"目录号: HY-14248
Letrozole(CGS-20267)是口服的非甾体芳香酶抑制剂。
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生物活性
Description
Letrozole(CGS-20267) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant.Target: AromataseInVitro: Letrozole potently inhibits aromatase derived from a variety of different sources including human placental microsomes, particulate fractions of human breast cancer, rat ovarian microsomes, MCF-7 cells transfected with aromatase (MCF-7Ca), JEG-3 human choriocarcinoma cells, CHO cells, hamster ovarian tissue, and particulate fractions of human breast cancer with IC50 of 11, 2, 7, 0.07, 0.07, 1.4, 20 and 0.8 nM. In the non-cellular systems, the IC50 of letrozole is calculated to be 1-13 nM [1]. Letrozole maximally inhibits estradiol production in vitro in LH-stimulated hamster ovarian tissue at 0.1 μM with an IC50 of 0.02 μM and does not significantly affect progesterone production up to 350 μM. In ACTH-stimulated rat adrenal tissue in vitro, aldosterone production is inhibited by with an IC50 of 210 μM [2].InVivo: Letrozole inhibits aromatase in vivo with ED50 of 1-3 μg/kg p.o. [2]. Letrozole displays anti-endocrine effects. Letrozole inhibits androstenedione-induced uterine hypertrophy in immature rats with ED50 of 1-3 μg/kg. In the adult female rat, Letrozole (0.3-1 mg/kg daily p.o., 14 days) completely interrupts ovarian cyclicity and reduces uterine weight and serum estradiol (E2) concentrations to a similar extent to that seen after ovariectomy [1]. Letrozole induces dose-dependent regression of estrogen-dependent, 9,10-dimethylbenz-a-anthracene (DMBA)-induced mammary tumors in adult female rats. The ED50 for Letrozole is determined to be 10 - 30μg/kg/day, with complete inhibition at a daily dose of 10μg /day [3]. Letrozole produces dose-dependent inhibition of tumor growth of MCF-7 cells transfected with human aromatase gene (MCF-7Ca) implanted athymic nude mice, with complete inhibition at 20 mg/kg per day p.o.[4].
Clinical Trial
Novartis Pharmaceuticals-Novartis
Breast Cancer
February 2006
Phase 3
The University of Hong Kong-University of Southampton-Peking University Third Hospital-Chinese PLA General Hospital
Subfertility
November 2016
Phase 3
Nik Hazlina-University of Science Malaysia
Polycystic Ovarian Syndrome
May 2008
Phase 3
Novartis Pharmaceuticals-Novartis
Locally Advanced Breast Cancer
March 2003
Phase 4
University of California, San Francisco
Leiomyoma-Uterine Fibroids
July 2015
Phase 4
Carol Fabian, MD-Novartis-National Cancer Institute (NCI)-University of Kansas Medical Center
Breast Cancer
October 2006
Phase 2
Cairo University-Ahmed Elgazzar Hospital
Infertility
September 2008
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2006
Phase 3
National Cancer Center, Korea
Metastatic Breast Cancer
October 2005
Phase 2
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
June 2001
Phase 2
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
December 1999
Phase 2
University of Cincinnati
Brain Tumor
May 16, 2017
Early Phase 1
Novartis Pharmaceuticals-Novartis
Breast Cancer
November 2005
Phase 3
The University of Hong Kong
Pregnancy
March 2013
Phase 2
Korean Breast Cancer Study Group
Breast Cancer
January 2010
Phase 4
M.D. Anderson Cancer Center
Ovarian Cancer-Fallopian Tube Cancer-Peritoneal Cancer
September 2003
Phase 2
Sinai Hospital of Baltimore
Ovarian Cancer-Endometrial Cancer
June 2014
Phase 2
M.D. Anderson Cancer Center-Novartis
Malignant Neoplasms of Female Genital Organs-Endometrial Carcinoma
September 2017
Phase 2
KK Women's and Children's Hospital
Azoospermia, Nonobstructive-Oligozoospermia
February 2015
Phase 3
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
March 2004
Phase 2
Weill Medical College of Cornell University
Breast Cancer-Infertility
November 2009
NCIC Clinical Trials Group-Canadian Cancer Trials Group
Endometrial Cancer
January 2000
Phase 2
University of Kansas Medical Center-Novartis Pharmaceuticals
Breast Cancer
February 2016
Phase 2
First Affiliated Hospital, Sun Yat-Sen University
Ovarian Hyperstimulation Syndrome
January 2012
Phase 4
Cairo University-Ahmed Elgazzar Hospital
Infertility
September 2008
Phase 2
Washington University School of Medicine-Novartis
Breast Neoplasms
March 2006
Phase 2
Dartmouth-Hitchcock Medical Center
Breast Cancer
January 2014
Dana-Farber Cancer Institute-Brigham and Women's Hospital-Novartis
Leiomyosarcoma
February 2009
Phase 2
IRCCS Azienda Ospedaliera Universitaria San Martino - IST Istituto Nazionale per la Ricerca sul Cancro, Genoa, Italy
Breast Cancer
August 2005
Phase 3
Massachusetts General Hospital-Dana-Farber Cancer Institute-Novartis
Breast Cancer
October 2007
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
June 2000
Phase 2-Phase 3
Heilongjiang University of Chinese Medicine
Polycystic Ovary Syndrome
September 2009
Duke University-Genentech, Inc.-Novartis Pharmaceuticals
Metastatic Breast Cancer
January 2000
Phase 2
Center for Human Reproduction
Infertility
September 2008
Phase 4
International Breast Cancer Study Group-Breast International Group
Breast Cancer
August 2007
Phase 3
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2008
Phase 4
Mansoura University
Polycystic Ovary Syndrome
August 2006
Dana-Farber Cancer Institute-Beth Israel Deaconess Medical Center-Brigham and Women's Hospital-Massachusetts General Hospital
Post-Menopausal-Breast Cancer
October 2005
Phase 2
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2004
Phase 3
Yunyang Medical College
Polycystic Ovarian Syndrome
January 2008
National University Hospital, Singapore-Eisai Co., Ltd.
Breast Cancer
September 2015
Phase 1-Phase 2
University of Alabama at Birmingham-Genentech, Inc.-Breast Cancer Research Foundation
Breast Cancer-Cancer of the Breast-Breast Neoplasm
October 2007
Phase 2
Yale University-Novartis-Genentech, Inc.
Hormone-Sensitive Breast Cancer-Breast Cancer
March 2007
Phase 2
Centro Nacional de Investigaciones Oncologicas CARLOS III-Dr. Miguel Angel Quintela Fandiño (CNIO)-Dr, Ramón Colomer i Bosch-FUNDACIÓN CRIS (Marta Cardona) as promotor
Breast Cancer
July 2015
Phase 1
Novartis Pharmaceuticals-Novartis
Breast Cancer
February 2003
Phase 4
Mansoura University
Endometriosis
May 2007
University of Washington-National Cancer Institute (NCI)
