Drug resistance testing in hepatitis C therapy

Future Virology

Volumn 7, Issue 3, 2012, Pages 309-321

  Poveda, Eva ^a   Soriano, Vincent ^a  

^a HOSPITAL UNIVERSITARIO LA PAZ   (Spain)

Author keywords

DAA; hepatitis C; resistance

Indexed keywords

ANTIVIRUS AGENT; BI 7127; BOCEPREVIR; DACLATASVIR; FILIBUVIR; MERICITABINE; MIRAVIRSEN; NONSTRUCTURAL PROTEIN 3; NONSTRUCTURAL PROTEIN 5A; PSI 7977; PSI 938; TEGOBUVIR; TELAPREVIR; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; ANTIVIRAL THERAPY; COVALENT BOND; CROSS RESISTANCE; DISSOCIATION; DOSE RESPONSE; DRUG BINDING; DRUG EFFICACY; DRUG POTENCY; DRUG SAFETY; ENZYME ACTIVITY; GENETIC POLYMORPHISM; GENETIC VARIABILITY; HEPATITIS C; HUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRACTICE GUIDELINE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REPLICON; REVIEW; TREATMENT DURATION; TREATMENT RESPONSE; VIRUS INHIBITION; VIRUS MUTANT; VIRUS MUTATION;

HEPATITIS C VIRUS;

EID: 84858421432     PISSN: 17460794     EISSN: 17460808     Source Type: Journal    
DOI: 10.2217/fvl.12.13     Document Type: Review

References (69)

