGFR inhibitor with Ki of 31 nM on EGFR(L858R/790M) mutant.
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT03529084	Carcinoma, Non-small Cell Lung	Phase 3	Withdrawn(strategic decision b... more >>y company) Collapse <<	May 31, 2024	-
  NCT03333343	EGFR-mutant Non-small Cell Lun... more >>g Cancer Collapse <<	Phase 1	Recruiting	May 21, 2021	Canada, Ontario ... more >> Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 Germany Novartis Investigative Site Recruiting Koeln, Germany, 50937 Italy Novartis Investigative Site Recruiting Ancona, AN, Italy, 60126 Novartis Investigative Site Recruiting Milano, MI, Italy, 20162 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Taiwan Novartis Investigative Site Recruiting Tainan, Taiwan, 70421 Novartis Investigative Site Recruiting Taipei, Taiwan, 10002 Collapse <<
  NCT02108964	Advanced Non-small Cell Lung C... more >>ancer Collapse <<	Phase 1 Phase 2	Active, not recruiting	September 20, 2019	United States, Massachusetts ... more >> Massachusetts General Hospital Mass General Boston, Massachusetts, United States, 02114 United States, New York Memorial Sloan Kettering Oncology Department New York, New York, United States, 10017 Canada, Ontario Novartis Investigative Site Toronto, Ontario, Canada, M5G 2M9 Germany Novartis Investigative Site Koeln, Nordrhein-Westfalen, Germany, 50937 Novartis Investigative Site Berlin, Germany, 13125 Japan Novartis Investigative Site Nagoya, Aichi, Japan, 464-8681 Novartis Investigative Site Fukuoka-city, Fukuoka, Japan, 811-1395 Korea, Republic of Novartis Investigative Site Seoul, Korea, Korea, Republic of, 03080 Novartis Investigative Site Seoul, Korea, Korea, Republic of, 05505 Netherlands Novartis Investigative Site Amsterdam, Netherlands, 1066 Singapore Novartis Investigative Site Singapore, Singapore, 169610 Spain Novartis Investigative Site Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Madrid, Spain, 28041 Taiwan Novartis Investigative Site Taipei, Taiwan ROC, Taiwan, 10041 Collapse <<

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• 参考文献

• [1] Lelais G, Epple R, et al. Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl] azepan-3-yl)-1H-benzo[d] imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers. J Med Chem. 2016 Jul 28;59(14):6671-89.

  [2] Jia Y, Juarez J, et al. EGF816 Exerts Anticancer Effects in Non-Small Cell Lung Cancer by Irreversibly and Selectively Targeting Primary and Acquired Activating Mutations in the EGF Receptor. Cancer Res. 2016 Mar 15;76(6):1591-602.