"目錄號: HY-13998
ABT-333 是一種非核苷抑制劑龙巨,抑制RNA依賴性的HCV NS5B基因編碼的 RNA 聚合酶吓蘑,抑制 HCV 基因型 1a 和 1b 臨床分離株衍生的重組 NS5B 聚合酶训枢,IC50為 2.2 到 10.7 nM。
相關(guān)產(chǎn)品
Asunaprevir-PSI-7977-Simeprevir-Daclatasvir-Paritaprevir-Telaprevir-Boceprevir-Ledipasvir-Ombitasvir-MK-5172-Elbasvir-Ribavirin-R-1479-Balapiravir-Artemisinin-
生物活性
Description
ABT-333 is a nonnucleoside inhibitor of the RNA-dependent RNA polymerase encoded by theHCV NS5Bgene, inhibits recombinant NS5B polymerases derived from HCV genotype 1a and 1b clinical isolates, withIC50between 2.2 and 10.7 nM.
IC50& Target
IC50: 2.2-10.7 nM (NS5B polymerase)[1]
In Vitro
ABT-333 (Dasabuvir) is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases. ABT-333 (Dasabuvir) inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC50s between 2.2 and 10.7 nM. ABT-333 inhibits replication of HCV subgenomic replicons in cell culture assays, with EC50values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC50s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively[1].
Clinical Trial
AbbVie
Relative Bioavailability
November 2013
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Compensated Cirrhosis
October 2012
Phase 3
AbbVie
Healthy Volunteer
September 2015
Phase 1
Abbott
HCV Infection
April 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
August 2012
Phase 3
Abbott
HCV Infection
May 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
HCV Infection
August 2008
Phase 2
AbbVie
Chronic Hepatitis C Infection-Chronic Hepatitis C
April 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Virus Infection
March 2009
Phase 2
Abbott-Abbott Japan Co.,Ltd
HCV Infections
June 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Hepatitis C-Hepatitis C Virus
February 2011
Phase 2
AbbVie
Chronic Hepatitis C Virus (HCV) Infection Genotype 1
June 12, 2014
Phase 3
AbbVie
Chronic Hepatitis C Virus (HCV) Infection Genotype 1
October 30, 2014
Phase 3
AbbVie
Chronic Hepatitis C Virus
July 16, 2015
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
December 2012
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C-HCV-Chronic Hepatitis C Infection-Hepatitis C Genotype 1
March 2010
Phase 2
AbbVie
Chronic Hepatitis C Infection
March 2013
Phase 3
AbbVie
Chronic Hepatitis C Virus
July 2015
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
November 2012
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
November 2012
Phase 3
Abbott
HCV Infection
June 2008
Phase 1
Abbott
HCV Infection
October 2008
Phase 1
AbbVie
Hepatitis C Virus Infection-Human Immunodeficiency Virus Infection-Chronic Hepatitis C-Compensated Cirrhosis and Non-cirrhotics
August 2013
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C-Hepatitis C (HCV)-Hepatitis C Genotype 1
October 2011
Phase 2
AbbVie
Chronic Hepatitis C Infection
June 2013
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
February 2012
Phase 2
AbbVie
Chronic Hepatitis C Infection
March 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
February 25, 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C
June 2013
Phase 3
AbbVie
Chronic Hepatitis C-Hepatitis C Virus-Compensated Cirrhosis
November 2013
Phase 2
Ottawa Hospital Research Institute-AbbVie
Hepatitis C
July 2015
Phase 4
AbbVie
Relative Bioavailability
November 2013
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Compensated Cirrhosis
October 2012
Phase 3
AbbVie
Healthy Volunteer
September 2015
Phase 1
Abbott
HCV Infection
April 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
August 2012
Phase 3
Abbott
HCV Infection
May 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
HCV Infection
August 2008
Phase 2
AbbVie
Chronic Hepatitis C Infection-Chronic Hepatitis C
April 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Virus Infection
March 2009
Phase 2
Abbott-Abbott Japan Co.,Ltd
HCV Infections
June 2009
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Hepatitis C-Hepatitis C Virus
February 2011
Phase 2
AbbVie
Chronic Hepatitis C Virus (HCV) Infection Genotype 1
June 12, 2014
Phase 3
AbbVie
Chronic Hepatitis C Virus (HCV) Infection Genotype 1
October 30, 2014
Phase 3
AbbVie
Chronic Hepatitis C Virus
July 16, 2015
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
December 2012
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C-HCV-Chronic Hepatitis C Infection-Hepatitis C Genotype 1
March 2010
Phase 2
AbbVie
Chronic Hepatitis C Infection
March 2013
Phase 3
AbbVie
Chronic Hepatitis C Virus
July 2015
Phase 3