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New NS5B polymerase inhibitors for hepatitis C

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Pages 963-975 | Published online: 15 Jul 2010

Bibliography

  • Choo QL, Kuo G, Weiner AJ, Isolation of a cDNA clone derived from a blood-borne non-A, non-B viral hepatitis genome. Science 1989;244:359-62
  • Simmonds P, Bukh J, Combet C, Consensus proposals for a unified system of nomenclature of hepatitis C virus genotypes. Hepatology 2005;42:962-73
  • Fried MW, Shiffman ML, Reddy KR, Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection. N Engl J Med 2002;347:975-82
  • Manns MP, McHutchison JG, Gordon SC, Peginterferon alfa-2b plus ribavirin compared with interferon alfa-2b plus ribavirin for initial treatment of chronic hepatitis C: a randomised trial. Lancet 2001;358:958-65
  • Lohmann V, Korner F, Koch J, Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line. Science 1999;285:110-3
  • Zhong J, Gastaminza P, Cheng G, Robust hepatitis C virus infection in vitro. Proc Natl Acad Sci USA 2005;102:9294-9
  • Wakita T, Pietschmann T, Kato T, Production of infectious hepatitis C virus in tissue culture from a cloned viral genome. Nat Med 2005;11:791-6
  • Moradpour D, Penin F, Rice CM. Replication of hepatitis C virus. Nat Rev Microbiol 2007;5:453-63
  • Lesburg CA, Cable MB, Ferrari E, Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site. Nat Struct Biol 1999;6:937-43
  • Bressanelli S, Tomei L, Roussel A, Crystal structure of the RNA-dependent RNA polymerase of hepatitis C virus. Proc Natl Acad Sci USA 1999;96:13034-9
  • Lin K, Hazuda DJ, Otto MJ, Initial recommendations for HCV drug resistance analysis: a consensus statement from the HCV Drug Resistance Advisory Board [abstract 28]. HepDart, frontiers in drug development for viral hepatitis, 9 – 13 December 2007; Lahaina, Hawaii
  • Pierra C, Benzaria S, Amador A, Nm 283, an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine. Nucleosides Nucleotides Nucleic Acids 2005;24:767-70
  • Bassit L, Grier J, Bennett M, Combinations of 2′-C-methylcytidine analogues with interferon-alpha2b and triple combination with ribavirin in the hepatitis C virus replicon system. Antivir Chem Chemother 2008;19:25-31
  • Toniutto P, Fabris C, Bitetto D, Valopicitabine dihydrochloride: a specific polymerase inhibitor of hepatitis C virus. Curr Opin Investig Drugs 2007;8:150-8
  • Pockros PJ, Nelson D, Godofsky E, R1626 plus peginterferon alfa-2a provides potent suppression of hepatitis C virus RNA and significant antiviral synergy in combination with ribavirin. Hepatology 2008;48:385-97
  • Murakami E, Bao H, Ramesh M, Mechanism of activation of beta-D-2′-deoxy-2′-fluoro-2′-c-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. Antimicrob Agents Chemother 2007;51:503-9
  • Reddy R, Rodrigues-Torres M, Gane EJ, Antiviral activity, pharmacokinetics, safety, and tolerability of R7128, a novel nucleoside HCV RNA polymerase inhibitor, following multiple, ascending, oral doses in patients with genotype 1 infection who have failed prior interferon therapy. Hepatology 2008;46:862A
  • Lalezari J, Gane EJ, Rodrigues-Torres M, Potent antiviral activity of the HCV nucleoside polymerase inhibitor R7128 with Peg-IFN and ribavirin: interim results of R7128 500 mg BID for 28 days. J Hepatol 2008;48:S29
  • Gane EJ, Rodrigues-Torres M, Nelson DR, Antiviral activity of the nucleoside polymerase inhibitor R7128 in HCV genotype 2 and 3 prior non-responders: interim results of R7128 1500 mg bid with peg-IFN and ribavirin for 28 days. Hepatology 2008;48:1024A
  • Gane EJ, Roberts SK, Stedman CA, INFORM Study: HCV protease R7227+HCV nucleoside R7128; twice daily oral medication shows promise in treating patients with hepatitis C. Hepatology 2009;50:394A
  • Carroll SS, Ludmerer S, Handt L, Robust antiviral efficacy upon administration of a nucleoside analog to hepatitis C virus-infected chimpanzees. Antimicrob Agents Chemother 2009;53:926-34
  • Standring D, Lanford R, Cretto-Scott E, Potent antiviral activity of 2nd generation HCV nucleotide inhibitors, IDX102 and IDX184, in HCV-infected Chimps. J Hepatol 2009;48:S30
