"目录号: HY-13636
Fulvestrant 是一种有效的特异性雌激素作用抑制剂，作用于雌激素受体 (Estrogen Receptor)，IC50为 9.4 nM。
Estrogen Receptor/ERRAutophagy
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生物活性
Description
Fulvestrant is a potent and specific inhibitor of estrogen action withIC50of 9.4 nM forEstrogen Receptor.
IC50& Target
IC50: 9.4 nM (Estrogen Receptor)[1]
In Vitro
Fulvestrant (ICI 182,780) is a potent and specific inhibitor of estrogen action and demonstrates excellent growth-inhibitory effects in both cell and animal models of human breast cancer. Fulvestrant inhibits MCF-7 human breast cancer cells growth with IC50of 290 nM. The relative binding affinities of Fulvestrant is 0.89 compare with that of Estradiol. Fulvestrant has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity[1]. Fulvestrant is the first of a new type of endocrine treatment-an oestrogen receptor (ER) antagonist that downregulates the ER[2]. Treatment of MCF-7 cells with 1?μM Tamoxifen has no effect on the expression of ERα, whereas 100?nM Fulvestrant completely inhibits ERα expression[3].
In Vivo
When administered alone, parenterally (s.c.), to immature female rats Fulvestrant (ICI 182,780) is devoid of uterotropic activity and, when coadministered with Estradiol, it effectively blocks the uterotropic action of Estradiol in a dose-dependent manner (ED50: 0.06 mg/kg/day s.c.). Complete antagonism of Estrogen action is achieved with a dose of 0.5 mg Fulvestrant/kg/day s.c. The effects of Fulvestrant administered p.o. are qualitatively similar but potency is reduced by an order of magnitude compare with s.c. dosing (ED50 0.46 and complete antagonism at 5 mg/kg/day p.o.)[1]. The antitumour activity of Fulvestrant is first demonstrated in two models of human breast cancer in nude mice. In one of these models, the growth of MCF-7 tumour xenografts, supported by continuous treatment with oestradiol, is completely blocked for at least 4 weeks following a single injection of Fulvestrant 5?mg. Similar reductions in growth are seen in the Br10 human tumour model. In other studies in nude mice bearing MCF-7 xenografts, Fulvestrant suppresses the growth of established tumours for twice as long and tumour growth is delayed to a greater extent than is observed with Tamoxifen treatment. Tamoxifen-resistant breast tumours, which grow in nude mice after long-term treatment with Tamoxifen, remain ensitive to growth inhibition by Fulvestrant[2]. These are comparable to the tumor growth inhibition (TGI) observed for Tamoxifen and Fulvestrant, which on day 40 are 86 and 88%, respectively[3].
Clinical Trial
Beth Israel Deaconess Medical Center-Dana-Farber Cancer Institute-Brigham and Women's Hospital-Massachusetts General Hospital-Lowell General Hospital-University of Colorado, Denver-University of Maryland Greenebaum Cancer Center-South Shore Hospital
Breast Cancer
April 2004
Phase 2
University of Colorado, Denver-United States Department of Defense
Breast Cancer
July 2017
Phase 2
University of Wisconsin, Madison-AstraZeneca-University of Pittsburgh
Carcinoma, Non Small Cell Lung
November 2009
Phase 1
Masonic Cancer Center, University of Minnesota
Ovarian Cancer
June 2007
Phase 2
AstraZeneca
Advanced Metastatic Breast Cancer
May 8, 2012
Phase 1
Fresenius Kabi
Healthy
June 2016
Phase 1
University of Colorado, Denver-United States Department of Defense
Breast Cancer
July 2017
Phase 2
Dana-Farber Cancer Institute
Breast Cancer
May 2012
Phase 2
Atossa Genetics, Inc.
