Ciluprevir (BILN-2061) (Synonyms: BILN 2061; BILN 2061ZW)

Ciluprevir is a selective inhibitor of NS3 protease with IC50 value of 3.0 nM [1].
NS3 (non-structural protein 3) protease is a protein whose C-terminal two-thirds contain a helicase and nucleic acid-stimulated NTPase activities and plays a pivotal role in HCV replication. It is reported that NS3 has regarded as a target to control HCV RNA replication via designing new drugs to inhibit it [2, 3].
Ciluprevir is a NS3 protease inhibitor and has a different affinity with the reported NS3 protease inhibitor VX-950. When using covalent adducts formation method, Svahn Gustafsson S found that ciluprevir showed faster association and slower dissociation kinetics [1].
NS3.4 protease inhibitor ciluprevir has potential for treating chronic HCV and robust antiviral activities have been reported. Furthermore, treatment HCV patients with ciluprevir showed significant HCV RNA reduction in plasma levels in clinical [4].
References:
[1].    Svahn Gustafsson, S., et al., Identification of weak points of hepatitis C virus NS3 protease inhibitors using surface plasmon resonance biosensor-based interaction kinetic analysis and genetic variants. J Med Chem, 2014. 57(5): p. 1802-11.
[2].    Howe, J.A., et al., Clinical Implications of Detectable Baseline Hepatitis C Virus-Genotype 1 NS3/4A-Protease Variants on the Efficacy of Boceprevir Combined With Peginterferon/Ribavirin. Open Forum Infect Dis, 2014. 1(2): p. ofu078.
[3].    Susser, S., et al., Evolution of Hepatitis C Virus Quasispecies during Repeated Treatment with the NS3/4A Protease Inhibitor Telaprevir. Antimicrob Agents Chemother, 2015.
[4].    Goudreau, N. and M. Llinas-Brunet, The therapeutic potential of NS3 protease inhibitors in HCV infection. Expert Opin Investig Drugs, 2005. 14(9): p. 1129-44.