"目录号: HY-13613
Dutasteride (GG745)是5α还原酶同工酶抑制剂，还可能因其结构域DHT相似对雄激素受体（AR）产生脱靶效应。
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生物活性
Description
Dutasteride (GG745) is a potent inhibitor of both 5 alpha-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.IC50 Value:Target: 5 alpha-reductasein vitro: Dutasteride inhibited (3)H-T conversion to (3)H-DHT and, as anticipated, inhibited T-induced secretion of PSA and proliferation. However the drug also inhibited DHT-induced PSA secretion and cell proliferation (IC(50) approximately 1 microM). Dutasteride competed for binding the LNCaP cell AR with an IC(50) approximately 1.5 microM. High concentrations of dutasteride (10-50 microM), but not finasteride, in steroid-free medium, resulted in enhanced cell death, possibly by apoptosis [1]. Dutasteride reduces cell viability and cell proliferation in both cell lines tested (androgen-responsive (LNCaP) and androgen-unresponsive (DU145) human prostate cancer (PCa)) [2].in vivo: GG745 has a terminal half-life of approximately 240 hr, and single doses of >10 mg decreased DHT levels significantly more than did single 5-mg doses of finasteride [3]. In placebo treated men without prostate cancer there was an 8.3% median increase in PSA at month 24 compared with -59.5% in those who received dutasteride, using doubled values to correct for dutasteride treatment [4].Toxicity: Dutasteride may affect male fertility and steroid hormone dynamics. Therefore, a 21-day reproduction study was conducted to determine the effects of dutasteride (10, 32 and 100 μg/L) on fish reproduction. Exposure to dutasteride significantly reduced fecundity of fish and affected several aspects of reproductive endocrine functions in both males and females [5].Clinical trial: Bioequivalence Study Of Dutasteride Five 0.1 mg And One 0.5 mg Soft Gelatin Capsules In Healthy Male Volunteers. Phase 1
Clinical Trial
UConn Health-National Institutes of Health (NIH)-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Alcohol Related Disorders-Alcoholism-Alcohol Abuse
April 2006
GlaxoSmithKline
Alopecia
April 2010
University of Colorado, Denver-GlaxoSmithKline
Prostate Cancer
September 2009
Phase 2
University of California, San Francisco
Nonmalignant Neoplasm-Prostate Cancer
June 2005
Sunnybrook Health Sciences Centre-Toronto Sunnybrook Regional Cancer Centre
Prostate Cancer
May 2010
GlaxoSmithKline
Prostatic Hyperplasia
October 25, 2013
Phase 1
North Florida/South Georgia Veterans Health System
Benign Prostatic Hypertrophy
November 2004
UConn Health-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Alcoholism-Alcohol Abuse-Alcohol Dependence
January 2011
Phase 4
GlaxoSmithKline
Prostatic Hyperplasia
September 9, 2015
Phase 1
GlaxoSmithKline
Alopecia
December 15, 2006
Phase 3
National Institute of Neurological Disorders and Stroke (NINDS)-National Institutes of Health Clinical Center (CC)
Kennedy's Disease-Spinal and Bulbar Muscular Atrophy
March 2006
Phase 2
GlaxoSmithKline
Prostatic Hyperplasia
September 10, 2010
Phase 1
GlaxoSmithKline
Neoplasms, Prostate
July 2006
Phase 4
Canadian Urology Research Consortium-GlaxoSmithKline
Prostate Cancer
March 2007
Phase 2-Phase 3
Memorial Sloan Kettering Cancer Center-GlaxoSmithKline-University of Washington
