2. Academic Validation
  3. An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

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

  • Nature. 2003 Nov 13;426(6963):186-9. doi: 10.1038/nature02099.
Daniel Lamarre 1,  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,  Montse Llinàs-Brunet
Affiliations

Affiliation

  • 1 Department of Biological Sciences Boehringer Ingelheim (Canada) Ltd, Laval, Québec, H7S 2G5, Canada. dlamarre@lav.boehringer-ingelheim.com
PMID: 14578911 DOI: 10.1038/nature02099
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 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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