742
Views
43
CrossRef citations to date
0
Altmetric
Drug Evaluations

Ledipasvir: a novel synthetic antiviral for the treatment of HCV infection

, MD, , , &

Bibliography

  • WHO. Hepatitis C. 2013. Available from: http://www.who.int/mediacentre/factsheets/fs164/en/index.html [Last accessed 17 January 2014]
  • Carney K, Dhalla S, Aytaman A, et al. Association of tattooing and hepatitis C virus infection: a multicenter case-control study. Hepatology 2013;57:2117-23
  • Coppola N, Pisapia R, Tonziello G, et al. Improvement in the aetiological diagnosis of acute hepatitis C: a diagnostic protocol based on the anti-HCV-IgM titre and IgG Avidity Index. J Clin Virol 2009;46:222-9
  • Petruzziello A, Coppola N, Diodato AM, et al. Age and gender distribution of hepatitis C virus genotypes in the metropolitan area of Naples. Intervirology 2013;56:206-12
  • Coppola N, Pisapia R, Marrocco C, et al. Anti-HCV IgG avidity index in acute hepatitis. C, J Clin Virol 2007;40:110-15
  • Gentile I, De Stefano A, Di Flumeri G, et al. Concomitant interferon-alpha and chemotherapy in hepatitis C and colorectal cancer: a case report. In Vivo 2013;27:527-9
  • Bourlière M, Poordad F, Vrijens B, et al. High medication adherence in HCV-infected patients taking a triple-DAA regimen for 12 weeks. Hepatology 2013;58:740A
  • Gentile I, Di Flumeri G, Scarica S, et al. Acute hepatitis C in patients undergoing hemodialysis: experience with high-dose interferon therapy. Minerva Urol Nefrol 2013;65:83-4
  • Gentile I, Coppola N, Pasquale G, et al. A simple noninvasive score based on routine parameters can predict liver cirrhosis in patients with chronic Hepatitis C. Hepat Mon 2013;13:e8352
  • Zampino R CN, Cirillo G, Boemio A, et al. Abdominal fat interacts with PNPLA3 I148M, but not with the APOC3 variant in the pathogenesis of liver steatosis in chronic hepatitis C. J Viral Hep 2013;20(8):517-23
  • Sagnelli E, Pisaturo M, Stanzione M, et al. Presentation, outcomes, and response to therapy among patients with acute exacerbation of chronic hepatitis C. Clin Gastroenterol Hepatol 2013;13:00466-7
  • Coppola N, Zampino R, Bellini G, et al. Association between a polymorphism in cannabinoid receptor 2 and severe necroinflammation in patients with chronic hepatitis C. Clin Gastroenterol Hepatol 2013;21:00687-3
  • Gentile I, Meola M, Buonomo AR, et al. Human platelet antigen-3 genotype predicts platelet count in patients with HCV infection. In Vivo 2013;27:773-7
  • Maasoumy B, Wedemeyer H. Natural history of acute and chronic hepatitis C. Best Pract Res Clin Gastroenterol 2012;26:401-12
  • Coppola N, Gentile I, Pasquale G, et al. Anti-HBc positivity was associated with histological cirrhosis in patients with chronic hepatitis C. Ann Hepatol 2014;13:20-6
  • Ferrari SM, Fallahi P, Mancusi C, et al. HCV-related autoimmune disorders in HCV chronic infection. Clin Ter 2013;164:e305-12
  • Coppola N, Pisaturo M, Guastafierro S, et al. Increased hepatitis C viral load and reactivation of liver disease in HCV RNA-positive patients with onco-haematological disease undergoing chemotherapy. Dig Liver Dis 2012;44:49-54
  • Fusco F, D'Anzeo G, Rossi A, et al. Erectile dysfunction in patients with chronic viral hepatitis: a systematic review of the literature. Expert Opin Pharmacother 2013;14:2533-44
