Effect on hepatitis C virus replication of combinations of direct-acting antivirals, including NS5A inhibitor daclatasvir

Antimicrobial Agents and Chemotherapy

Volumn 56, Issue 10, 2012, Pages 5230-5239

  Pelosi, Lenore A ^a   Voss, Stacey ^a   Liu, Mengping ^a   Gao, Min ^a   Lemm, Julie A ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIVIRUS AGENT; ASUNAPREVIR; BMS 791325; DACLATASVIR; NONSTRUCTURAL PROTEIN 3; NONSTRUCTURAL PROTEIN 5A; NONSTRUCTURAL PROTEIN 5B; UNCLASSIFIED DRUG;

ANTIVIRAL RESISTANCE; ARTICLE; CONTROLLED STUDY; DRUG POTENTIATION; GENE TARGETING; HEPATITIS C VIRUS; MONOTHERAPY; NONHUMAN; PRIORITY JOURNAL; REPLICON; VIRAL CLEARANCE; VIRUS INHIBITION; VIRUS REPLICATION;

ANTIVIRAL AGENTS; CELL LINE; DRUG INTERACTIONS; DRUG RESISTANCE, VIRAL; HEPACIVIRUS; HUMANS; IMIDAZOLES; VIRAL NONSTRUCTURAL PROTEINS; VIRUS REPLICATION;

EID: 84866315985     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.01209-12     Document Type: Article

References (62)

