"目录号: HY-14248
OthersAutophagy-
Letrozole(CGS-20267)是口服的非甾体芳香酶抑制剂。
AromataseAutophagy
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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
NCT00330317
Novartis Pharmaceuticals-Novartis
Breast Cancer
February 2006
Phase 3
NCT02912988
The University of Hong Kong-University of Southampton-Peking University Third Hospital-Chinese PLA General Hospital
Subfertility
November 2016
Phase 3
NCT01577017
Nik Hazlina-University of Science Malaysia
Polycystic Ovarian Syndrome
May 2008
Phase 3
NCT00237133
Novartis Pharmaceuticals-Novartis
Locally Advanced Breast Cancer
March 2003
Phase 4
NCT02470741
University of California, San Francisco
Leiomyoma-Uterine Fibroids
July 2015
Phase 4
NCT00579826
Carol Fabian, MD-Novartis-National Cancer Institute (NCI)-University of Kansas Medical Center
Breast Cancer
October 2006
Phase 2
NCT01219153
Cairo University-Ahmed Elgazzar Hospital
Infertility
September 2008
Phase 2
NCT00332852
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2006
Phase 3
NCT00532272
National Cancer Center, Korea
Metastatic Breast Cancer
October 2005
Phase 2
NCT00237211
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
June 2001
Phase 2
NCT00247663
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
December 1999
Phase 2
NCT03122197
University of Cincinnati
Brain Tumor
May 16, 2017
Early Phase 1
NCT00329940
Novartis Pharmaceuticals-Novartis
Breast Cancer
November 2005
Phase 3
NCT02457312
The University of Hong Kong
Pregnancy
March 2013
Phase 2
NCT01072318
Korean Breast Cancer Study Group
Breast Cancer
January 2010
Phase 4
NCT00505661
M.D. Anderson Cancer Center
Ovarian Cancer-Fallopian Tube Cancer-Peritoneal Cancer
September 2003
Phase 2
NCT02188550
Sinai Hospital of Baltimore
Ovarian Cancer-Endometrial Cancer
June 2014
Phase 2
NCT03008408
M.D. Anderson Cancer Center-Novartis
Malignant Neoplasms of Female Genital Organs-Endometrial Carcinoma
September 2017
Phase 2
NCT02900105
KK Women's and Children's Hospital
Azoospermia, Nonobstructive-Oligozoospermia
February 2015
Phase 3
NCT00237198
Novartis Pharmaceuticals-Chugai Pharmaceutical-Novartis
Postmenopausal Women With Advanced Breast Cancer
March 2004
Phase 2
NCT01035099
Weill Medical College of Cornell University
Breast Cancer-Infertility
November 2009
NCT00004251
NCIC Clinical Trials Group-Canadian Cancer Trials Group
Endometrial Cancer
January 2000
Phase 2
NCT02712723
University of Kansas Medical Center-Novartis Pharmaceuticals
Breast Cancer
February 2016
Phase 2
NCT02670304
First Affiliated Hospital, Sun Yat-Sen University
Ovarian Hyperstimulation Syndrome
January 2012
Phase 4
NCT01232075
Cairo University-Ahmed Elgazzar Hospital
Infertility
September 2008
Phase 2
NCT00263198
Washington University School of Medicine-Novartis
Breast Neoplasms
March 2006
Phase 2
NCT02010021
Dartmouth-Hitchcock Medical Center
Breast Cancer
January 2014
NCT00856050
Dana-Farber Cancer Institute-Brigham and Women's Hospital-Novartis
Leiomyosarcoma
February 2009
Phase 2
NCT01064635
IRCCS Azienda Ospedaliera Universitaria San Martino - IST Istituto Nazionale per la Ricerca sul Cancro, Genoa, Italy
Breast Cancer
August 2005
Phase 3
NCT00549822
Massachusetts General Hospital-Dana-Farber Cancer Institute-Novartis
Breast Cancer
October 2007
Phase 2
NCT00535418
Novartis Pharmaceuticals-Novartis
Breast Cancer
June 2000
Phase 2-Phase 3
NCT01431352
Heilongjiang University of Chinese Medicine
Polycystic Ovary Syndrome
September 2009
NCT00134680
Duke University-Genentech, Inc.-Novartis Pharmaceuticals
Metastatic Breast Cancer
January 2000
Phase 2
NCT00804960
Center for Human Reproduction
Infertility
September 2008
Phase 4
NCT00553410
International Breast Cancer Study Group-Breast International Group
Breast Cancer
August 2007
Phase 3
NCT00688909
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2008
Phase 4
NCT00956267
Mansoura University
Polycystic Ovary Syndrome
August 2006
NCT00280930
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
NCT00171314
Novartis Pharmaceuticals-Novartis
Breast Cancer
March 2004
Phase 3
NCT00894608
Yunyang Medical College
Polycystic Ovarian Syndrome
January 2008
NCT02562118
National University Hospital, Singapore-Eisai Co., Ltd.
Breast Cancer
September 2015
Phase 1-Phase 2
NCT00530868
University of Alabama at Birmingham-Genentech, Inc.-Breast Cancer Research Foundation
Breast Cancer-Cancer of the Breast-Breast Neoplasm
October 2007
Phase 2
NCT00461773
Yale University-Novartis-Genentech, Inc.
Hormone-Sensitive Breast Cancer-Breast Cancer
March 2007
Phase 2
NCT02619162
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
NCT00237224
Novartis Pharmaceuticals-Novartis
Breast Cancer
February 2003
Phase 4
NCT01334762
Mansoura University
Endometriosis
May 2007
NCT00416715
University of Washington-National Cancer Institute (NCI)