Reports from Bristol-Myers Squibb Company Add New Data to Research in Hepatitis C Virus
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NewsRx.com
March 17, 2011
Investigators publish new data in the report 'Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect.' According to recent research from the United States, "The worldwide prevalence of chronic hepatitis C virus (HCV) infection is estimated to be approaching 200 million people. Current therapy relies upon a combination of pegylated interferon-alpha and ribavirin, a poorly tolerated regimen typically associated with less than 50% sustained virological response rate in those infected with genotype 1 virus."
"The development of direct-acting antiviral agents to treat HCV has focused predominantly on inhibitors of the viral enzymes NS3 protease and the RNA-dependent RNA polymerase NS5B. Here we describe the profile of BMS-790052, a small molecule inhibitor of the HCV NS5A protein that exhibits picomolar half-maximum effective concentrations (EC(50)) towards replicons expressing a broad range of HCV genotypes and the JFH-1 genotype 2a infectious virus in cell culture. In a phase I clinical trial in patients chronically infected with HCV, administration of a single 100-mg dose of BMS-790052 was associated with a 3.3 log(10) reduction in mean viral load measured 24 h post-dose that was sustained for an additional 120 h in two patients infected with genotype 1b virus. Genotypic analysis of samples taken at baseline, 24 and 144 h post-dose revealed that the major HCV variants observed had substitutions at amino-acid positions identified using the in vitro replicon system," wrote M. Gao and colleagues, Bristol-Myers Squibb Company (see also Hepatitis C Virus).
The researchers concluded: "These results provide the first clinical validation of an inhibitor of HCV NS5A, a protein with no known enzymatic function, as an approach to the suppression of virus replication that offers potential as part of a therapeutic regimen based on combinations of HCV inhibitors."
Gao and colleagues published their study in Nature (Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature, 2010;465(7294):96-100).
For additional information, contact M. Gao, Bristol-Myers Squibb Research and Development, Dept. of Virology, 5 Research Parkway, Wallingford, Connecticut 06492 USA.
Keywords: City:Wallingford, State:Connecticut, Country:United States, Digestive System Diseases, Flaviviridae Infections, HCV, Hepatitis C Virus, Hepatology, Human Hepatitis, Liver Diseases, RNA Viruses, Viral RNA, Virology.
This article was prepared by Clinical Trials Week editors from staff and other reports. Copyright 2011, Clinical Trials Week via NewsRx.com.
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