The Sound of Evolution
Simeprevir
Mechanism of action:
Simeprevir is a hepatitis C virus NS3/4A protease inhibitor (HCV NS3/4A protease inhibitor). The hepatitis C virus polyprotein requires cleavage by the NS3/4A protease into multiple functional proteins, including NS3, NS4A, NS4B, NS5A, and NS5B. Simeprevir binds with high affinity to the active site of the NS3/4A protease and inhibits its proteolytic activity, preventing the virus from producing mature, functional proteins needed for viral RNA replication and assembly.
Reference(s):
1. Raboisson P et al. (2008). Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350. Bioorg Med Chem Lett.
2. Kanda T et al. (2014). New treatments for genotype 1 chronic hepatitis C - focus on simeprevir. Ther Clin Risk Manag.