  • Morisco F, Granata R, Stroffolini T, et al. Sustained virological response: a milestone in the treatment of chronic hepatitis C. World J Gastroenterol 2013;19:2793-8
  • Gentile I, Borgia G. Surrogate endpoints and non-inferiority trials in chronic viral hepatitis. J Hepatol 2010;52:778
  • Bruno S, Stroffolini T, Colombo M, et al. Sustained virological response to interferon-alpha is associated with improved outcome in HCV-related cirrhosis: a retrospective study. Hepatology 2007;45:579-87
  • Di Marco V, Almasio PL, Ferraro D, et al. Peg-interferon alone or combined with ribavirin in HCV cirrhosis with portal hypertension: a randomized controlled trial. J Hepatol 2007;47:484-91
  • Coppola N, Pisaturo M, Tonziello G, et al. Efficacy of Pegylated interferon alpha-2a and alpha-2b in patients with genotype 1 chronic hepatitis C: a meta-analysis. BMC Infect Dis 2012;12:1471-2334
  • Lange CM, Bojunga J, Ramos-Lopez E, et al. Vitamin D deficiency and a CYP27B1-1260 promoter polymorphism are associated with chronic hepatitis C and poor response to interferon-alfa based therapy. J Hepatol 2011;54:887-93
  • Ismail MH. Prediction of sustained virologic responses to combination therapy of pegylated interferon-alpha and ribavirin in patients with chronic hepatitis C infection. J Family Community Med 2013;20:35-40
  • Coppola N, Pascalis SD, Pisaturo M, et al. Sustained virological response to antiviral treatment in chronic hepatitis C patients may be predictable by HCV-RNA clearance in peripheral blood mononuclear cells. J Clin Virol 2013;58:748-50
  • Coppola N, Marrone A, Pisaturo M, et al. Role of interleukin 28-B in the spontaneous and treatment-related clearance of HCV infection in patients with chronic HBV/HCV dual infection. Eur J Clin Microbiol Infect Dis 2013. [ Epub ahead of print]
  • Abu-Mouch S, Fireman Z, Jarchovsky J, et al. Vitamin D supplementation improves sustained virologic response in chronic hepatitis C (genotype 1)-naive patients. World J Gastroenterol 2011;17:5184-90
  • Nimer A, Mouch A. Vitamin D improves viral response in hepatitis C genotype 2-3 naive patients. World J Gastroenterol 2012;18:800-5
  • Venkatraman S, Bogen SL, Arasappan A, et al. Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection. J Med Chem 2006;49:6074-86
  • Tong X, Chase R, Skelton A, et al. Identification and analysis of fitness of resistance mutations against the HCV protease inhibitor SCH 503034. Antiviral Res 2006;70:28-38
  • Lin C, Kwong AD, Perni RB. Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease. Infect Disord Drug Targets 2006;6:3-16
  • Gentile I, Carleo MA, Borgia F, et al. The efficacy and safety of telaprevir - a new protease inhibitor against hepatitis C virus. Expert Opin Investig Drugs 2010;19:151-9
  • Gentile I, Viola C, Borgia F, et al. Telaprevir: a promising protease inhibitor for the treatment of hepatitis C virus infection. Curr Med Chem 2009;16:1115-21
  • Ghany MG, Strader DB, Thomas DL, et al. Diagnosis, management, and treatment of hepatitis C: an update. Hepatology 2009;49:1335-74
  • Jacobson IM, McHutchison JG, Dusheiko G, et al. Telaprevir for previously untreated chronic hepatitis C virus infection. N Engl J Med 2011;364:2405-16
  • Zeuzem S, Andreone P, Pol S, et al. Telaprevir for retreatment of HCV infection. N Engl J Med 2011;364:2417-28
  • Bacon BR, Gordon SC, Lawitz E, et al. Boceprevir for previously treated chronic HCV genotype 1 infection. N Engl J Med 2011;364:1207-17
