生物活性

• 描述PF-06747775 provides potent EGFR activity against the four common mutants (exon 19 deletion (Del), L858R, and double mutants T790M/L858R and T790M/Del), selectivity over wild-type EGFR, and desirable ADME properties.
• 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
  NCT02349633	Non-Small Cell Lung Cancer	Phase 2	Active, not recruiting	March 15, 2020	United States, California ... more >> UC San Diego Moores Cancer Center - Investigational Drug Services La Jolla, California, United States, 92037-0845 UC San Diego Medical Center - La Jolla La Jolla, California, United States, 92037 UC San Diego Moores Cancer Center La Jolla, California, United States, 92093-0698 UC San Diego Medical Center - Hillcrest San Diego, California, United States, 92103 United States, Connecticut Smilow Cancer Hospital at Yale-New Haven New Haven, Connecticut, United States, 06510 United States, Pennsylvania Hillman Cancer Center Pittsburgh, Pennsylvania, United States, 15232 UPMC Cancer Pavilion Pittsburgh, Pennsylvania, United States, 15232 UPMC Hillman Cancer Center Pittsburgh, Pennsylvania, United States, 15232 United States, Washington Seattle Cancer Care Alliance Seattle, Washington, United States, 98109 University of Washington Medical Center Seattle, Washington, United States, 98195 Australia, New South Wales Chris O'Brien Lifehouse Camperdown, New South Wales, Australia, 2050 Royal Prince Alfred Hospital Camperdown, New South Wales, Australia, 2050 Australia, Queensland Prince Charles Hospital, Cancer Care Services Chermside, Queensland, Australia, 4032 Japan National Hospital Organization Shikoku Cancer Center Matsuyama, Ehime, Japan, 791-0280 The Cancer Institute Hospital of JFCR Koto-ku, Tokyo, Japan, 135-8550 Korea, Republic of Seoul National University Hospital / Department of Internal Medicine Seoul, Korea, Republic of, 03080 Severance Hospital, Yonsei University Health System Seoul, Korea, Republic of, 03722 Asan Medical Center Seoul, Korea, Republic of, 05505 Clinical Trial Pharmacy Seoul, Korea, Republic of, 05505 Collapse <<

• 参考文献

• [1] Wang S, Cang S, et al. Third-generation inhibitors targeting EGFR T790M mutation in advanced non-small cell lung cancer. J Hematol Oncol. 2016 Apr 12;9:34.

  [2] Planken S, Behenna DC, et al. Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR. J Med Chem. 2017 Apr 13;60(7):3002-3019.