Novel protease and polymerase inhibitors for the treatment of hepatitis C virus infection

Bibliography

• SHARMA P, LOK A: Viral hepatitis and liver transplantation. Semin. Liver Dis. (2006) 26(3):285-297.
   PubMed Web of Science ®Google Scholar
• FRIED MW, HADZIYANNIS SJ: Treatment of chronic hepatitis C infection with peginterferons plus ribavirin. Semin. Liver Dis. (2004) 24(Suppl. 2):47-54.
   PubMed Web of Science ®Google Scholar
• LOHMANN V, KORNER F, KOCH J et al.: Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line. Science (1999) 285:110-113.
   PubMed Web of Science ®Google Scholar
• WAKITA T, PIETSCHMANN T, KATO T et al.: Production of infectious hepatitis C virus in tissue culture from a cloned viral genome. Nat. Med. (2005) 11(7):791-796.
   PubMed Web of Science ®Google Scholar
• HORSCROFT N, LAI VC, CHENEY W et al.: Replicon cell culture system as a valuable tool in antiviral drug discovery against hepatitis C virus. Antivir. Chem. Chemother. (2005) 16(1):1-12.
   PubMedGoogle Scholar
• DI BISCEGLIE AM, MCHUTCHISON J, RICE CM: New therapeutic strategies for hepatitis C. Hepatology (2002) 35(1):224-231.
   PubMed Web of Science ®Google Scholar
• MORADPOUR D, BRASS V, GOSERT R, WOLK B, BLUM HE: Hepatitis C: molecular virology and antiviral targets. Trends Mol. Med. (2002) 8(10):476-482.
   PubMed Web of Science ®Google Scholar
• PAWLOTSKY JM, CHEVALIEZ S, MCHUTCHISON JG: The hepatitis C virus life cycle as a target for new antiviral therapies. Gastroenterology (2007) 132(5):1979-1998.
   PubMed Web of Science ®Google Scholar
• WARDELL AD, ERRINGTON W, CIARAMELLA G, MERSON J, MCGARVEY MJ: Characterization and mutational analysis of the helicase and NTPase activities of hepatitis C virus full-length NS3 protein. J. Gene Virol. (1999) 80(Part 3):701-709.
   PubMed Web of Science ®Google Scholar
• BOROWSKI P, SCHALINSKI S, SCHMITZ H: Nucleotide triphosphatase/helicase of hepatitis C virus as a target for antiviral therapy. Antiviral Res. (2002) 55(3):397-412.
   PubMed Web of Science ®Google Scholar
• KOLYKHALOV AA, MIHALIK K, FEINSTONE SM, RICE CM: Hepatitis C virus-encoded enzymatic activities and conserved RNA elements in the 3′ nontranslated region are essential for virus replication in vivo. J. Virol. (2000) 74(4):2046-2051.
   PubMed Web of Science ®Google Scholar
• 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(1):3-16.
   PubMedGoogle Scholar
• PERNI RB, ALMQUIST SJ, BYRN RA et al.: Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob. Agents Chemother. (2006) 50(3):899-909.
   PubMed Web of Science ®Google Scholar
• LIN K, PERNI RB, KWONG AD, LIN C: VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCV replicon cells. Antimicrob. Agents Chemother. (2006) 50(5):1813-1822.
   PubMed Web of Science ®Google Scholar
• MCHUTCHISON JG, EVERSON G, GORDON SC et al.: Results of an interim analysis of a Phase 2 study of telaprevir (VX-950) with peginterferon α-2a and ribavirin in previously untreated subjects with hepatitis C. Hepatology (2007) 46(S1):S296.
   Google Scholar
• LAWITZ EJ, RODRIGUEZ-TORRES M, MUIR A et al.: 28 Days of the hepatitis c protease inhibitor VX-950, in combination with peg-interferon-α-2a and ribavirin, is well-tolerated and demonstrates robust antiviral effects. Gastroenterology (2006) 130(4):(Suppl. 2).
