"目录号: HY-14434
Anti-infectionMetabolic Enzyme/Protease-
Asunaprevir 是一种有效的hepatitis C virus (HCV) NS3 protease抑制剂，IC50值为 0.2 nM-3.5 nM。
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生物活性
Description
Asunaprevir is a potenthepatitis C virus (HCV) NS3 proteaseinhibitor, with theIC50of 0.2 nM-3.5 nM.
IC50& Target
IC50: 0.2 nM-3.5 nM (HCV NS3 protease)
In Vitro
In multiple experiments, populations of resistant colonies are markedly reduced when cells are treated with a combination of DCV and Asunaprevir[1]. Asunaprevir (ASV) inhibits the NS3 proteolytic activity of genotype 1a (H77 strain) and genotype 1b (J4L6S strain), with IC50s of 0.7 and 0.3 nM, respectively.?The EC50s of ASV against replicons encoding the NS3 protease domains representing genotypes 1a, 1b, and 4a, range from 1.2 to 4.0 nM[2]. Replicon cells are maintained under selective pressure with asunaprevir at concentrations of 10 and 30 times the EC50values (50 or 150 nM final concentrations, respectively). For genotype 1b resistance selection, replicon cells are maintained in the presence of asunaprevir at 10 or 30 times the EC50values (30 or 90 nM final concentrations, respectively)[3]. Asunaprevir, administered at single or multiple doses of 200 to 600 mg twice daily, is generally well tolerated, achieving rapid and substantial decreases in HCV RNA levels in subjects chronically infected with genotype 1 HCV[4].
In Vivo
Asunaprevir (ASV, 3-15 mg/kg, p.o.) displays a hepatotropic disposition (liver-to-plasma ratios ranging from 40- to 359-fold across species) in several animal species. Twenty-four hours postdose, liver exposures across all species tested are ≥110-fold above the inhibitor EC50observed with HCV genotype-1 replicons[2].
Clinical Trial
Sang Gyune Kim-Seoul National University Boramae Hospital-Severance Hospital-Inha University Hospital-Korea University-Gachon University Gil Medical Center-Hanyang University Seoul Hospital-Ewha Womans University Mokdong Hospital-Bristol-Myers Squibb-Soonchunhyang University Hospital
Chronic Hepatitis C
September 2016
Bristol-Myers Squibb
Hepatitis C
November 2012
Phase 1
Bristol-Myers Squibb
Hepatitis C
February 7, 2012
Kaohsiung Medical University Chung-Ho Memorial Hospital-Chang Gung Memorial Hospital-National Taiwan University Hospital-Taipei Veterans General Hospital, Taiwan-China Medical University Hospital-National Cheng-Kung University Hospital
Hepatitis C
November 2016
Phase 3
National Institutes of Health Clinical Center (CC)-National Institute of Allergy and Infectious Diseases (NIAID)-Bristol-Myers Squibb
HIV-HCV
February 2014
Phase 2
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)-Bristol-Myers Squibb
Hepatitis C Virus Genotype 4 Infection
December 2014
Phase 2
Bristol-Myers Squibb
Hepatitis C
August 2015
Phase 3
Myeong Jun Song-Bristol-Myers Squibb-Soonchunhyang University Hospital-Dankook University-Chungnam National University Hospital-Konyang University Hospital-Eulji University Hospital-Saint Vincent's Hospital, Korea-Konkuk University Hospital-Cheongju St. Mary's Hospital, Cheongju, Korea-Severance Hospital-Korea University Guro Hospital-Eulji General Hospital-The Catholic University of Korea
Hepatitis C
February 2016
Phase 4
Bristol-Myers Squibb
Hepatitis C
February 2014
Phase 3
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)-Bristol-Myers Squibb
