"目录号: HY-13632
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Exemestane(FCE 24304)是芳香酶（aromatase）抑制剂，能抑制人胎盘和鼠卵巢芳香酶，IC50分别为30 nM和40 nM。
Aromatase
相关产品
Letrozole-Anastrozole-Testolactone-Formestane-Aminoglutethimide-4-Hydroxytestosterone-Fadrozole-Org30958-
生物活性
Description
Exemestane(FCE 24304) is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.Target: AromataseApproved: October 2005Exemestane competitively inhibits and time-dependently inactivates of human placental aromatase with Ki of 4.3 nM. Exemestane displaces [3H]DHT from rat prostate androgen receptor with IC50 of 0.9 μM [1]. Exemestane (1 μM) increases alkaline phosphatase activity in hFOB and Saos-2 cells and induces the expression of MYBL2, OSTM1, HOXD11, ADCYAP1R1, and glypican 2 in hFOB cells [2]. Exemestane causes aromatase degradation in a dose-responsive manner in MCF-7aro cells [3].Exemestane increases lumbar spine BMD by 14.0% in OVX rats at dose of 100 mg/kg. Exemestane (100 mg/kg) and 17-hydroexemestane (20 mg/kg) significantly reduces an ovariectomy-induced increase in serum pyridinoline and serum osteocalcin in rats and causes significant reductions of serum cholesterol and low-density lipoprotein cholesterol inOVX rats [4].Exemestane (20 mg/kg/day s.c.) induces 26% complete (CR) and 18% partial (PR) tumor regressions in rats with 7,12-dimethylbenzanthracene (DMBA)-induced mammary tumors [5].
Clinical Trial
NCT00810706
Hellenic Breast Surgeons Society
Breast Cancer
April 2001
Phase 3
NCT01655004
National University Hospital, Singapore
Breast Carcinoma
August 2012
NCT01965080
Nordic Society for Gynaecologic Oncology
Endometrial Cancer
March 2004
Phase 2
NCT01760980
Actavis Inc.
Healthy
November 2012
Phase 1
NCT00201773
Ohio State University Comprehensive Cancer Center-Pfizer
Breast Cancer
July 2003
Phase 2
NCT01648608
Tianjin Medical University
Breast Cancer
January 2012
Phase 2-Phase 3
NCT01743560
Novartis Pharmaceuticals-Novartis
Oestrogen Receptor Positive Advanced Breast Cancer
January 2013
Phase 4
NCT00676663
Syndax Pharmaceuticals
Breast Cancer-Estrogen Receptor-Positive Breast Cancer-Breast Cancer, Estrogen Receptor-Positive-ER+ Breast Cancer
May 2008
Phase 2
NCT00073073
Georgetown University-National Cancer Institute (NCI)
Breast Neoplasms
November 2003
Phase 2
NCT00200174
Memorial Sloan Kettering Cancer Center-Pharmacia
Breast Cancer
July 1999
NCT00919399
Institut Claudius Regaud-PHARMACIA SAS
Breast Neoplasms
January 2002
Phase 2
NCT01431053
Chinese Academy of Medical Sciences
Breast Neoplasms
July 2011
Phase 2
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Ewa Mrozek-Pfizer-Ohio State University Comprehensive Cancer Center
Breast Cancer
September 2005
Phase 2
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National Taiwan University Hospital-Merck Sharp & Dohme Corp.
Premenopausal Breast Cancer
December 2016
Phase 1-Phase 2
NCT01658176
Pfizer
Breast Neoplasms
January 2013
Phase 2
NCT02025712
Organisation for Oncology and Translational Research
Hormone Receptor Positive Malignant Neoplasm of Breast
Phase 2
NCT01155063
Pfizer
Early Breast Cancer
September 2010
NCT00031889
Swiss Group for Clinical Cancer Research
Prostate Cancer
August 2001
Phase 2
NCT00767520
Bristol-Myers Squibb
Breast Cancer
February 2009
Phase 2
NCT00649090
Pfizer
Breast Neoplasms
March 2005
Phase 4
NCT00083174
NCIC Clinical Trials Group-Grupo Espanol de Investigacion del Cancer de Mama-UNICANCER-Canadian Cancer Trials Group
Breast Cancer
February 2004
Phase 3
NCT02482753
Chipscreen Biosciences, Ltd.