  • Lalezari J, Poordad F, Mehra P, Antiviral activity, pharmacokinetics and safety of IDX184 in combination with pegylatyed interferon (PEGIFN) and ribavirin (RBV) in treatment-naive HCV gebotype 1-infected subjects. J Hepatol 2010;52:S469
  • Furman PW, Niu C, Bao D, PSI-7851: a novel liver targetting prodrug for the treatment of hepatitis C. Hepatology 2009;48:1161A
  • Lam AM, Espiritu CL, Steuer HM, Novel 2′-F-2′-methyl purine nucleotide analogue are active inhibitors of HCV replication and lack cross resistance with other nucleos(t)ide analogs. Hepatology 2009;50:1047A
  • Le Pogam S, Jiang WR, Leveque V, In vitro selected Con1 subgenomic replicons resistant to 2′-C-methyl-cytidine or to R1479 show lack of cross resistance. Virology 2006;351:349-59
  • Harper S, Pacini B, Avolio S, Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase. J Med Chem 2005;48:1314-7
  • Tomei L, Altamura S, Bartholomew L, Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J Virol 2003;77:13225-31
  • Chan L, Reddy TJ, Proulx M, Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase. J Med Chem 2003;46:1283-5
  • Gopalsamy A, Lim K, Ciszewski G, Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors. J Med Chem 2004;47:6603-8
  • Li H, Tatlock J, Linton A, Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors. Bioorg Med Chem Lett 2006;16:4834-8
  • Dhanak D, Duffy KJ, Johnston VK, Identification and biological characterization of heterocyclic inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem 2002;277:38322-7
  • Pfefferkorn JA, Greene ML, Nugent RA, Inhibitors of HCV NS5B polymerase. Part 1: evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid. Bioorg Med Chem Lett 2005;15:2481-6
  • Pfefferkorn JA, Nugent R, Gross RJ, Inhibitors of HCV NS5B polymerase. Part 2: evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid. Bioorg Med Chem Lett 2005;15:2812-8
  • Gopalsamy A, Aplasca A, Ciszewski G, Design and synthesis of 3, 4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran derivatives as non-nucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase. Bioorg Med Chem Lett 2006;16:457-60
  • Erhardt A, Deterding K, Benhamou Y, Safety, pharmacokinetics and antiviral effect of BILB 1941, a novel hepatitis C virus RNA polymerase inhibitor, after 5 days oral treatment. Antivir Ther 2009;14:23-32
  • Larrey D, Benhamou Y, Lohse AW, BI 207127 is a potent HCV RNA polymerase inhibitor during 5 days monotherapy in patients with chronic hepatitis C. Hepatology 2009;50:1044A
  • Brainard DM, Anderson MS, Petry AS, Safety and antiviral activity of NS5B polymerase inhibitor MK-3281 in genotype 1 and 3 HCV-infected patients. Hepatology 2009;50:1026A
  • Hammond JL, Maria C, Rosario MC, Antiviral activity of the HCV polymerase inhibitor PF-00868554 administered as monotherapy in HCV genotype 1 infected subjects. Hepatology 2008;48:1159A
  • Jacobson I, Pockros P, Lalezari J, Antiviral activity of filibuvir in combination with pegylated interferon alpha 2a and ribavirin for 28 days in treatment naive patients chronically infected with HCV genotype 1. J Hepatol 2009;50:S382-3
  • Troke P, Lewis M, Simpson P, Genotypic characterisation of the HCV NS5B following 8-days-monotherapy with the polymerase inhibitor PF-00868554 in HCV infected subjects. J Hepatol 2009;50:S351
  • Cooper C, Lawitz EJ, Ghali P, Evaluation of VCH-759 monotherapy in hepatitis C infection. J Hepatol 2009;51:39-46
  • Lawitz E, Cooper C, Rodriguez-Torres M, Tolerability and antiviral activity of VCH-916, a novel non-nucleoside HCV polymerase inhibitor in patients with chronic HCV genotype-1 infection. J Hepatol 2009;50:S37
  • Cooper C, Larouche R, Bourgault B, Safety, tolerability and pharmacokinetics of the HCV polymerase inhibitor VCH-222 following single dose administration in healthy volunteers and antiviral activity in HCV infected individuals. J Hepatol 2009;50:S342
  • Rodriguez-Torres M, Lawitz E, Conway B, Safety and antiviral activity of the non-nucleoside polymearse inhibitor VX-222 in treatment naive genotype 1 HCV infected patients. J Hepatol 2010;52:S14
  • Lawitz E, Rodrigues-Torres M, DeMicco T, Antiviral activity of ANA598, a potent non-nucleoside polymerase inhibitor, in chronic hepatitis C patients. J Hepatol 2009;50:S384
