Hepatitis C virus (HCV) is a single-stranded positive RNA virus in the Flaviviridae family, which includes several non-structural proteins (NS1, NS2, NS3, NS4a, NS5a, and NS5b). The NS3 protein possesses serine protease activity and is considered essential for viral replication and infectivity. So far, there is about 3-5% of population infected with HCV worldwide. This presentation discloses the toxicity and PK results of some highly potent HCV inhibitors with new macropolycyclic based structure.  Currently, several novel macropolycyclic HCV inhibitors have been determined to show not only very potent (IC50 and EC50 for Ia, Ib, and IIa of NS3-NS4A: 0.1nM-10.0nM) but also non-toxic and competitive or better PK results in comparison with other reported HCV inhibitors such as ITMN-191 (R-7227) and MK-7009 in clinical Phase-II. Furthermore, preclinical study is ongoing and looking forward to discover 2-3 highly competitive HCV inhibitors for further clinical trial.

Development of new non-toxic HCV inhibitors with high efficacy and good PK

243rd National Meeting (2012)

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