Prostate Cancer-Castration-resistant, Metastatic
March 2009
Phase 2
Beth Israel Deaconess Medical Center-Massachusetts General Hospital-Dana-Farber Cancer Institute-Sunnybrook Health Sciences Centre-Oregon Health and Science University-M.D. Anderson Cancer Center-Sidney Kimmel Comprehensive Cancer Center
Prostate Cancer
February 2005
Phase 2
GlaxoSmithKline
Prostatic Hyperplasia
June 30, 2011
Phase 1
GlaxoSmithKline
Alopecia
April 2013
Phase 3
University of Washington-GlaxoSmithKline-Seattle Institute for Biomedical and Clinical Research-VA Office of Research and Development-Solvay Pharmaceuticals
Hypogonadism-Benign Prostatic Hyperplasia
March 2005
Phase 4
Samsung Medical Center-GlaxoSmithKline
Benign Prostatic Hyperplasia
June 2006
Phase 4
GlaxoSmithKline
Benign Prostatic Hyperplasia-Prostatic Hyperplasia
December 2004
GlaxoSmithKline
Hypogonadism-Hypogonadism, Male
October 2006
Phase 1
GlaxoSmithKline
Prostatic Hyperplasia
November 2003
Phase 3
UConn Health-National Institute on Alcohol Abuse and Alcoholism (NIAAA)
Alcoholism-Alcohol Abuse-Alcohol Dependence
January 2013
Phase 4
GlaxoSmithKline
Prostatic Hyperplasia
June 2012
Phase 4
NorthShore University HealthSystem Research Institute-University of Chicago-Northwestern University
Prostate Cancer
March 2007
Phase 2
Kaunas University of Medicine
Prostate Cancer
April 2007
Phase 3
Stiefel, a GSK Company-GlaxoSmithKline
Alopecia
July 2014
Phase 3
GlaxoSmithKline
Prostatic Hyperplasia
July 30, 2015
Phase 1
GlaxoSmithKline
Urologic Diseases
February 19, 2014
Phase 1
GlaxoSmithKline
Prostatic Hyperplasia
October 2003
Phase 4
GlaxoSmithKline
Prostatic Hyperplasia
August 23, 2012
Phase 1
GlaxoSmithKline
Urologic Diseases
February 11, 2014
Phase 1
Seoul National University Hospital-The Korean Urological Association-GlaxoSmithKline
Benign Prostatic Hyperplasia
January 2008
Phase 4
CHU de Quebec-Universite Laval-GlaxoSmithKline
Prostate Cancer-Erectile Dysfunction-Lower Urinary Tract Symptoms
March 2009
Phase 2
University of Rochester
Prostate Cancer
September 2014
Phase 2
GlaxoSmithKline
Benign Prostatic Hyperplasia-Prostatic Hyperplasia
October 2007
Phase 3
GlaxoSmithKline
Prostatic Hyperplasia
May 12, 2011
Phase 1
GlaxoSmithKline
Prostatic Hyperplasia
February 2006
Phase 3
Mary-Ellen Taplin, MD-Dana-Farber Cancer Institute
Prostate Cancer
September 2011
Phase 2
Sidney Kimmel Cancer Center at Thomas Jefferson University-National Cancer Institute (NCI)
Prostate Cancer
November 2006
Phase 3
GlaxoSmithKline
Hypogonadism-Hypogonadism, Male
October 2006
Phase 2
Siami, Paul F., M.D.-GlaxoSmithKline-Pfizer
Benign Prostatic Hyperplasia (BPH)
July 2009
Phase 4
Yuyu Pharma, Inc.
Benign Prostate Hyperplasia
May 2016
Phase 1
Northwestern University-GlaxoSmithKline
Benign Prostatic Hyperplasia
October 2006
Phase 3
Toni Choueiri, MD-Dana-Farber Cancer Institute
Adenocarcinoma of the Prostate
April 2011
Phase 2
GlaxoSmithKline
Prostatic Hyperplasia
December 2010
Phase 4
GlaxoSmithKline
Prostatic Hyperplasia
November 2011
Phase 1
National Institute of Mental Health (NIMH)-National Institutes of Health Clinical Center (CC)
Premenstrual Syndrome-PMS-Healthy-Depression
March 31, 2004
Phase 1
Urology of Virginia-GlaxoSmithKline
Beni