   Google Scholar
• MALCOLM BA, LIU R, LAHSER F et al.: SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of α interferon in replicon cells. Antimicrob. Agents Chemother. (2006) 50(3):1013-1020.
   PubMed Web of Science ®Google Scholar
• ZEUZEM S, SARRAZIN C, WAGNER F et al.: 78 The HCV NS3 protease inhibitor SCH 503034 in combination with PEG-IFNa-2b in the treatment of HCV-1 PEG-IFNa-2b non-responders: antiviral activity and HCV variant analysis. J. Hepatol. (2006) 42(Suppl. 2):S35.
   Web of Science ®Google Scholar
• SEIWERT S, ANDREWS S, YANG H et al.: Preclinical characteristics of ITMN 191, an orally active inhibitor of the HCV NS3/4a protease nominated for preclinical development. Digestive Disease Week. Los Angeles, California, USA (20 – 25 May 2006).
   Google Scholar
• INTERMUNE: InterMune Submits Clinical Trial Authorization Application for ITMN-191 for Hepatitis C Infections (2006) (Press Release).
   Google Scholar
• TAN H, SEIWERT S, BLATT L: In vitro synergistic antiviral activity of ITMN - 191, an orally active inhibitor of the hepatitis C virus ( HCV ) NS3/4A protease, in combination with PEG-interferon α-2a. Hepatology (2006) 44(S1):A534.
   Google Scholar
• SEIWERT S, TAN H, BLATT L: Additive to synergistic antiviral effects of an NS3/4a protease inhibitor (ITMN-191) and an NS5b RNA-dependent RNA dependent polymerase inhibitor (R1479) in an HCV replicon system. Hepatology (2007) 46(S1):S167.
   Google Scholar
• HINRICHSEN H, BENHAMOU Y, WEDEMEYER H et al.: Short-term antiviral efficacy of BILN 2061, a hepatitis C virus serine protease inhibitor, in hepatitis C genotype 1 patients. Gastroenterology (2004) 127(5):1347-1355.
   PubMed Web of Science ®Google Scholar
• LAMARRE D, ANDERSON PC, BAILEY M et al.: An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus. Nature (2003) 426(6963):186-189.
   PubMed Web of Science ®Google Scholar
• REISER M, HINRICHSEN H, BENHAMOU Y et al.: Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C. Hepatology (2005) 41(4):832-835.
   PubMed Web of Science ®Google Scholar
• LESBURG CA, CABLE MB, FERRARI E et al.: Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site. Nat. Struct. Biol. (1999) 6(10):937-943.
   PubMedGoogle Scholar
• BRESSANELLI S, TOMEI L, REY FA, DE FRANCESCO R: Structural analysis of the hepatitis C virus RNA polymerase in complex with ribonucleotides. J. Virol. (2002) 76(7):3482-3492.
   PubMed Web of Science ®Google Scholar
• LEE JH, NAM IY, MYUNG H: Nonstructural protein 5B of hepatitis C virus. Mol. Cells (2006) 21(3):330-336.
   PubMed Web of Science ®Google Scholar
• PIERRA C, AMADOR A, BENZARIA S et al.: Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine. J. Med. Chem. (2006) 49(22):6614-6620.
   PubMed Web of Science ®Google Scholar
• LAWITZ EJ, NGUYEN T, YOUNES Z et al.: Clearance of HCV RNA with valopitabine (NM283) plus peg-interferon in treatment-naive patients with HCV-1 infection: results at 24 and 48 weeks. Hepatology (2007) 46(S1):S9.
   PubMedGoogle Scholar
• TONIUTTO P, FABRIS C, BITETTO D et al.: Valopicitabine dihydrochloride:a specific polymerase inhibitor of hepatitis C virus. Curr. Opin. Investig. Drugs (2007) 8(2):150-158.
   PubMed Web of Science ®Google Scholar
• RODRIGUEZ-TORRES M, LAWITZ E, GODOFSKY E: Valopicitabine (nm283) alone and in combination with peg-interferon in patients with genotype 1 chronic hepatitis C: preliminary results from an ongoing Phase II, multicenter study. Gastroenterology (2005) 128(4 Suppl. 2):A695-A696.
