Thursday, February 7, 2013
This week in
HCV NS3/4A protease complex
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.
Pharmaceuticals Inc. markets Incivek
telaprevir, a small molecule HCV NS3/4A protease inhibitor, to
treat HCV infection.
& Co. Inc. markets Victrelis
boceprevir, a small molecule HCV NS3/4A protease inhibitor, for
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.
Published online Feb. 7, 2013
Patent and licensing status
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
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