"目錄號: HY-13632
Exemestane(FCE 24304)是芳香酶（aromatase）抑制劑，能抑制人胎盤和鼠卵巢芳香酶，IC50分別為30 nM和40 nM。
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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
Hellenic Breast Surgeons Society
Breast Cancer
April 2001
Phase 3
National University Hospital, Singapore
Breast Carcinoma
August 2012
Nordic Society for Gynaecologic Oncology
Endometrial Cancer
March 2004
Phase 2
Actavis Inc.
Healthy
November 2012
Phase 1
Ohio State University Comprehensive Cancer Center-Pfizer
Breast Cancer
July 2003
Phase 2
Tianjin Medical University
Breast Cancer
January 2012
Phase 2-Phase 3
Novartis Pharmaceuticals-Novartis
Oestrogen Receptor Positive Advanced Breast Cancer
January 2013
Phase 4
Syndax Pharmaceuticals
Breast Cancer-Estrogen Receptor-Positive Breast Cancer-Breast Cancer, Estrogen Receptor-Positive-ER+ Breast Cancer
May 2008
Phase 2
Georgetown University-National Cancer Institute (NCI)
Breast Neoplasms
November 2003
Phase 2
Memorial Sloan Kettering Cancer Center-Pharmacia
Breast Cancer
July 1999
Institut Claudius Regaud-PHARMACIA SAS
Breast Neoplasms
January 2002
Phase 2
Chinese Academy of Medical Sciences
Breast Neoplasms
July 2011
Phase 2
Ewa Mrozek-Pfizer-Ohio State University Comprehensive Cancer Center
Breast Cancer
September 2005
Phase 2
National Taiwan University Hospital-Merck Sharp & Dohme Corp.
Premenopausal Breast Cancer
December 2016
Phase 1-Phase 2
Pfizer
Breast Neoplasms
January 2013
Phase 2
Organisation for Oncology and Translational Research
Hormone Receptor Positive Malignant Neoplasm of Breast
Phase 2
Pfizer
Early Breast Cancer
September 2010
Swiss Group for Clinical Cancer Research
Prostate Cancer
August 2001
Phase 2
Bristol-Myers Squibb
Breast Cancer
February 2009
Phase 2
Pfizer
Breast Neoplasms
March 2005
Phase 4
NCIC Clinical Trials Group-Grupo Espanol de Investigacion del Cancer de Mama-UNICANCER-Canadian Cancer Trials Group
Breast Cancer
February 2004
Phase 3
Chipscreen Biosciences, Ltd.
Breast Cancer
July 2015
Phase 3
Masonic Cancer Center, University of Minnesota
Non-Small Cell Lung Cancer
August 2016
Phase 2
Pfizer
Breast Neoplasms
June 2002
Phase 2
New York University School of Medicine
Metastatic Beast Cancer
September 2013
Phase 2
Pfizer
Breast Neoplasms
August 2001
Phase 3
Chinese Academy of Medical Sciences-Cancer Institute and Hospital, Chinese Academy of Medical Sciences
Breast Cancer
December 2015
Phase 2
Syndax Pharmaceuticals
Breast Cancer-Estrogen Receptor Positive Breast Cancer
June 2016
Phase 1
NCIC Clinical Trials Group-Canadian Cancer Trials Group
Breast Cancer
August 2001
Pfizer
Breast Neoplasms
November 2001
Phase 2
Novartis Pharmaceuticals-Novartis
Neoplasms-Breast Neoplasms-Kidney Neoplasms-Pancreatic Neuroendocine Neoplasms
May 2014
Phase 1
Novartis Pharmaceuticals-Novartis
Breast Cancer
June 3, 2009
Phase 3
Jonsson Comprehensive Cancer Center-National Cancer Institute (NCI)
Stage IV Non-small Cell Lung Cancer
September 2012
Phase 1
Pfizer
Advanced Breast Cancer
February 2009
Phase 2
City of Hope Medical Center-National Cancer Institute (NCI)
Breast Cancer
December 2008
Phase 2
Institut Català d'Oncologia-National Cancer Institute (NCI)
Breast Cancer
March 2009
Phase 1-Phase 2
Baylor Breast Care Center-Pfizer
Metastatic Breast Cancer
March 2010
Phase 1-Phase 2
M.D. Anderson Cancer Center-Susan G. Komen Breast Cancer Foundation
Breast Cancer
September 2012
Phase 2
Samsung Medical Center
Metastatic Breast Cancer
June 2016
Phase 2
Biogen
Breast Cancer
November 2009
Phase 2
Merrimack Pharmaceuticals
Her2 Negative Breast Cancer Patients
June 2010
Phase 2
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
Medivation, Inc.-Astellas Pharma Inc
Breast Cancer
December 2013
Phase 2
Pfizer
Breast Neoplasms
January 2002
Phase 2
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
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
Novartis Pharmaceuticals-Novartis
Breast Cancer
June 14, 2016
Phase 1-Phase 2
NSABP Foundation Inc-National Cancer Institute (NCI)
Breast Cancer
May 2001
Phase 3
Memorial Sloan Kettering Cancer Center-Novartis Pharmaceuticals
Metastatic or Locally-advanced Unresectable Breast Cancer
May 2013
Phase 1
Novartis Healthcare A/S-Novartis
Breast Cancer
