title: Simeprevir: a macrocyclic HCV protease inhibitor.
abstract: Simeprevir is a macrocyclic NS3/4A HCV protease inhibitor with potent activity against genotypes 1, 2, 4, 5 and 6 of the hepatitis C virus (HCV). Phase II and III studies of simeprevir combined with pegylated interferon (peg-IFN) and ribavirin (RBV) demonstrated that the combination was safe and effective in HCV genotype 1 patients, with more than 75% of treatment-naive patients attaining a sustained virological response (SVR). Simeprevir is administered once daily as a single 150-mg capsule. It has a moderate drug interaction potential, but less than that of the first-generation HCV protease inhibitors. Based on positive results from the product's phase III clinical program, simeprevir was approved and launched in Japan, the U.S. and Canada in late 2013 for use in combination with peg-IFN/RBV in HCV genotype 1 infections. Phase II interferon-free studies of simeprevir are ongoing.
authors: Institute of Human Virology and Division of Infectious Diseases, University of Maryland Medical Center, Baltimore, Maryland, USA.
authors: R
authors: R
authors: Talwani
authors: Department of Pharmacy Services, University of Maryland Medical Center, Baltimore, Maryland, USA.
authors: E L
authors: EL
authors: Heil
authors: Institute of Human Virology and Division of Infectious Diseases, University of Maryland Medical Center, Baltimore, Maryland, USA.
authors: B L
authors: BL
authors: Gilliam
authors: Division of Infectious Diseases, Mayo Clinic, Rochester, Minnesota, USA. temesgen.zelalem@mayo.edu.
authors: Z
authors: Z
authors: Temesgen
mesh_terms: D000998:Antiviral Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D017277:Drug Approval; D004347:Drug Interactions; D004359:Drug Therapy, Combination; D005838:Genotype; D016174:Hepacivirus / Q000235:genetics / Q000302:isolation & purification; D006526:Hepatitis C / Q000188:drug therapy* / Q000821:virology; D006575:Heterocyclic Compounds, 3-Ring / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D011480:Protease Inhibitors / Q000627:therapeutic use; D000069616:Simeprevir; D013449:Sulfonamides / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*
chemical_list: D000998:Antiviral Agents; D006575:Heterocyclic Compounds, 3-Ring; D011480:Protease Inhibitors; D013449:Sulfonamides; D000069616:Simeprevir
keywords: GT-1; Hepatitis C virus; Macrolide; Simeprevir; TMC-435