Breast Cancer
July 2015
Phase 3
NCT02666105
Masonic Cancer Center, University of Minnesota
Non-Small Cell Lung Cancer
August 2016
Phase 2
NCT00040014
Pfizer
Breast Neoplasms
June 2002
Phase 2
NCT01963481
New York University School of Medicine
Metastatic Beast Cancer
September 2013
Phase 2
NCT00036270
Pfizer
Breast Neoplasms
August 2001
Phase 3
NCT02646735
Chinese Academy of Medical Sciences-Cancer Institute and Hospital, Chinese Academy of Medical Sciences
Breast Cancer
December 2015
Phase 2
NCT02820961
Syndax Pharmaceuticals
Breast Cancer-Estrogen Receptor Positive Breast Cancer
June 2016
Phase 1
NCT00066586
NCIC Clinical Trials Group-Canadian Cancer Trials Group
Breast Cancer
August 2001
NCT00174343
Pfizer
Breast Neoplasms
November 2001
Phase 2
NCT02077933
Novartis Pharmaceuticals-Novartis
Neoplasms-Breast Neoplasms-Kidney Neoplasms-Pancreatic Neuroendocine Neoplasms
May 2014
Phase 1
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Novartis Pharmaceuticals-Novartis
Breast Cancer
June 3, 2009
Phase 3
NCT01664754
Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Stage IV Non-small Cell Lung Cancer
September 2012
Phase 1
NCT00793546
Pfizer
Advanced Breast Cancer
February 2009
Phase 2
NCT00810797
City of Hope Medical Center-National Cancer Institute (NCI)
Breast Cancer
December 2008
Phase 2
NCT00931450
Institut Català d'Oncologia-National Cancer Institute (NCI)
Breast Cancer
March 2009
Phase 1-Phase 2
NCT00905021
Baylor Breast Care Center-Pfizer
Metastatic Breast Cancer
March 2010
Phase 1-Phase 2
NCT01627067
M.D. Anderson Cancer Center-Susan G. Komen Breast Cancer Foundation
Breast Cancer
September 2012
Phase 2
NCT02592746
Samsung Medical Center
Metastatic Breast Cancer
June 2016
Phase 2
NCT01004081
Biogen
Breast Cancer
November 2009
Phase 2
NCT01151046
Merrimack Pharmaceuticals
Her2 Negative Breast Cancer Patients
June 2010
Phase 2
NCT02598557
National Cancer Institute (NCI)
Estrogen Receptor Positive-Postmenopausal-Stage 0 Breast Cancer-Stage I Breast Cancer-Stage IA Breast Cancer-Stage IB Breast Cancer-Stage II Breast Cancer-Stage IIA Breast Cancer-Stage IIB Breast Cancer
December 6, 2016
Phase 2
NCT02007512
Medivation, Inc.-Astellas Pharma Inc
Breast Cancer
December 2013
Phase 2
NCT00038103
Pfizer
Breast Neoplasms
January 2002
Phase 2
NCT01149356
National Cancer Institute (NCI)
Estrogen Receptor Positive-HER2/Neu Negative-Male Breast Carcinoma-Recurrent Breast Carcinoma-Stage IIIB Breast Cancer-Stage IIIC Breast Cancer-Stage IV Breast Cancer
October 2010
Phase 1
NCT02871791
Dana-Farber Cancer Institute-Pfizer
Human Epidermal Growth Factor 2 Negative Carcinoma of Breast-Hormone Receptor (HR)-Positive Breast Cancer
August 24, 2016
Phase 1-Phase 2
NCT02732119
Novartis Pharmaceuticals-Novartis
Breast Cancer
June 14, 2016
Phase 1-Phase 2
NCT00016432
NSABP Foundation Inc-National Cancer Institute (NCI)
Breast Cancer
May 2001
Phase 3
NCT01870505
Memorial Sloan Kettering Cancer Center-Novartis Pharmaceuticals
Metastatic or Locally-advanced Unresectable Breast Cancer
May 2013
Phase 1
NCT02023359
Novartis Healthcare A/S-Novartis
Breast Cancer