  • Poordad F, McCone J Jr, Bacon BR, et al. Boceprevir for untreated chronic HCV genotype 1 infection. N Engl J Med 2011;364:1195-206
  • Hezode C, Fontaine H, Dorival C, et al. Triple therapy in treatment-experienced patients with HCV-cirrhosis in a multicentre cohort of the French Early Access Programme (ANRS CO20-CUPIC) - NCT01514890. J Hepatol 2013;59:434-41
  • Gentile I, Borgia F, Coppola N, et al. Daclatasvir: the first of a new class of drugs targeted against hepatitis C virus NS5A. Curr Med Chem 2013. [ Epub ahead of print]
  • Stedman CA. Current prospects for interferon-free treatment of hepatitis C in 2012. J Gastroenterol Hepatol 2013;28:38-45
  • Gallay PA, Lin K. Profile of alisporivir and its potential in the treatment of hepatitis C. Drug Des Devel Ther 2013;7:105-15
  • Lange CM, Zeuzem S. Perspectives and challenges of interferon-free therapy for chronic hepatitis C. J Hepatol 2013;58:583-92
  • Sarrazin C, Hezode C, Zeuzem S, et al. Antiviral strategies in hepatitis C virus infection. J Hepatol 2012;56:S88-S100
  • Flisiak R, Jaroszewicz J, Parfieniuk-Kowerda A. Emerging treatments for hepatitis C. Expert Opin Emerg Drugs 2013;18:461-75
  • Gentile I, Borgia F, Zappulo E, et al. Efficacy and safety of sofosbuvir in treatment of chronic hepatitis C: the dawn of the a new era. Rev Recent Clin Trials 2013. [ Epub ahead of print]
  • Gentile I, Borgia F, Buonomo AR, et al. A novel promising therapeutic option against hepatitis C virus: an oral nucleotide NS5B polymerase inhibitor sofosbuvir. Curr Med Chem 2013;20:3733-42
  • Jacobson IM, Gordon SC, Kowdley KV, et al. Sofosbuvir for hepatitis C genotype 2 or 3 in patients without treatment options. N Engl J Med 2013;368:1867-77
  • Lawitz E, Mangia A, Wyles D, et al. Sofosbuvir for previously untreated chronic hepatitis C infection. N Engl J Med 2013;368:1878-87
  • Approval of Sovaldi (sofosbuvir) tablets for the treatment of chronic hepatitis C. FDA. FDA press release. 2013. Available from: http://www.fda.gov/forconsumers/byaudience/forpatientadvocates/ucm377920.htm [Last accessed 17 January2014]
  • Cheng G, Peng B, Corsa A, et al. Antiviral activity and resistance profile of the novel HCV NS5A inhibitor GS-5885. J Hepatol 2012;56:S464-S64
  • Parfieniuk A, Jaroszewicz J, Flisiak R. Specifically targeted antiviral therapy for hepatitis C virus. World J Gastroenterol 2007;13(43):5673-81
  • Pawlotsky JM. NS5A inhibitors in the treatment of hepatitis C. J Hepatol 2013;59:375-82
  • Lindenbach BD, Rice CM. Unravelling hepatitis C virus replication from genome to function. Nature 2005;436:933-8
  • Moradpour D, Penin F, Rice CM. Replication of hepatitis C virus. Nat Rev Microbiol 2007;5:453-63
  • Link JO, Bannister R, Beilke LD, et al. Nonclinical profile and phase I results in healthy volunteers for the novel and potent HCV NS5A inhibitor GS-5885. Hepatology 2010;52:1215A-6A
  • Lawitz EJ, Gruener D, Hill JM, et al. A phase 1, randomized, placebo-controlled, 3-day, dose-ranging study of GS-5885, an NS5A inhibitor, in patients with genotype 1 hepatitis C. J Hepatol 2012;57:24-31
  • German P, Mathias A, Yang JC, et al. The Pharmacokinetics of Ledipasvir, an HCV Specific NS5A Inhibitor in HCV-Uninfected Subjects with Moderate and Severe Hepatic Impairment. Hepatology 2013;58:432A
