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

Daniel Lamarre (), Paul C. Anderson, Murray Bailey, Pierre Beaulieu, Gordon Bolger, Pierre Bonneau, Michael Bös, Dale R. Cameron, Mireille Cartier, Michael G. Cordingley, Anne-Marie Faucher, Nathalie Goudreau, Stephen H. Kawai, George Kukolj, Lisette Lagacé, Steven R. LaPlante, Hans Narjes, Marc-André Poupart, Jean Rancourt, Roel E. Sentjens, Roger St George, Bruno Simoneau, Gerhard Steinmann, Diane Thibeault, Youla S. Tsantrizos, Steven M. Weldon, Chan-Loi Yong and Montse Llinàs-Brunet
Additional contact information
Daniel Lamarre: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Paul C. Anderson: Boehringer Ingelheim (Canada) Ltd
Murray Bailey: Boehringer Ingelheim (Canada) Ltd
Pierre Beaulieu: Boehringer Ingelheim (Canada) Ltd
Gordon Bolger: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Pierre Bonneau: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Michael Bös: Boehringer Ingelheim (Canada) Ltd
Dale R. Cameron: Boehringer Ingelheim (Canada) Ltd
Mireille Cartier: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Michael G. Cordingley: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Anne-Marie Faucher: Boehringer Ingelheim (Canada) Ltd
Nathalie Goudreau: Boehringer Ingelheim (Canada) Ltd
Stephen H. Kawai: Boehringer Ingelheim (Canada) Ltd
George Kukolj: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Lisette Lagacé: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Steven R. LaPlante: Boehringer Ingelheim (Canada) Ltd
Hans Narjes: Clinical Research, Boehringer Ingelheim Pharma KG
Marc-André Poupart: Boehringer Ingelheim (Canada) Ltd
Jean Rancourt: Boehringer Ingelheim (Canada) Ltd
Roel E. Sentjens: Academisch Medisch Center
Roger St George: Boehringer Ingelheim Pharmaceuticals, Inc.
Bruno Simoneau: Boehringer Ingelheim (Canada) Ltd
Gerhard Steinmann: Clinical Research, Boehringer Ingelheim Pharma KG
Diane Thibeault: Departments of Biological Sciences Boehringer Ingelheim (Canada) Ltd
Youla S. Tsantrizos: Boehringer Ingelheim (Canada) Ltd
Steven M. Weldon: Boehringer Ingelheim Pharmaceuticals, Inc.
Chan-Loi Yong: Boehringer Ingelheim Pharmaceuticals, Inc.
Montse Llinàs-Brunet: Boehringer Ingelheim (Canada) Ltd

Nature, 2003, vol. 426, issue 6963, 186-189

Abstract: Abstract 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 mortality1,2,3. Current interferon-based therapies4 are suboptimal especially in patients infected with HCV genotype 1, and they are poorly tolerated, highlighting the unmet medical need for new therapeutics5,6. The HCV-encoded NS3 protease is essential for viral replication7,8 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.

Date: 2003
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DOI: 10.1038/nature02099

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