Telaprevir-d4 is intended for use as an internal standard for the quantification of telaprevir by GC- or LC-MS. Telaprevir is an inhibitor of hepatitis C virus (HCV) nonstructural protease 3/4A (NS3/4A; Ki = 7 nM).1 It inhibits viral replication in genotype 1b HCV replicon cells and isolated human fetal hepatocytes infected with genotype 1a HCV-positive patient sera (IC50s = 354 and 280 nM, respectively). Telaprevir (10-300 mg/kg) reduces plasma levels of a secreted placental alkaline phosphatase (SEAP) reporter gene in a mouse model of HCV NS3/4A protease activity. Formulations containing telaprevir have been used in the treatment of HCV.
1.Perni, R.B., Almquist, S.J., Byrn, R.A., et al.Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine proteaseAntimicrob. Agents Chemother.50(3)899-909(2006)