Female Breast Carcinoma-Female Ductal Carcinoma In Situ
March 2016
Phase 2
Stanford University-AstraZeneca
Prostatic Neoplasms-Prostate Cancer
September 2006
Phase 2
Fudan University
Metastatic Breast Cancer
July 2017
AstraZeneca
Breast Cancer
March 2011
Phase 3
Sidney Kimmel Comprehensive Cancer Center-Pfizer
Metastatic Breast Cancer
August 2016
Phase 2
Gynecologic Oncology Group-National Cancer Institute (NCI)
Recurrent Uterine Corpus Carcinoma-Stage III Uterine Corpus Cancer-Stage IV Uterine Corpus Cancer
August 2004
Phase 2
Consorzio Oncotech-Clinical Research Technology S.r.l.
Metastatic Breast Cancer
November 2015
Phase 3
Celgene
Breast Neoplasms
March 13, 2015
Phase 2
AstraZeneca
Advanced Breast Cancer
April 2004
Phase 1
Swiss Group for Clinical Cancer Research
Breast Cancer
August 2010
Phase 2
Ewa Mrozek-Pfizer-Ohio State University Comprehensive Cancer Center
Breast Cancer
September 2005
Phase 2
Mara Chambers-Novartis-University of Kentucky
Breast Cancer
April 2008
Phase 2
AstraZeneca-Dendrix - Scientific Information Architecture
Breast Cancer
May 2008
Regina Elena Cancer Institute-AstraZeneca
Breast Cancer
October 2008
Phase 2
Velindre NHS Trust-Cancer Research UK-AstraZeneca
Neoplasms
April 2015
Phase 2
Isabel Blancas-Hospital Clinico Universitario San Cecilio
Malignant Neoplasm of Breast Stage IV
January 2012
Fudan University
Breast Neoplasms
July 1, 2017
Phase 2
Hellenic Oncology Research Group
Breast Cancer
April 2011
Icahn School of Medicine at Mount Sinai-AstraZeneca
Breast Cancer
October 2016
Phase 1
University of Kansas Medical Center-AstraZeneca
Invasive Breast Cancer
May 2009
Phase 2
Accelerated Community Oncology Research Network-Hoffmann-La Roche-AstraZeneca
Metastatic Breast Cancer
October 2007
Phase 2
AstraZeneca
Breast Cancer
June 2004
Phase 2
AstraZeneca
Advanced Breast Cancer-Metastatic Breast Cancer
May 2006
Phase 2
AstraZeneca
Breast Cancer
February 8, 2005
Phase 3
Hospital Affiliated to Military Medical Science, Beijing
Metastatic Breast Cancer
January 2014
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
July 23, 2015
Phase 3
Fudan University
Metastatic Breast Cancer
April 2014
Phase 2
Roswell Park Cancer Institute
Prostate Cancer
June 2004
Phase 2
AstraZeneca
Advanced Breast Cancer-Metastatic Breast Cancer
March 2006
Phase 2
Mayo Clinic-National Cancer Institute (NCI)
Estrogen Receptor Positive-Progesterone Receptor Positive-Recurrent Breast Carcinoma-Stage IIIB Breast Cancer-Stage IIIC Breast Cancer-Stage IV Breast Cancer
September 2014
Phase 1
Spanish Breast Cancer Research Group-AstraZeneca
Breast Neoplasms
February 2016
Phase 2
AstraZeneca
Endometrial Carcinoma
December 2002
Phase 2
PrECOG, LLC.-Novartis
Metastatic Breast Cancer
May 31, 2013
Phase 2
National Cancer Institute (NCI)
Estrogen Receptor-positive Breast Cancer-Recurrent Breast Cancer-Stage IIIB Breast Cancer-Stage IIIC Breast Cancer-Stage IV Breast Cancer
March 2004
Phase 2
Wales Cancer Trials Unit-Velindre NHS Trust
Estrogen Receptor Positive Breast Cancer
May 2014
Phase 1-Phase 2
Fudan University
Carcinoma Breast Stage IV
March 2014
Phase 2
Syndax Ph