1. Beaulieu PL. 2009. Recent advances in the development of NS5B polymerase inhibitors for the treatment of hepatitis C virus infection. Expert Opin. Ther. Pat. 19:145-164.
2. Blight KJ, Kolykhalov AA, Rice CM. 2000. Efficient initiation of HCV RNA replication in cell culture. Science 290:1972-1974.
3. Brown NA. 2009. Progress towards improving antiviral therapy for hepatitis C with hepatitis C virus polymerase inhibitors. Part I: nucleoside analogues. Expert Opin. Invest. Drugs 18:709-725.
4. Burton JR, Jr, Everson GT. 2009. HCV NS5B polymerase inhibitors. Clin. Liver Dis. 13:453-465.
5. Chase R, et al. 2009. A novel HCV NS3 protease mutation selected by combination treatment of the protease inhibitor boceprevir and NS5B polymerase inhibitors. Antiviral Res. 84:178-184.
6. Chou T. 2006. Theoretical basis, experimental design, and computerized simulation of synergism and antagonism in drug combination studies. Pharmacol. Rev. 58:621-681. (Pubitemid 44403686)
7. Dimitrova M, Imbert I, Kieny MP, Schuster C. 2003. Protein-protein interactions between hepatitis C virus nonstructural proteins. J. Virol. 77:5401-5414. (Pubitemid 36460954)
8. Egger D, et al. 2002. Expression of hepatitis C virus proteins induces distinct membrane alterations including a candidate viral replication complex. J. Virol. 76:5974-5984. (Pubitemid 34556292)
9. Failla C, Tomei L, De Francesco R. 1994. Both NS3 and NS4A are required for proteolytic processing of hepatitis C virus nonstructural proteins. J. Virol. 68:3753-3760. (Pubitemid 24177400)
10. Flint M, et al. 2009. Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034). Antimicrob. Agents Chemother. 53:401-411.
11. Foote BS, Spooner LM, Belliveau PP. 9 August 2011, posting date. Boceprevir: a protease inhibitor for the treatment of chronic hepatitis C. Ann. Pharmacother. 45:1085-1093.
12. Fridell RA, Qiu D, Wang C, Valera L, Gao M. 2010. Resistance analysis of the HCV NS5A inhibitor BMS-790052 in the in vitro replicon system. Antimicrob. Agents Chemother. 54:3641-3650.
13. Fridell RA, et al. 2011. Genotypic and phenotypic analysis of variants resistant to hepatitis C virus nonstructural protein 5A replication complex inhibitor BMS-790052 in humans: in vitro and in vivo correlations. Hepatology 54:1924-1935.
14. Gane EJ, et al. 2010. Oral combination therapy with a nucleoside polymerase inhibitor (RG7128) and danoprevir for chronic hepatitis C genotype 1 infection (INFORM-1): a randomised, double-blind, placebo-controlled, dose-escalation trial. Lancet 376:1467-1475.
15. Gao M, et al. 2010. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature 465:96-100.
16. Gentile I, Carleo MA, Borgia F, Castaldo G, Borgia G. 2010. The efficacy and safety of telaprevir - a new protease inhibitor against hepatitis C virus. Expert Opin. Invest. Drugs 19:151-159.
17. Grakoui A, McCourt DW, Wychowski C, Feinstone SM, Rice CM. 1993. A second hepatitis C virus-encoded proteinase. Proc. Natl. Acad. Sci. U. S. A. 90:10583-10587. (Pubitemid 23347086)
18. Jacobson IM, et al. 2011. Telaprevir for previously untreated chronic hepatitis C virus infection. N. Engl. J. Med. 364:2405-2416.
19. Kieffer TL, Kwong AD, Picchio GR. 2010. Viral resistance to specifically targeted antiviral therapies for hepatitis C (STAT-Cs). J. Antimicrob. Chemother. 65:202-212.
20. Kneteman NM, et al. 2009. HCV796: a selective nonstructural protein 5B polymerase inhibitor with potent anti-hepatitis C virus activity in vitro, in mice with chimeric human livers, and in humans infected with hepatitis C virus. Hepatology 49:745-752.
21. Kronenberger B, Zeuzem S. 2008. Future treatment options for HCV: double, triple, what is the optimal combination? Best Pract. Res. Clin. Gastroenterol. 22:1123-1136.
22. Kronenberger B, Zeuzem S. 2009. Treatment of chronic hepatitis C: anticipated impact of resistance in patients treated with protease inhibitors. Curr. Gastroenterol. Rep. 11:15-21.
23. Kukolj G, et al. 2005. Binding site characterization and resistance to a class of non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase. J. Biol. Chem. 280:39260-39267. (Pubitemid 41713879)
24. Kwong AD, Kim JL, Rao G, Lipovsek D, Raybuck SA. 1999. Hepatitis C virus NS3/4A protease. Antiviral Res. 41:67-84.
25. Lamarre D, et al. 2003. An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus. Nature 426:186-189. (Pubitemid 37442587)
26. Legrand-Abravanel F, Nicot F, Izopet J. 2010. New NS5B polymerase inhibitors for hepatitis C. Expert Opin. Invest. Drugs 19:963-975.
27. Lemm JA, et al. 2010. Identification of hepatitis C virus NS5A inhibitors. J. Virol. 84:482-491.
28. Lenz O, Verbinnen et al. 2010. In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. Antimicrob. Agents Chemother. 54:1878-1887.
29. Le Pogam S, et al. 2006. Selection and characterization of replicon variants dually resistant to thumb- and palm-binding nonnucleoside polymerase inhibitors of the hepatitis C virus. J. Virol. 80:6146-6154. (Pubitemid 43849192)
30. Lin K. 2010. Development of novel antiviral therapies for hepatitis C virus. Virol. Sin. 25:246-266.
31. Lin K, Perni RB, Kwong AD, Lin C. 2006. VX-950, a novel hepatitis C virus (HCV) NS3-4A protease inhibitor, exhibits potent antiviral activities in HCV replicon cells. Antimicrob. Agents Chemother. 50:1813-1822.