Hepatitis C Virus Genotype 4 Infection
November 2013
Phase 2
Bristol-Myers Squibb
Hepatitis C Virus Infection
April 2014
Phase 3
Bristol-Myers Squibb
Hepatitis C
April 2014
Phase 1
Bristol-Myers Squibb
Hepatitis C Virus Infection
November 2012
Phase 3
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)-Bristol-Myers Squibb
HCV-HIV Co-Infection
December 2012
Phase 2
Tainan Municipal Hospital
Hepatitis c
July 2017
Bristol-Myers Squibb
Hepatitis C
January 2012
Phase 3
Bristol-Myers Squibb
Hepatitis C Infection
December 2014
Phase 1
Bristol-Myers Squibb
Hepatitis C
April 2014
Phase 1
Bristol-Myers Squibb
Hepatitis C Virus Infection
September 2011
Phase 2
Bristol-Myers Squibb
Hepatitis C Virus
May 2012
Phase 3
Foundation for Liver Research
Chronic Hepatitis C
February 2014
Phase 3
Bristol-Myers Squibb
Hepatitis C
December 2013
Phase 3
Bristol-Myers Squibb
Hepatitis C Virus
May 2012
Phase 3
Bristol-Myers Squibb
Hepatic Insufficiency
December 2009
Phase 1
Bristol-Myers Squibb
Chronic Hepatitis C
December 2008
Phase 2
Bristol-Myers Squibb
Chronic Hepatitis C
January 2008
Phase 1-Phase 2
Bristol-Myers Squibb
Hepatitis C Infection
April 2010
Phase 2
Bristol-Myers Squibb
Hepatitis C
May 2009
Phase 1
Bristol-Myers Squibb
Hepatitis C Virus
January 2010
Phase 1
Bristol-Myers Squibb
Hepatitis C Virus
February 2010
Phase 2
Bristol-Myers Squibb
Hepatitis C
March 2011
Phase 2
Bristol-Myers Squibb
Chronic Hepatitis C
November 30, 2011
Phase 2
Bristol-Myers Squibb
Chronic Hepatitis C
December 2009
Phase 2
Sang Gyune Kim-Seoul National University Boramae Hospital-Severance Hospital-Inha University Hospital-Korea University-Gachon University Gil Medical Center-Hanyang University Seoul Hospital-Ewha Womans University Mokdong Hospital-Bristol-Myers Squibb-Soonchunhyang University Hospital
Chronic Hepatitis C
September 2016
Bristol-Myers Squibb
Hepatitis C
November 2012
Phase 1
Bristol-Myers Squibb
Hepatitis C
February 7, 2012
Kaohsiung Medical University Chung-Ho Memorial Hospital-Chang Gung Memorial Hospital-National Taiwan University Hospital-Taipei Veterans General Hospital, Taiwan-China Medical University Hospital-National Cheng-Kung University Hospital
Hepatitis C
November 2016
Phase 3
National Institutes of Health Clinical Center (CC)-National Institute of Allergy and Infectious Diseases (NIAID)-Bristol-Myers Squibb
HIV-HCV
February 2014
Phase 2
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)-Bristol-Myers Squibb
Hepatitis C Virus Genotype 4 Infection
December 2014
Phase 2
Bristol-Myers Squibb
Hepatitis C
August 2015
Phase 3
Myeong Jun Song-Bristol-Myers Squibb-Soonchunhyang University Hospital-Dankook University-Chungnam National University Hospital-Konyang University Hospital-Eulji University Hospital-Saint Vincent's Hospital, Korea-Konkuk University Hospital-Cheongju St. Mary's Hospital, Cheongju, Korea-Severance Hospital-Korea University Guro Hospital-Eulji General Hospital-The Catholic University of Korea
Hepatitis C
February 2016
Phase 4
Bristol-Myers Squibb
Hepatitis C
February 2014
Phase 3
French National Institute for Health and Medical Research-French National Agency for Research on AIDS and Viral Hepatitis (Inserm-ANRS)-Bristol-Myers Squibb
Hepatitis C Virus Genotype 4 Infection
November 2013
Phase 2
Bristol-Myers Squibb
Hepatitis C Virus Infection
April 2014
Phase 3
