生物活性

• 描述LSZ102 is a potent ERα antagonist and degrader. LSZ102 showed ERα degradation IC50 = 0.2 nM. LSZ102 demonstrated IC50 for MCF-7 cells = 1.7 nM. Upon administration of LSZ102, this agent binds to the ER and induces the degradation of the receptor. This prevents ER activation and ER-mediated signaling, and inhibits the growth and survival of ER-expressing cancer cells.
• 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
  NCT02734615	Advanced or Metastatic ER+ Bre... more >>ast Cancer Collapse <<	Phase 1	Recruiting	October 30, 2020	United States, Maryland ... more >> Novartis Investigative Site Recruiting Baltimore, Maryland, United States, 21287 United States, Massachusetts Massachusetts General Hospital Massachusetts General Hospital Recruiting Boston, Massachusetts, United States, 02114 Contact: Dejan Juric, MD    617-726-6500    Juric.Dejan@mgh.harvard.edu    Contact: Meghan Miles    617-726-6500    MEMILES@mgh.harvard.edu    Principal Investigator: Dejan Juric, MD          United States, New York Novartis Investigative Site Recruiting New York, New York, United States, 10021 Contact: Alexandra Burleigh    646-422-4394    burleiga@mskcc.org    Principal Investigator: Komal Jhaveri          United States, Texas Novartis Investigative Site Recruiting Houston, Texas, United States, 77030 Contact: Daniela Westerhold       diwesterhold@mdanderson.org    Principal Investigator: Rachel M Layman          Belgium Novartis Investigative Site Recruiting Bruxelles, Belgium, 1200 Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 France Novartis Investigative Site Recruiting Lyon Cedex, France, 69373 Italy Novartis Investigative Site Recruiting Milano, MI, Italy, 20133 Novartis Investigative Site Recruiting Milano, MI, Italy, 20141 Japan Novartis Investigative Site Recruiting Koto-ku, Tokyo, Japan, 135 8550 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08036 Novartis Investigative Site Recruiting Madrid, Spain, 28007 Collapse <<