ArticleAntimicrobial agents and chemotherapy2010
MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease.
Article in Antimicrobial agents and chemotherapy, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 49 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
49 citing papers in PubMed.
- Single-Dose and Multiple-Dose Pharmacokinetics of Vaniprevir in Healthy Men.Clinical and translational science · 2017Trial
- Vaniprevir plus peginterferon alfa-2b and ribavirin in treatment-naive Japanese patients with hepatitis C virus genotype 1 infection: a randomized phase III study.Journal of gastroenterology · 2016Trial
- Vaniprevir plus peginterferon alfa-2a and ribavirin in treatment-experienced Japanese patients with hepatitis C virus genotype 1 infection: a randomized phase II study.Journal of gastroenterology · 2015Trial
- Liver-to-plasma vaniprevir (MK-7009) concentration ratios in HCV-infected patients.Antiviral therapy · 2015Trial
- Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.Antimicrobial agents and chemotherapy · 2012Trial
- Unraveling the therapeutic landscape of approved non-peptide macrocycles.Acta pharmaceutica Sinica. B · 2025Review
- An orally bioavailable SARS-CoV-2 main protease inhibitor exhibits improved affinity and reduced sensitivity to mutations.Science translational medicine · 2024Article
- Article
- Preclinical evaluation of Amphihevir, a first-in-class clinical Hepatitis C virus NS4B inhibitor.Antimicrobial agents and chemotherapy · 2019Article
- Complex macrocycle exploration: parallel, heuristic, and constraint-based conformer generation using ForceGen.Journal of computer-aided molecular design · 2019Article
- Resistance outside the substrate envelope: hepatitis C NS3/4A protease inhibitors.Critical reviews in biochemistry and molecular biology · 2019Review
- Resistance detection and re-treatment options in hepatitis C virus-related chronic liver diseases after DAA-treatment failure.Infection · 2018Review
- ForceGen 3D structure and conformer generation: from small lead-like molecules to macrocyclic drugs.Journal of computer-aided molecular design · 2017Article
- New directions for protease inhibitors directed drug discovery.Biopolymers · 2016Review
- Role of Marine Natural Products in the Genesis of Antiviral Agents.Chemical reviews · 2015Review
- Policresulen, a novel NS2B/NS3 protease inhibitor, effectively inhibits the replication of DENV2 virus in BHK-21 cells.Acta pharmacologica Sinica · 2015Article
- LC-ESI-MS/MS analysis and pharmacokinetics of GP205, an innovative potent macrocyclic inhibitor of hepatitis C virus NS3/4A protease in rats.Molecules (Basel, Switzerland) · 2015Article
- Hepatitis C virus molecular evolution: transmission, disease progression and antiviral therapy.World journal of gastroenterology · 2014Review
- Structural analysis of asunaprevir resistance in HCV NS3/4A protease.ACS chemical biology · 2014Article
- Kinetic analyses reveal potent and early blockade of hepatitis C virus assembly by NS5A inhibitors.Gastroenterology · 2014Article
Corrections and comments
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Authors and funding
14 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The administration of hepatitis C virus (HCV) NS3/4A protease inhibitors to patients with chronic HCV infections has demonstrated that they have dramatic antiviral effects and that compounds acting via this mechanism are likely to form a key component of future anti-HCV therapy. We report here on the preclinical profile of MK-7009, an inhibitor of genotype 1a and 1b proteases at subnanomolar concentrations with modestly shifted potency against genotype 2a and 2b proteases at low nanomolar concentrations. Potent activity was also observed in a cell-based HCV replicon assay in the presence of added human serum (50%). In multiple species evaluated in preclinical studies, the MK-7009 concentrations in the liver were maintained at a significant multiple of the cell-based replicon 50% effective concentration over 12 to 24 h following the administration of moderate oral doses (5 to 10 mg per kg of body weight). MK-7009 also had excellent selectivity against both a range of human proteases and a broad panel of pharmacologically relevant ion channels, receptors, and enzymes. On the basis of this favorable profile, MK-7009 was selected for clinical development and is currently being evaluated in controlled clinical trials with both healthy volunteers and HCV-infected patients.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.