1. European Association for the Study of the Liver. EASL Clinical Practice Guidelines: Management of hepatitis C virus infection. J. Hepatol. 55, 245-264 (2011).
2. McHutchison J, Lawitz E, Shiffman M et al. Peginterferon alfa-2b or alfa-2a with ribavirin for treatment of hepatitis C infection. N. Engl. J. Med. 361, 580-593 (2009).
3. Hadziyannis S, Sette H, Morgan T et al. Peginterferon-a 2a and ribavirin combination therapy in chronic hepatitis C: A randomized study of treatment duration and ribavirin dose. Ann. Intern. Med. 140, 346-355 (2004).
4. Poordad F, McCone J, Bacon B et al. Boceprevir for untreated chronic HCV genotype 1 infection. N. Engl. J. Med. 364, 1195-1206 (2011).
5. Bacon B, Gordon S, Lawitz E et al. Boceprevir for previously treated chronic HCV genotype 1 infection. N. Engl. J. Med. 364, 1207-1217 (2011).
6. Jacobson I, McHutchison J, Dusheiko G et al. Telaprevir for previously untreated chronic hepatitis C virus infection. N. Engl. J. Med. 364, 2405-2416 (2011).
7. Zeuzem S, Andreone P, Pol S et al. Telaprevir for retreatment of HCV infection. N. Engl. J. Med. 364, 2417-2428 (2011).
8. Soriano V, Vispo E, Poveda E et al. Directly acting antivirals against hepatitis C virus. J. Antimicrob. Chemother. 66, 1673-1686 (2011). n Reviews the main features of molecules in more advanced stages of clinical development for the treatment of chronic hepatitis C.
9. De Meyer S, Dierynck I, Ghys A et al. Similar incidence of virological failure and emergence of resistance with or without a lead-in: Results of a telaprevir Phase 3 study in patients who did not achieve SVR with prior Peg-IFN/RBV treatment. Antivir. Ther. 16(Suppl. 1), A25 (2011).
10. Lenz O, Vijgen L, Moreno C et al. Virological response and characterization of HCV genotypes 2 to 6 under TMC435 monotherapy (study TMC435-C202). Antivir. Ther. 16(Suppl. 1), A24 (2011).
11. McPhee F, Hernandez D, Yu F et al. Characterization of virologic escape in HCV genotype 1 null responders receiving a combination of the NS3 protease inhibitor BMS-650032 and NS5A inhibitor BMS-790052. J. Hepatol. 54(Suppl. 1), 28-29 (2011).
12. Pawlotsky JM, Chevaliez S, McHutchison J. The hepatitis C virus life cycle as a target for new antiviral therapies. Gastroenterology, (132), 1979-1998 (2007).
13. Sherman K, Flamm S, Afdhal N et al. Response-guided telaprevir combination treatment for hepatitis C virus infection. N. Engl. J. Med. 365, 1014-1024. (2011).
14. Marcellin P, Forns X, Goeser T et al. Telaprevir is effective given every 8 or 12hours with ribavirin and peginterferon alfa-2a or 2b to patients with chronic hepatitis C. Gastroenterology 140, 459-468 (2011).
15. Poveda E, Vispo E, Barreiro P et al. Predicted challenges using direct acting antivirals in the current HIV-HCV coinfected population in Spain. Antivir. Ther. (2012) (In Press).
16. Sulkowski M, Asselah T, Ferenci P et al. Treatment with the 2nd generation HCV protease inhibitor BI201335 results in high and consistent SVR rates -results from SILEN-C1 in treatment-naive patients across different baseline factors. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). SanFrancisco, CA, USA, 5-8 November 2011.
17. Dietrich D, Asselah T, Guyader D et al. Treatment for 12 or 24 weeks with BI201335 combined with peginterferon alfa-2a and ribavirin (P/R) in treatment-naive patients with chronic genotype-1 HCV infection. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8 November 2011.
18. Terrault N, Cooper C, Balar LA et al. High sustained virologic response (SVR24) rates with response-guided danoprevir (DNV; RG7227) plus PegIFN a-2a (40KD) and ribavirin (P/R) in treatment-naive HCV genotype 1 (G1) patients: Results from the ATLAS study. Presented at: 62nd AnnualMeeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8 November 2011.
19. Fried M, Buti M, Dore G et al. TMC435 in combination with peginterferon and ribavirin in treatment-naive HCV genotype 1 patients: Final analysis of the PILLAR phase IIb study. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8 November 2011.
20. Jensen D, Wedemeyer H, Herring R et al. High rates of early viral response, promising safety profile and lack of resistance-related breakthrough in HCV GT 1/4 patients treated with RG-7128 plus pefIFN-a-2a/RBV: Planned week 12 interim analysis from the PROPEL study. Presented at: 61st AnnualMeeting of the American Association for the Study of Liver Diseases (AASLD). Boston, MA, USA, 30 October-2 November 2010.
21. Pockros P, Jensen D, Tsai N et al. First SVR data with the nucleoside analogue polymerase inhibitor mericitabine (RG-7128) combined with peginterferon/ribavirin in treatment-naive HCV G1/4 patients: Interim analysis from the JUMP-C trial. Presented at: 46th EASL Annual Meeting. Berlin, Germany, 30March-3 April, 2011.
22. Nelson D, Lalezari J, Lawitz E et al. Once daily PSI-9777 plus pegIFN/RBV in HCV GT1: 98% rapid virologic response, complete early virologic response: PROTON study. Presented at: 46th EASL Annual Meeting. Berlin, Germany, 30 March-3 April 2011.
23. Lawitz E, Lalerzari J, Hassanein T et al. Once-daily PSI-7977 plus peg/RBV in treatment-naive patients with HCV GT1: Robust end of treatment response rates are sustained post-treatment. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). SanFrancisco, CA, USA, 5-8 November 2011.