   PubMed Web of Science ®Google Scholar
• AFDAL N, O'BRIEN C, GODOFSKY E et al.: Valopicitabine (NM283), alone or with peg-interferon, compared to peg-interferon/ribervirin (PEGIFN/RBV) retreatment in patients with HCV-1 infection and prior non-response to PEGIFN/RBV: one year results. Hepatology (2007) 46(S1):S5.
   Google Scholar
• COELMONT L, PAESHUYSE J, WINDISCH MP et al.: Ribavirin antagonizes the in vitro anti-hepatitis C virus activity of 2′-C-methylcytidine, the active component of valopicitabine. Antimicrob. Agents Chemother. (2006) 50(10):3444-3446.
   PubMed Web of Science ®Google Scholar
• STUYVER L, MCBRAYER T, THARNISH P et al.: β-d-2′-deoxy-2′-fluoro-2′-c-methylcytidine is a potent and specific inhibitor of hepatitis C virus in Huh-7 cells. 45th Interscience Conference on Antimicrobial Agents and Chemotherapy. Washington, USA (16 – 19 December 2005), (Abstract F-481).
   Google Scholar
• MURAKAMI E, RAMESH M, MCBRAYER T et al.: Mechanism of activation of β-D-2′-deoxy-2′-fluoro-2′-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. 45th Interscience Conference on Antimicrobial Agents and Chemotherapy. Washington, USA (16 – 19 December 2005), (Abstract 476).
   Google Scholar
• XTL, BIOPHARMACUETICALS, INC.: XTL Biopharmaceuticals Ltd initiates patient dosing in Phase 1 clinical trial of XTL-2125, an oral, non-nucleoside polymerase inhibitor for the treatment of hepatitis C. 4 May 2006, New York, USA (Press Release).
   Google Scholar
• VILLANO S, CHANDRA P, RAIBLE D et al.: Antiviral activity of the non-nucleoside polymerase inhibitor, HCV-796, in patients with chronic hepatitis C virus: preliminary results from a randomized, double-blind, placebo-controlled, ascending multiple dose study. Digestive Disease Week; Los Angeles, California, USA (20 – 25 May 2006), (Abstract 1).
   Google Scholar
• VILLANO S, RAIBLE D, HARPER D et al.: Antiviral activity of the non-nucleoside polymerase inhibitor, HCV-796, in combination with pegylated interferon α-2b in treatment-naive patients with chronic HCV. Hepatology (2007) 46(S1):S24.
   Web of Science ®Google Scholar
• KLUMPP K, LEVEQUE V, LE POGAM S et al.: The novel nucleoside analog R1479 (4′-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J. Biol. Chem. (2006) 281(7):3793-3799.
   PubMed Web of Science ®Google Scholar
• ROBERTS S, COOKSLEY G, DORE G et al.: Results of a Phase 1B, multiple dose study of R1626, a novel nucleoside analog targeting HCV polymerase in chronic HCV genotype 1 patients. Hepatology (2006) 44(S1):A692.
   Google Scholar
• JIANG W, CHIU S, ALI S et al.: In vitro antiviral interactions of a novel HCV inhibitor R1479 with interferon α–2α, ribavirin and other HCV inhibitors. Hepatology (2006) 44(S1):A533.
   Google Scholar
• WAGNER R, LARSON D, BOSSE T et al.: Discovery, characterization and anti-HCV activity of a novel NS5B inhibitor. Hepatology (2006) 44(S1):A236-A237.
   Web of Science ®Google Scholar
• KOEV G, DEKHTYAR T, HAN L et al.: In vitro antiviral effects of combinations of Abbott HCV polymerase inhibitors with IFN or NS3/4A protease inhibitors. Hepatology (2006) 44(S1):A352.
   PubMed Web of Science ®Google Scholar
• CARROLL S, DAVIES M, HANDT L et al.: Robust suppression of viral replication by a nucleoside polymerase inhibitor in chimpanzees infected with hepatitis C virus. Hepatology (2006) 44(S1):A535.