  • German P, Mathias A, Pang PS, et al. Lack of a Clinically Significant Pharmacokinetic Drug-Drug Interaction between Sofosbuvir (GS-7977) and GS-5885 or GS-9669 in Healthy Volunteers. Hepatology 2012;56:1072A-3A
  • Yang H, Robinson M, Corsa AC, et al. Preclinical characterization of the novel hepatitis C virus NS3 protease inhibitor GS-9451. Antimicrob Agents Chemother 2013;12:12
  • Marcellin P, Manns MP, Janczewska E, et al. 12 week response-guided treatment with the NS5A inhibitor, GS-5885, the NS3 protease inhibitor, GS-9451, plus Pegylated Interferon/Ribavirin in treatment naive genotype 1 hepatitis C infected patients. J Hepatol 2013;58:S355-S55
  • Thompson A, Han S, Shiffman ML, et al. GS-5885+GS-9451+Peginterferon and Ribavirin (PR) for six or twelve weeks achieves high SVR12 rates in treatment-naive genotype 1 IL28B CC patients. J Hepatol 2013;58:S29-9
  • Everson GT, Di Bisceglie AM, Vierling JM, et al. Combination of the NS5A inhibitor, GS-5885, the NS3 protease inhibitor, GS-9451, and Pegylated Interferon plus Ribavirin in treatment experienced patients with genotype 1 hepatitis C infection. J Hepatol 2013;58:S6-6
  • Sulkowski M, Rodriguez-Torres M, Lawitz E, et al. High sustained virologic response rate in treatment-naive Hcv genotype 1a and 1b patients treated for 12 weeks with an Interferon-free all-oral quad regimen: interim results. J Hepatol 2012;56:S560-S60
  • Fenaux M, Eng S, Leavitt SA, et al. Preclinical characterization of GS-9669, a thumb site II inhibitor of the hepatitis C virus NS5B polymerase. Antimicrob Agents Chemother 2013;57:804-10
  • Gane EJ, Stedman CA, Hyland RH, et al. Efficacy of Nucleotide Polymerase Inhibitor Sofosbuvir plus the NS5A Inhibitor Ledipasvir or the NS5B Non-nucleoside Inhibitor GS-9669 Against HCV Genotype 1 Infection. Gastroenterology 2014;146(3):736-43
  • Kohli A, Sims Z, Marti M, et al. Combination oral, ribavirin free, antiviral therapy to optimize treatment outcomes for hepatitis C GT-1 treatment naive patients: interim results from the NIAID SYNERGY Trial. Hepatology 2013;58:1382
  • Lawitz E, Poordad FF, Pang PS, et al. Sofosbuvir and ledipasvir fixed-dose combination with and without ribavirin in treatment-naive and previously treated patients with genotype 1 hepatitis C virus infection (LONESTAR): an open-label, randomised, phase 2 trial. Lancet 2013;1:62121-2
  • Everson GT, Lawitz E, Thompson AJ, et al. The NS5A Inhibitor GS-5885 Is Safe and Well-Tolerated in Over 1000 Patients Treated in Phase 2 Studies. Hepatology 2012;56:572A-3A
  • Wong KA, Worth A, Brainard DM, et al. Persistence of NS5A GS-5885 drug resistance mutations following 3 days of monotherapy in genotype-1 HCV patients is dependent on the HCV subtype and specific mutation. J Hepatol 2012;56:S482-S82
  • Wong KA, Worth A, Martin R, et al. Characterization of hepatitis C virus resistance from a multiple dose clinical trial of the novel NS5A inhibitor GS-5885. Antimicrob Agents Chemother 2013;22:22
  • Gane EJ, Stedman CA, Hyland RH, et al. Once daily sofosbuvir/ledipasvir fixed-dose combination with or without ribavirin: data from the ELECTRON trials. Hepatology 2013;58:243A
  • Borgia G, Gentile I. Treating chronic hepatitis B: today and tomorrow. Curr Med Chem 2006;13:2839-55
  • Gane EJ, Stedman CA, Hyland RH, et al. All-oral sofosbuvir-based 12-week regimens for the treatment of chronic HCV infection: the ELECTRON study. J Hepatol 2013;58:S6-7

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.