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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
6963
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pubmed:dateCreated |
2003-11-17
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pubmed:abstractText |
Hepatitis C virus (HCV) infection is a serious cause of chronic liver disease worldwide with more than 170 million infected individuals at risk of developing significant morbidity and mortality. Current interferon-based therapies are suboptimal especially in patients infected with HCV genotype 1, and they are poorly tolerated, highlighting the unmet medical need for new therapeutics. The HCV-encoded NS3 protease is essential for viral replication and has long been considered an attractive target for therapeutic intervention in HCV-infected patients. Here we identify a class of specific and potent NS3 protease inhibitors and report the evaluation of BILN 2061, a small molecule inhibitor biologically available through oral ingestion and the first of its class in human trials. Administration of BILN 2061 to patients infected with HCV genotype 1 for 2 days resulted in an impressive reduction of HCV RNA plasma levels, and established proof-of-concept in humans for an HCV NS3 protease inhibitor. Our results further illustrate the potential of the viral-enzyme-targeted drug discovery approach for the development of new HCV therapeutics.
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pubmed:commentsCorrections |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Antiviral Agents,
http://linkedlifedata.com/resource/pubmed/chemical/Carbamates,
http://linkedlifedata.com/resource/pubmed/chemical/Macrocyclic Compounds,
http://linkedlifedata.com/resource/pubmed/chemical/NS3 protein, hepatitis C virus,
http://linkedlifedata.com/resource/pubmed/chemical/Polyproteins,
http://linkedlifedata.com/resource/pubmed/chemical/Quinolines,
http://linkedlifedata.com/resource/pubmed/chemical/Serine Proteinase Inhibitors,
http://linkedlifedata.com/resource/pubmed/chemical/Thiazoles,
http://linkedlifedata.com/resource/pubmed/chemical/Viral Nonstructural Proteins,
http://linkedlifedata.com/resource/pubmed/chemical/Viral Proteins
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pubmed:status |
MEDLINE
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pubmed:month |
Nov
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pubmed:issn |
1476-4687
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pubmed:author |
pubmed-author:AndersonPaul CPC,
pubmed-author:BösMichaelM,
pubmed-author:BaileyMurrayM,
pubmed-author:BeaulieuPierreP,
pubmed-author:BolgerGordonG,
pubmed-author:BonneauPierreP,
pubmed-author:CameronDale RDR,
pubmed-author:CartierMireilleM,
pubmed-author:CordingleyMichael GMG,
pubmed-author:FaucherAnne-MarieAM,
pubmed-author:GoudreauNathalieN,
pubmed-author:KawaiStephen HSH,
pubmed-author:KukoljGeorgeG,
pubmed-author:LaPlanteSteven RSR,
pubmed-author:LagacéLisetteL,
pubmed-author:LamarreDanielD,
pubmed-author:Llinàs-BrunetMontseM,
pubmed-author:NarjesHansH,
pubmed-author:PoupartMarc-AndréMA,
pubmed-author:RancourtJeanJ,
pubmed-author:SentjensRoel ERE,
pubmed-author:SimoneauBrunoB,
pubmed-author:St GeorgeRogerR,
pubmed-author:SteinmannGerhardG,
pubmed-author:ThibeaultDianeD,
pubmed-author:TsantrizosYoula SYS,
pubmed-author:WeldonSteven MSM,
pubmed-author:YongChan-LoiCL
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pubmed:issnType |
Electronic
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pubmed:day |
13
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pubmed:volume |
426
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
186-9
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:14578911-Administration, Oral,
pubmed-meshheading:14578911-Antiviral Agents,
pubmed-meshheading:14578911-Carbamates,
pubmed-meshheading:14578911-Double-Blind Method,
pubmed-meshheading:14578911-Hepacivirus,
pubmed-meshheading:14578911-Hepatitis C,
pubmed-meshheading:14578911-Humans,
pubmed-meshheading:14578911-Macrocyclic Compounds,
pubmed-meshheading:14578911-Male,
pubmed-meshheading:14578911-Polyproteins,
pubmed-meshheading:14578911-Protein Processing, Post-Translational,
pubmed-meshheading:14578911-Quinolines,
pubmed-meshheading:14578911-Serine Proteinase Inhibitors,
pubmed-meshheading:14578911-Thiazoles,
pubmed-meshheading:14578911-Viral Load,
pubmed-meshheading:14578911-Viral Nonstructural Proteins,
pubmed-meshheading:14578911-Viral Proteins
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pubmed:year |
2003
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pubmed:articleTitle |
An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus.
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pubmed:affiliation |
Department of Biological Sciences Boehringer Ingelheim (Canada) Ltd, Laval, Québec, H7S 2G5, Canada. dlamarre@lav.boehringer-ingelheim.com
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial,
Controlled Clinical Trial,
Research Support, Non-U.S. Gov't,
Clinical Trial, Phase I
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