   Google Scholar
• LU L, PILOT-MATIAS TJ, STEWART KD et al.: Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro. Antimicrob. Agents Chemother. (2004) 48(6):2260-2266.
   PubMed Web of Science ®Google Scholar
• LIN C, LIN K, LUONG YP et al.: In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms. J. Biol. Chem. (2004) 279(17):17508-17514.
   PubMed Web of Science ®Google Scholar
• 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(2):28-38.
   PubMed Web of Science ®Google Scholar
• SARRAZIN C, KIEFFER TL, BARTELS D et al.: Dynamic hepatitis C virus genotypic and phenotypic changes in patients treated with the protease inhibitor telaprevir. Gastroenterology (2007) 132(5):1767-1777.
   PubMed Web of Science ®Google Scholar
• SEIWERT S, ANDREWS S, TAN H et al.: Generation and characterisation of HCV replicons with reduced sensitivity to ITMN 191, a macrocyclic inhibitor of NS3/4a. Digestive Disease Week. Los Angeles, California, USA (2006), (Abstract 195).
   Google Scholar
• YANG W, ZHAO Y, FABRYCKI J et al.: Induction of resistance by a novel class of compounds active against hepatitis C virus with no cross-resistance to NS3 protease and NS5B polymerase inhibitors. Hepatology (2006) 44(S1):A535.
   Google Scholar
• OLSEN D, CARROLL SS, HANDT L et al.: HCV antiviral activity and resistance analysis in chronically infected chimpanzees treated with Ns3/4a protease and NS5b polymerase inhibitors. Hepatology (2007) 46(Suppl. 1):S298.
   Google Scholar
• MIGLIACCIO G, TOMASSINI JE, CARROLL SS et al.: Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro. J. Biol. Chem. (2003) 278(49):49164-49170.
   PubMed Web of Science ®Google Scholar
• CARROLL SS, TOMASSINI JE, BOSSERMAN M et al.: Inhibition of hepatitis C virus RNA replication by 2′-modified nucleoside analogs. J. Biol. Chem. (2003) 278(14):11979-11984.
   PubMed Web of Science ®Google Scholar
• LUDMERER SW, GRAHAM DJ, BOOTS E et al.: Replication fitness and NS5B drug sensitivity of diverse hepatitis C virus isolates characterized by using a transient replication assay. Antimicrob. Agents Chemother. (2005) 49(5):2059-2069.
   PubMed Web of Science ®Google Scholar
• LE POGAM S, JIANG WR, LEVEQUE V et al.: In vitro selected Con1 subgenomic replicons resistant to 2′-C-methyl-cytidine or to R1479 show lack of cross resistance. Virology (2006) 351(2):349-359.
   PubMed Web of Science ®Google Scholar
• LU L, KRISHNAN P, PITHAWALLA R et al.: Selection and characterization of hepatitis C virus replicons resistant to a potent polymerase inhibitor A-837093. Hepatology (2006) 44(S2):A351.
   Google Scholar
• VILLANO S, HOWE A, RAIBLE D et al.: Analysis of HCV NS5B genetic variants following monotherapy with HCV-796, a non-nucleoside polymerase inhibitor, in treatment-naïve HCV-infected patients. Hepatology (2006) 44(S1):A607-A608.
   Web of Science ®Google Scholar
• SHI S, HERLIHY K, GONZALEZ J, PATICK A, DUGGAL R: In vitro resistance studies of AG-021541, a novel nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Hepatology (2006) 44(S1):A534.
   Google Scholar
• SORIANO V, PUOTI M, SULKOWSKI M et al.: Care of patients coinfected with HIV and hepatitis C virus: 2007 updated recommendations from the HCV-HIV International Panel. AIDS (2007) 21(9):1073-1089.
   PubMed Web of Science ®Google Scholar
• AMPARO E, SAHA A, YOUNG C et al.: HCV-796: a potent and selective non-nucleoside inhibitor of HCV NS5b. 46th Interscience Conference on Antimicrobial Agents and Chemotherapy. San Francisco, USA (2006), (Abstract F1-1378).
   Google Scholar