32. Liverton NJ, et al. 2010. MK-7009, a potent and selective inhibitor of hepatitis C virus NS3/4A protease. Antimicrob. Agents Chemother. 54:305-311.
33. Lohmann V, Koch JO, Bartenschlager R. 1996. Processing pathways of the hepatitis C virus proteins. J. Hepatol. 24(2 Suppl):11-19. (Pubitemid 26267058)
34. Lok AS, et al. 2012. Preliminary study of two antiviral agents for hepatitis C genotype 1. N. Engl. J. Med. 366:216-224.
35. Love RA, Brodsky O, Hickey MJ, Wells PA, Cronin CN. 2009. Crystal structure of a novel dimeric form of NS5A domain I protein from hepatitis C virus. J. Virol. 83:4395-4403.
36. Lu L, et al. 2004. Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro. Antimicrob. Agents Chemother. 48:2260-2266. (Pubitemid 38691627)
37. Macdonald A, Harris M. 2004. Hepatitis C virus NS5A: tales of a promiscuous protein. J. Gen. Virol. 85(Pt 9):2485-2502. (Pubitemid 39214345)
38. McPhee F, et al. 2012. Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir. Antimicrob. Agents Chemother. 56:3670-3681.
39. McPhee F, et al. 2009. The discovery and early development of the HCV NS3 protease inhibitor BMS-605339. Global Antiviral J. 5(Suppl 1):51.
40. Miyanari Y, et al. 2007. The lipid droplet is an important organelle for hepatitis C virus production. Nat. Cell Biol. 9:1089-1097. (Pubitemid 47338147)
41. Neddermann P, Clementi A, De Francesco R. 1999. Hyperphosphorylation of the hepatitis C virus NS5A protein requires an active NS3 protease, NS4A, NS4B, and NS5A encoded on the same polyprotein. J. Virol. 73:9984-9991.
42. Nettles RE, et al. 2011. Multiple ascending dose study of BMS-790052, a nonstructural protein 5A replication complex inhibitor, in patients infected with hepatitis C virus genotype 1. Hepatology 54:1956-1965.
43. O'Boyle DR, Jr, et al. 2005. Development of a cell-based high-throughput specificity screen using a hepatitis C virus-bovine viral diarrhea virus dual replicon assay. Antimicrob. Agents Chemother. 49:1346-1353.
44. Ohara E, et al. 2011. Elimination of hepatitis C virus by short term NS3-4A and NS5B inhibitor combination therapy in human hepatocyte chimeric mice. J. Hepatol. 54:872-878.
45. Pasquinelli C, et al. 2012. Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C. Antimicrob. Agents Chemother. 56:1838-1844.
46. Pierra C, et al. 2006. Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2′-C- methylcytidine. J. Med. Chem. 49:6614-6620. (Pubitemid 44657456)
47. Poordad F, et al. 2011. Boceprevir for untreated chronic HCV genotype 1 infection. N. Engl. J. Med. 364:1195-1206.
48. Qin W, et al. 2001. Mutational analysis of the structure and functions of hepatitis C virus RNA-dependent RNA polymerase. Hepatology 33:728-737. (Pubitemid 32185237)
49. Romano KP, Ali A, Royer WE, Schiffer CA. 2010. Drug resistance against HCV NS3/4A inhibitors is defined by the balance of substrate recognition versus inhibitor binding. Proc. Natl. Acad. Sci. U. S. A. 107:20986-20991.
50. Rydberg EH, et al. 2009. Structural basis for resistance of the genotype 2b hepatitis C virus NS5B polymerase to site A non-nucleoside inhibitors. J. Mol. Biol. 390:1048-1059.
51. Sarrazin C, Zeuzem S. 2010. Resistance to direct antiviral agents in patients with hepatitis C virus infection. Gastroenterology 138:447-462.
52. Sarrazin C, Hézode C, Zeuzem S, Pawlotsky JM. 2012. Antiviral strategies in hepatitis C virus infection. J. Hepatol. 56(Suppl):S88-S100.
53. Seiwert SD, et al. 2008. Preclinical characteristics of the hepatitis C virus NS3/4A protease inhibitor ITMN-191 (R7227). Antimicrob. Agents Chemother. 52:4432-4441.
54. Shepard CW, Finelli L, Alter MJ. 2005. Global epidemiology of hepatitis C virus infection. Lancet Infect. Dis. 5:558-567. (Pubitemid 41196755)
55. Shirota Y, et al. 2002. Hepatitis C virus (HCV) NS5A binds RNA-dependent RNA polymerase (RdRP) NS5B and modulates RNA-dependent RNA polymerase activity. J. Biol. Chem. 277:11149-11155. (Pubitemid 34952876)
56. Soriano V, Peters MG, Zeuzem S. 2009. New therapies for hepatitis C virus infection. Clin. Infect. Dis. 48:313-320.
57. Susser S, et al. 2009. Characterization of resistance to the protease inhibitor boceprevir in hepatitis C virus-infected patients. Hepatology 50:1709-1718.
58. Tellinghuisen T, Foss KL, Treadaway J. 2008. Regulation of hepatitis C virion production via phosphorylation of the NS5A protein. PLoS Pathog. 4:e1000032. doi:10.1371/journal.ppat.1000032.
59. Tellinghuisen TL, Marcotrigiano J, Rice CM. 2005. Structure of the zinc-binding domain of an essential component of the hepatitis C virus replicase. Nature 435:374-379. (Pubitemid 40745549)
60. Thompson AJ, McHutchison JG. 2009. Antiviral resistance and specifically targeted therapy for HCV (STAT-C). J. Viral Hepatol. 16:377-387.
61. Tong X, et al. 2008. Characterization of resistance mutations against HCV ketoamide protease inhibitors. Antiviral Res. 77:177-185.
62. Zheng X, et al. 2011. Syntheses and initial evaluation of a series of indolo-fused heterocyclic inhibitors of the polymerase enzyme (NS5B) of the hepatitis C virus. Bioorg. Med. Chem. Lett. 21:2925-2929.