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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2005-4-5
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pubmed:abstractText |
BILN-2061, a specific and potent peptidomimetic inhibitor of the HCV NS3 protease, has recently been shown to markedly lower serum hepatitis C virus (HCV)-RNA levels in patients chronically infected with HCV genotype 1 in three 2-day proof of principle studies. The aim of the current study was to assess the antiviral efficacy of BILN-2061 in patients with genotypes 2 and 3 HCV infection. The antiviral efficacy, pharmacokinetics, and tolerability of 500 mg twice-daily BILN-2061 given as monotherapy for 2 days in 10 patients chronically infected with non-genotype 1 HCV (genotype 2: n = 3; genotype 3: n =7) and minimal liver fibrosis (Ishak score 0-2) were assessed in a placebo-controlled (placebo n = 2), double-blind pilot study. HCV-RNA levels decreased by > or =1 log(10) copies/mL in 4 of 8 patients treated with BILN-2061. One patient showed a weak response of <1 log(10) copies/mL. Three of 8 treated patients showed no response. There was no correlation between baseline viral concentration or genotype and response. BILN-2061 exhibited good systemic exposure after oral administration and was well tolerated. In conclusion, the antiviral efficacy of the HCV serine protease inhibitor BILN-2061 is less pronounced and more variable in patients with HCV genotype 2 or 3 infection compared with previous results in patients with HCV genotype 1. A lower affinity of BILN-2061 for the NS3 protease of genotypes 2 and 3 HCV is most likely a major contributor to these findings.
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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 |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0270-9139
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
41
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
832-5
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:15732092-Administration, Oral,
pubmed-meshheading:15732092-Adult,
pubmed-meshheading:15732092-Carbamates,
pubmed-meshheading:15732092-Double-Blind Method,
pubmed-meshheading:15732092-Drug Administration Schedule,
pubmed-meshheading:15732092-Female,
pubmed-meshheading:15732092-Genotype,
pubmed-meshheading:15732092-Hepacivirus,
pubmed-meshheading:15732092-Hepatitis C, Chronic,
pubmed-meshheading:15732092-Humans,
pubmed-meshheading:15732092-Kinetics,
pubmed-meshheading:15732092-Macrocyclic Compounds,
pubmed-meshheading:15732092-Male,
pubmed-meshheading:15732092-Middle Aged,
pubmed-meshheading:15732092-Pilot Projects,
pubmed-meshheading:15732092-Prospective Studies,
pubmed-meshheading:15732092-Quinolines,
pubmed-meshheading:15732092-Serine Proteinase Inhibitors,
pubmed-meshheading:15732092-Thiazoles,
pubmed-meshheading:15732092-Viral Load,
pubmed-meshheading:15732092-Viral Nonstructural Proteins
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pubmed:year |
2005
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pubmed:articleTitle |
Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C.
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pubmed:affiliation |
Ruhr-Universität Bochum, Bochum, Germany. markus.reiser@rub.de
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pubmed:publicationType |
Journal Article,
Clinical Trial,
Randomized Controlled Trial,
Research Support, Non-U.S. Gov't,
Multicenter Study
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