  • Rodrigues-Torres M, Lawitz E, Cohen D, Treatment naive, HCV genotype 1-infected subjects show significantly greater decrease when treated for 28 days of ABT-333 plus peginterferon and ribavirin than peginterferon and ribavirin alone. Hepatology 2009;50:5A
  • Wagner R, Maring C, Donner P, Preclinical characterization of ABT-072: a novel non nucleoside HCV polymerase inhibitor. J Hepatol 2009;50:S352
  • Standring D, Bilello JP, Dousson C, In vitro activity and pharmacological properties of IDX375, a novel HCV non-nucleoside inhibitor. Hepatology 2008;48:1167A
  • Good SS, Bu C, Camire MH-S, Preclinical pharmacokinetic and safety profile of IDX375, a novel and potent non-nucleoside HCV polymerase inhibitor. J Hepatol 2009;50:S125
  • Villano SA, Raible D, Harper D, Antiviral activity of the non-nucleoside polymerase inhibitor, HCV-796, in combination with pegylated interferon alpha-2b in tratment naive patients with chronic HCV. J Hepatol 2007;56:S24
  • Shih I, Vliegen I, Peng B, Mechanistic characterization of GS-9190, a novel non nucleoside inhibitor of the hcv NS5B polymerase with potent antiviral activity and a unique mechanism of action. Hepatology 2007;46:859A
  • Vliegen I, Paeshuyse J, Marbery E, GS-9190, a novel substituted imidazopyridine analogue, is a potent inhibitor of hepatitis C virus replication in vitro and remains active against known drug resistant mutants. Hepatology 2007;46:855A
  • Neumann AU, Lam AM, Dahari H, Hepatitis C viral dynamics in vivo and the antiviral efficacy of interferon-alpha therapy. Science 1998;282:103-7
  • Herrmann E, Neumann AU, Schmidt JM, Hepatitis C virus kinetics. Antivir Ther 2000;5:85-90
  • Bartenschlager R, Lohmann V. Replication of hepatitis C virus. J Gen Virol 2000;81:1631-48
  • Ludmerer SW, Graham DJ, Boots E, Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assay. Antimicrob Agents Chemother 2005;49:2059-69
  • Migliaccio G, Tomassini JE, Carroll SS, Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro. J Biol Chem 2003;278:49164-70
  • Le Pogam S, Seshaadr A, Kosaka A, No evidence of R7128 drug resistance after up to 4 weeks treatment of GT1, 2 and 3 hepatitis C virus infected individuals. J Hepatol 2009;50:S348
  • Kukolj G, McGibbon GA, McKercher G, Binding site characterization and resistance to a class of non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase. J Biol Chem 2005;280:39260-7
  • Shi ST, Herlihy KJ, Graham JP, In vitro resistance study of AG-021541, a novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Antimicrob Agents Chemother 2008;52:675-83
  • Nicolas O, Boivin I, Berneche-D'Amours A, Genotypic and phenotypic analysis of the HCV NS5B variants selected from patients treated with VCH-916. J Hepatol 2009;50:S349
  • Marquis M, Deterding K, Erhardt A, Genotypic and phenotypic analysis of hepatitis C virus NS5B polymerase variants to BILB-1941 inhibition [abstract 1897]. 59th Annual Meeting of the American Association for the Study of the Liver Diseases, San Fransisco, CA, USA; October 31 - 4 November 2008
  • McCown MF, Rajyaguru S, Le Pogam S, The hepatitis C virus replicon presents a higher barrier to resistance to nucleoside analogs than to nonnucleoside polymerase or protease inhibitors. Antimicrob Agents Chemother 2008;52:1604-12
  • Sarrazin C, Zeuzem S. Resistance to direct antiviral agents in patients with hepatitis C virus infection. Gastroenterology 2010;138:447-62
  • Lallos L, La Cola M, Serra I, Combination of IDX184, a nucleotide prodrug polymerase inhibitor, with other classes of HCV inhibitors is additive to synergistic in the HCV replicon in vitro. Hepatology 2009;50:1045A
  • Zennou V, Lam AM, Keilman M, Combination of two complementary nucletide analogues PSI-7977 and PSI-938 effectively clears wild type and NS5B S282T HCV replicons–comparison with combination of other antiviral compounds. J Hepatol 2010;52:S400-401
  • Tan H, Rajyaguru S, Wu T, Combination of the NS3/4 protease inhibitor ITMN-191 (R7227) with the active moiety of the NS5B inhibitor R1626 or R1728 enhances replicon clearance and reduces the emergence of drug resistant variants. Hepatology 2008;48:1153A
