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Anti-infectionMetabolic Enzyme/Protease-
Ombitasvir ?????????HCV NS5A??????????????? HCV ????????? 1-5 ??? 6a ???EC50???????????? 0.82-19.3 pM ??? 366 pM???
相關(guān)產(chǎn)品
Asunaprevir-PSI-7977-Simeprevir-Daclatasvir-Paritaprevir-Telaprevir-Boceprevir-Ledipasvir-MK-5172-Elbasvir-ABT-333-Ribavirin-R-1479-Balapiravir-Artemisinin-
生物活性
Description
Ombitasvir is a potent inhibitor of thehepatitis C virus protein NS5A, withEC50s of 0.82 to 19.3 pM against HCV genotypes 1 to 5 and 366 pM against genotype 6a.
IC50& Target
EC50: 0.82 to 19.3 pM (HCV genotypes 1 to 5), 366 pM (HCV genotype 6a)[1]
In Vitro
Ombitasvir is active against the genotype 2a JFH-1 replicon, with an EC50of 0.82 pM, and the EC50s of ombitasvir are 42 pM and 68 pM against the L28 and F28 variants of this genotype 6a replicon, respectively[1]. In GT1a, variants M28V, L31V, and H58D confers 58- to 243-fold resistance to Ombitasvir. Single variants M28T, Q30R, and Y93C/S confers 800- to 8965-fold resistance, while Y93H/N confers >40000-fold resistance to Ombitasvir[2].
Clinical Trial
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Compensated Cirrhosis
October 2012
Phase 3
AbbVie
Chronic Hepatitis C Infection-Chronic Hepatitis C
April 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
August 2012
Phase 3
AbbVie
Healthy Volunteer
September 2015
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
July 2012
Phase 2
AbbVie
Hepatitis C Virus
January 2014
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C-Hepatitis C Virus (HCV) Infection
March 2011
Phase 2
AbbVie
Absolute Bioavailability
January 2014
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
February 2012
Phase 2
AbbVie
Chronic Hepatitis C Virus
July 2015
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C, Chronic
August 2012
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
Chronic Hepatitis C Infection
December 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
March 2013
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
August 2010
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C Virus
September 2011
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C-Hepatitis C (HCV)-Hepatitis C Genotype 1
October 2011
Phase 2
AbbVie
Hepatitis C Virus Infection-Human Immunodeficiency Virus Infection-Chronic Hepatitis C-Compensated Cirrhosis and Non-cirrhotics
August 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
June 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
March 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
February 25, 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C-Hepatitis C (HCV)-Hepatitis C Genotype 1
December 18, 2012
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 (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection-Compensated Cirrhosis
October 2012
Phase 3
AbbVie
Chronic Hepatitis C Infection-Chronic Hepatitis C
April 2013
Phase 2
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
August 2012
Phase 3
AbbVie
Healthy Volunteer
September 2015
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
July 2012
Phase 2
AbbVie
Hepatitis C Virus
January 2014
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C-Hepatitis C Virus (HCV) Infection
March 2011
Phase 2
AbbVie
Absolute Bioavailability
January 2014
Phase 1
AbbVie (prior sponsor, Abbott)-AbbVie
Chronic Hepatitis C Infection
February 2012
Phase 2
AbbVie
Chronic Hepatitis C Virus
July 2015
Phase 3
AbbVie (prior sponsor, Abbott)-AbbVie
Hepatitis C, Chronic
August 2012
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
Chronic Hepatitis C Infection
December 2013
Phase 3
AbbVie
Chronic Hepatitis C Infection
March 2013
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