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HCV NS3/4A protease complex

In vitro studies identified a macrocyclic acyl sulfonamide-based inhibitor of HCV NS3/4A protease that could help treat drug-resistant HCV infection. In a panel of enzyme inhibition assays, the compound inhibited the NS3/4A protease from 13 HCV strains, including 6 with known resistance mutations, at nanomolar and subnanomolar concentrations. The inhibitor also showed no activity in a panel of seven off-target proteases and had low cytotoxicity in a human hepatocyte cell line. Next steps could include testing the lead inhibitor in models of HCV infection.
Vertex Pharmaceuticals Inc. markets Incivek telaprevir, a small molecule HCV NS3/4A protease inhibitor, to treat HCV infection.
Merck & Co. Inc. markets Victrelis boceprevir, a small molecule HCV NS3/4A protease inhibitor, for the indication.
Boehringer Ingelheim GmbH's faldaprevir, an oral HCV NS3/4A protease inhibitor, is in Phase III testing to treat HCV infection.
At least six other companies have inhibitors of the HCV NS3/4A protease in Phase III testing or earlier to treat HCV infection.

SciBX 6(5); doi:10.1038/scibx.2013.119
Published online Feb. 7, 2013

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O'Meara, J.A. et al. J. Biol. Chem.; published online Dec. 27, 2012;
Contact: Jeff A. O'Meara, Boehringer Ingelheim Ltd. R&D, Laval, Quebec, Canada