  • Gane EJ, Roberts SK, Stedman CA, First in man demonstration of potenet antiviral activity witha nucleoside polymerase R7128 and protease R7227/ITMN-191 inhibitor combination in HCV: safety pharmacokinetics and virologic results from INFORM-1. J Hepatol 2009;1:S380
  • Le Pogam S, Chhabra M, Ali S, Combination therapy with nucleoside polymerase R7128 and protease R7227/ITMN-191 inhibitors in genotype 1 HCV infected patients: interim resistance analysis of INFORM-1 cohorts A-D. Hepatology 2009;50:1037A
  • Herlihy KJ, Graham JP, Kumpf R, Development of intergenotypic chimeric replicons to determine the broad-spectrum antiviral activities of hepatitis C virus polymerase inhibitors. Antimicrob Agents Chemother 2008;52:3523-31
  • Pauwels F, Mostmans W, Quirynen LM, Binding-site identification and genotypic profiling of hepatitis C virus polymerase inhibitors. J Virol 2007;81:6909-19
  • Legrand-Abravanel F, Henquell C, Le Guillou-Guillemette H, Naturally occurring substitutions conferring resistance to hepatitis C virus polymerase inhibitors in treatment-naive patients infected with genotypes 1-5. Antivir Ther 2009;14:723-30
  • Cantaloube JF, Laperche S, Gallian P, Analysis of the 5′ noncoding region versus the NS5b region in genotyping hepatitis C virus isolates from blood donors in France. J Clin Microbiol 2006;44:2051-6
  • Nicot F, Legrand-Abravanel F, Sandres-Saune K, Heterogeneity of hepatitis C virus genotype 4 strains circulating in south-western France. J Gen Virol 2005;86:107-14
  • Sandres-Saune K, Deny P, Pasquier C, Determining hepatitis C genotype by analyzing the sequence of the NS5b region. J Virol Methods 2003;109:187-93
  • Chen Z, Weck KE. Hepatitis C virus genotyping: interrogation of the 5′ untranslated region cannot accurately distinguish genotypes 1a and 1b. J Clin Microbiol 2002;40:3127-34
  • Halfon P, Trimoulet P, Bourliere M, Hepatitis C virus genotyping based on 5′ noncoding sequence analysis (Trugene). J Clin Microbiol 2001;39:1771-3
  • Legrand-Abravanel F, Colson P, Leguillou-Guillemette H, Influence of the HCV subtype on the virological response to pegylated interferon and ribavirin therapy. J Med Virol 2009;81:2029-35
  • Kuntzen T, Timm J, Berical A, Naturally occurring dominant resistance mutations to hepatitis C virus protease and polymerase inhibitors in treatment-naive patients. Hepatology 2008;48:1769-78
  • Le Pogam S, Seshaadri A, Kosaka A, Existence of hepatitis C virus NS5B variants naturally resistant to non-nucleoside, but not to nucleoside, polymerase inhibitors among untreated patients. J Antimicrob Chemother 2008;61:1205-16
  • Sax PE, Islam R, Walensky RP, Should resistance testing be performed for treatment-naive HIV-infected patients? A cost-effectiveness analysis. Clin Infect Dis 2005;41:1316-23
  • Forestier N, Reesink HW, Weegink CJ, Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C. Hepatology 2007;46:640-8
  • Kieffer TL, Sarrazin C, Miller JS, Telaprevir and pegylated interferon-alpha-2a inhibit wild-type and resistant genotype 1 hepatitis C virus replication in patients. Hepatology 2007;46:631-9
  • Mederacke I, Wedemeyer H, Manns MP. Boceprevir, an NS3 serine protease inhibitor of hepatitis C virus, for the treatment of HCV infection. Curr Opin Investig Drugs 2009;10:181-9
  • Boguszewska-Chachulska AM, Krawczyk M, Najda A, Searching for a new anti-HCV therapy: synthesis and properties of tropolone derivatives. Biochem Biophys Res Commun 2006;341:641-7
  • Griffin S. Inhibition of HCV p7 as a therapeutic target. Curr Opin Investig Drugs 2010;11:175-81
  • Nettles RE, Chien C, Chung E, BMS-790052 is a first-in-class potent Hepatitis C Virus (HCV) NS5A inhibitor for patients with chronic hcv infection: results from a proof-of-concept Study. Hepatology 2008;48:A1025
  • Gallay PA. Cyclophilin inhibitors. Clin Liver Dis 2009;13:403-17
  • Pockros PJ, Guyader D, Patton H, Oral resiquimod in chronic HCV infection: safety and efficacy in 2 placebo-controlled, double-blind phase IIa studies. J Hepatol 2007;47:174-82
  • Miller RL, Meng TC, Tomai MA. The antiviral activity of Toll-like receptor 7 and 7/8 agonists. Drug News Perspect 2008;21:69-87

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