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An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

Author:
Lamarre, D  Anderson, PC  Bailey, M  Beaulieu, P  Bolger, G  Bonneau, P  Bos, M  Cameron, DR  Cartier, M  Cordingley, MG  Faucher, AM  Goudreau, N  Kawai, SH  Kukolj, G  Lagace, L  LaPlante, SR  Narjes, H  Poupart, MA  Rancourt, J  Sentjens, RE  St George, R  Simoneau, B  Steinmann, G  Thibeault, D  Tsantrizos, YS  Weldon, SM  Yong, CL  Llinas-Brunet, M  


Journal:
NATURE


Issue Date:
2003


Abstract(summary):

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(1-3). Current interferon-based therapies(4) are suboptimal especially in patients infected with HCV genotype 1, and they are poorly tolerated, highlighting the unmet medical need for new therapeutics(5,6). The HCV-encoded NS3 protease is essential for viral replication(7,8) 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.


Page:
186---189


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