Discovery of MK-1220 (Hepatitis C NS3/4A protease inhibitor)


A recent letter in ACS Med.Chem.Lett. details the optimisation of a series of inhibitors of the Hepatitis C virus (HCV) NS3/4A protease, and is interesting in that it provides detailed pharmacokinetic data for a series of macrocyclic lactones, a class of therapeutic agents with physicochemical properties that fall outside the typical range with which most medicinal chemists are familiar.

The current front line therapy for HCV infection (which can lead to liver cirrhosis) involves treatment with PEGylated interferon α (PEGasys or PEG-Intron, by injection) and ribavirin (orally).  Unfortunately this approach has limited efficacy due, in part, to the low completion rates observed for the lengthy (~1 year) course of therapy.   The clear need for improved therapies and the associated commercial opportunity has led to many companies progressing molecules into the clinic (see this overview of the area), a number of which have targeted NS3/4A protease.   The NS3/4A protease represents…

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