Literature DB >> 24666106

MK-5172 : a second-generation protease inhibitor for the treatment of hepatitis C virus infection.

Ivan Gentile1, Antonio Riccardo Buonomo, Federico Borgia, Emanuela Zappulo, Giuseppe Castaldo, Guglielmo Borgia.   

Abstract

INTRODUCTION: Approximately 170 million people worldwide are chronic carriers of the hepatitis C virus (HCV). Twenty-five percent of them develop liver cirrhosis and hepatocellular carcinoma during their life. Successful antiviral treatment dramatically reduces the risk of disease progression. HCV infection is treated with pegylated interferon and ribavirin; the addition of a protease inhibitor (boceprevir or telaprevir) can also be considered for patients with genotype 1. AREAS COVERED: This review summarizes the data about the pharmacokinetics, pharmacodynamics, efficacy and safety of MK-5172 , a second-generation inhibitor of HCV NS3/4A protease. EXPERT OPINION: The pharmacokinetic profile allows for once-a-day administration. Combined with pegylated interferon and ribavirin, MK-5172 results in a high rate of HCV eradication (in about 90% of cases) and a better outcome than boceprevir-based triple therapy. Also in interferon-free combinations, MK-5172-associated eradication rates are very high (89 - 100%). MK-5172 has a higher barrier to resistance than first-generation protease inhibitors and is active against most variants associated with resistance to first-generation protease inhibitors. Tolerability and safety profile are good. Although data are limited, MK-5172 appears to overcome most of the drawbacks of the first-generation protease inhibitors and is thus a very promising agent to be used in combination with other antivirals to eradicate HCV infection.

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Year:  2014        PMID: 24666106     DOI: 10.1517/13543784.2014.902049

Source DB:  PubMed          Journal:  Expert Opin Investig Drugs        ISSN: 1354-3784            Impact factor:   6.206


  9 in total

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Review 3.  Asunaprevir, a protease inhibitor for the treatment of hepatitis C infection.

Authors:  Ivan Gentile; Antonio Riccardo Buonomo; Emanuela Zappulo; Giuseppina Minei; Filomena Morisco; Francesco Borrelli; Nicola Coppola; Guglielmo Borgia
Journal:  Ther Clin Risk Manag       Date:  2014-06-26       Impact factor: 2.423

4.  Potent Antiviral Activities of the Direct-Acting Antivirals ABT-493 and ABT-530 with Three-Day Monotherapy for Hepatitis C Virus Genotype 1 Infection.

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Journal:  Antimicrob Agents Chemother       Date:  2015-12-28       Impact factor: 5.191

Review 5.  New era for management of chronic hepatitis C virus using direct antiviral agents: A review.

Authors:  Tamer Elbaz; Mohamed El-Kassas; Gamal Esmat
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Review 6.  Vertical transmission of hepatitis B virus: challenges and solutions.

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Review 7.  Pharmacokinetics, Efficacy, and Safety of Hepatitis C Virus Drugs in Patients with Liver and/or Renal Impairment.

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Review 8.  Grazoprevir/elbasvir for the treatment of adults with chronic hepatitis C: a short review on the clinical evidence and place in therapy.

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Journal:  Hepat Med       Date:  2018-05-04

9.  Direct acting antivirals treatment for hepatitis C virus infection does not increase the incidence of de novo hepatocellular carcinoma occurrence: Results from an Italian real-life cohort (LINA cohort).

Authors:  Antonio Riccardo Buonomo; Riccardo Scotto; Carmine Coppola; Biagio Pinchera; Giulio Viceconte; Costanza Maria Rapillo; Laura Staiano; Mariarosaria Saturnino; Ferdinando Scarano; Federica Portunato; Mariantonietta Pisaturo; Stefania De Pascalis; Salvatore Martini; Grazia Tosone; Salvatore Nappa; Nicola Coppola; Ivan Gentile
Journal:  Medicine (Baltimore)       Date:  2020-02       Impact factor: 1.817

  9 in total

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