Literature DB >> 24602156

Understanding the effect of the HCV polymerase inhibitor mericitabine on early viral kinetics in the phase 2 JUMP-C and PROPEL studies.

Ya-Chi Chen1, Coen Bernaards, Rohit Kulkarni, Sebastian Moreira, Yonghong Zhu, Anna Chan, Ethan Badman, Andrew Ackrill, James Thommes, Patrick F Smith.   

Abstract

AIMS: The aim was to evaluate early viral kinetics in patients receiving mericitabine [hepatitis C virus (HCV) nucleoside polymerase inhibitor] with peginterferon alfa-2a (40KD) and ribavirin in two clinical trials (PROPEL and JUMP-C).
METHODS: We examined rapid virological responses (RVRs; week 4 HCV RNA <15 IU ml(-1) ) and complete early virological responses (cEVR; week 12 HCV RNA <15 IU ml(-1) ) in HCV genotype 1/4-infected patients receiving mericitabine (500 or 1000 mg) or placebo twice daily plus peginterferon alfa-2a and ribavirin.
RESULTS: Among IL28B rs12979860 CC genotype patients receiving 500 or 1000 mg mericitabine or placebo, respectively, RVR rates were 64.3% (95% confidence interval: 38.8-83.7%), 95.1% (83.9-98.7%) and 33.3% (20.2-49.7%), and cEVR rates were 100% (78.5-100%), 100% (91.4-100%) and 80.6% (65.0-90.3%). Among non-CC genotype patients, RVR rates were 26.5% (14.6-43.1%), 52.3% (43.0-61.3%) and 5.7% (2.2-13.8%), and cEVR rates were 76.5% (60.0-87.6%), 84.6% (76.6-90.1%) and 28.6% (19.3-40.1%), respectively. In multiple regression analysis, IL28B genotype (P < 0.0001), mericitabine dose (P < 0.0001) and bodyweight (P = 0.0009) were associated with first-phase (α) slope (change in log10 HCV RNA from baseline to week 1).
CONCLUSIONS: Mericitabine-containing triple therapy reduces the impact of IL28B genotype on RVR and cEVR compared with peginterferon alfa-2a and ribavirin dual therapy. The IL28B genotype, mericitabine dose and bodyweight are the most important factors associated with the α slope, and there is no evidence of a pharmacokinetic drug-drug interaction between mericitabine and ribavirin.
© 2014 The British Pharmacological Society.

Entities:  

Keywords:  hepatitis C virus polymerase inhibitor; mericitabine; pharmacodynamics; pharmacokinetics; ribavirin

Mesh:

Substances:

Year:  2014        PMID: 24602156      PMCID: PMC4243904          DOI: 10.1111/bcp.12369

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  25 in total

Review 1.  Metabolism and antiviral activity of ribavirin.

Authors:  William B Parker
Journal:  Virus Res       Date:  2005-02       Impact factor: 3.303

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3.  A multi-variant, viral dynamic model of genotype 1 HCV to assess the in vivo evolution of protease-inhibitor resistant variants.

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Journal:  PLoS Comput Biol       Date:  2010-04-15       Impact factor: 4.475

4.  Combinations of 2'-C-methylcytidine analogues with interferon-alpha2b and triple combination with ribavirin in the hepatitis C virus replicon system.

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5.  Genetic variation in IL28B predicts hepatitis C treatment-induced viral clearance.

Authors:  Dongliang Ge; Jacques Fellay; Alexander J Thompson; Jason S Simon; Kevin V Shianna; Thomas J Urban; Erin L Heinzen; Ping Qiu; Arthur H Bertelsen; Andrew J Muir; Mark Sulkowski; John G McHutchison; David B Goldstein
Journal:  Nature       Date:  2009-08-16       Impact factor: 49.962

6.  Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species.

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Journal:  J Biol Chem       Date:  2007-08-13       Impact factor: 5.157

7.  Efficacy and safety of peginterferon alfa-2a (40KD) plus ribavirin in hepatitis C patients with advanced fibrosis and cirrhosis.

Authors:  Savino Bruno; Mitchell L Shiffman; Stuart K Roberts; Edward J Gane; Diethelm Messinger; Stephanos J Hadziyannis; Patrick Marcellin
Journal:  Hepatology       Date:  2010-02       Impact factor: 17.425

8.  Diagnosis, management, and treatment of hepatitis C: an update.

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Journal:  Hepatology       Date:  2009-04       Impact factor: 17.425

9.  Mechanism of activation of beta-D-2'-deoxy-2'-fluoro-2'-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase.

Authors:  Eisuke Murakami; Haiying Bao; Mangala Ramesh; Tamara R McBrayer; Tony Whitaker; Holly M Micolochick Steuer; Raymond F Schinazi; Lieven J Stuyver; Aleksandr Obikhod; Michael J Otto; Phillip A Furman
Journal:  Antimicrob Agents Chemother       Date:  2006-11-13       Impact factor: 5.191

10.  GT-1a or GT-1b subtype-specific resistance profiles for hepatitis C virus inhibitors telaprevir and HCV-796.

Authors:  Matthew F McCown; Sonal Rajyaguru; Simran Kular; Nick Cammack; Isabel Nájera
Journal:  Antimicrob Agents Chemother       Date:  2009-03-09       Impact factor: 5.191

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  1 in total

1.  Intracellular effects of the Hepatitis C virus nucleoside polymerase inhibitor RO5855 (Mericitabine Parent) and Ribavirin in combination.

Authors:  H Ma; S Le Pogam; S Fletcher; F Hinojosa-Kirschenbaum; H Javanbakht; J-M Yan; W-R Jiang; N Inocencio; K Klumpp; I Nájera
Journal:  Antimicrob Agents Chemother       Date:  2014-02-18       Impact factor: 5.191

  1 in total

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