24. Gane E, Stedman C, Hyland R et al. Once daily PSI-7977 plus RBV: Pegylated interferon-alfa not required for complete rapid viral response in treatment-naive patients with HCV GT2 or GT3. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). SanFrancisco, CA, USA, 5-8 November 2011.
25. Lawitz E, Rodriguez-Torres M, Denning M et al. Once daily dual-nucleotide combination of PSI-938 and PSI-7977 provides 94% HCV RNA
26. Bressanelli S, Tomei L, Rey F et al. Structural analysis of the hepatitis C virus RNA polymerase in complex with ribonucleotides. J. Virol. 76, 3482-3492 (2002).
27. De Francesco R, Carfi A. Advances in the development of new therapeutic agents targeting NS3-4A serine protease or the NS5b RNA-dependent RNA polymerase of the hepatitis C virus. Adv. Drug Del. Rev. 59, 1242-1262 (2007).
28. Lawitz E, Jacobson I, Godofsky E et al. A Phase 2b trial comparing 24 to 48 weeks treatment with tegobuvir (GS-9190)/peg/RBV to 48 weeks treatment with PEG/RBV for chronic genotype 1 HCV infection. Presented at: 46th EASL Annual Meeting. Berlin, Germany, 30 March-3 April 2011.
29. Foster G, Buggisch P, Marcellin P et al. Four-week treatment with GS-9256 and tegobuvir (GS-9190), ± RBV ± PEG, results in enhanced viral suppression on follow-up PEG/RBV therapy, in genotype 1a/1b HCV patients. Presented at: 46th EASL Annual Meeting. Berlin, Germany, 30 March-3 April 2011.
30. Jacobson I, Pockros P, Lalezari J et al. Virologic response rates following 4 weeks of filibuvir in combination with pegylated interferon a-2a and ribavirin in chronically infected HCV genotype 1 patients. J. Hepatol. 52(Suppl.), 465 (2010).
31. Larrey D, Benhamoy Y, Lohse A et al. BI-207127 is a potent HCV RNA polymerase inhibitor during 5 days monotherapy in patients with chronic hepatitis C. Presented at: 61st Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). Boston, MA, USA, 30October-2November 2010.
32. Larrey D, Lohse A, de Ledinghen V et al. 4-week therapy with the non-nucleoside polymerase inhibitor BI-207127 in combination with peginterferon a-2a and ribavirin in treatment naive and treatment experienced chronic HCV GT1 patients. J. Hepatol. 52(Suppl.), 466 (2010).
33. Zeuzem S, Asselah T, Angus P et al. Strong antiviral activity and safety of IFN-sparing treatment with the protease inhibitor BI-201335, the HCV polymerase inhibitor BI-207127, and ribavirin, in patients with chronic hepatitis C: The SOUND-C1 trial. Presented at: 61st Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). Boston, MA, USA, 30October-2 November 2010.
34. Zeuzem S, Soriano V, Asselah T et al. Virologic response to an interferon-free regimen of BI201335 and BI207127, with and without ribavirin, in treatment-naive patients with chronic genotype-1 HCV infection: Week12 interim results of the SOUND-C2 study. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8 November 2011.
35. Gao M, Nettles R, Belema M et al. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature 465, 96-100 (2010).
36. Chayama K, Takahashi S, Kawakami Y et al. Dual oral combination therapy with the NS5A inhibitor BMS-790052 and the NS3 protease inhibitor BMS-650032 achieved 90% sustained virologic response (SVR12) in HCV genotype 1b-infected null responders. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8 November 2011.
37. Huang M, Yang G, Patel D et al. ACH-2928: A novel highly potent HCV NS5A inhibitor with favorable preclinical characteristics. Presented at: 46th EASL Annual Meeting. Berlin, Germany, 30 March-3 April 2011.
38. Coelmont L, Hanoulle X, Chatterji U et al. DEB-025 (alisporivir) inhibits HCV replication by preventing a cyclophilin A induced cis-trans isomerisation in domain II of NS5A. PLoS One 5, E13687 (2010).
39. Fernandes F, Ansari IH, Striker R. Cyclosporine inhibits a direct interaction between cyclophylins and hepatitis C NS5A. PLos One 5, e9815 (2010).
40. Janssen H, Reesink H, Zeuzem S et al. A randomized, double-blind, placebo (PLB) controlled safety and anti-viral proof of concept study of miravirsen (MIR), an oligonucleotide targeting miR-122, in treatment naive patients with genotype 1 (GT1) chronic HCV infection. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). San Francisco, CA, USA, 5-8November 2011.
41. Domingo E, Gomez J. Quasispecies and its impact on viral hepatitis. Virus Res. 127, 131-150 (2007).
42. Franco S, Parera M, Aparicio E et al. Genetic and catalytic efficiency sturucture of an HCV protease quasispecies. Hepatology 45, 899-910 (2007).
43. Kieffer T, Sarrazin C, Miller J et al. Telaprevir and pegylated interferon-alpha-2a inhibit wild-type and resistant genotype 1 hepatitis C virus replication in patients. Hepatology 46, 631-639 (2007).
44. Kieffer TL, Kwong AD, Picchio GR. Viral resistance to specifically targeted antiviral therapies for hepatitis C (STAT-Cs). J. Antimicrob. Chemother. 65, 202-212 (2010).
45. Sarrazin C, Zeuzem S. Resistance to direct antiviral agents in patients with hepatitis C virus infection. Gastroenterology 138, 447-462 (2010). n Outstanding review about drug resistance in HCV.
46. Halfon P, Locarnini S. Hepatitis C virus resistance to protease inhibitors. J. Hepatol. 55, 192-206 (2011).
47. Ludmerer S, Graham D, 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. 49, 2059-2069 (2005).
48. Bartels D, Zhou Y, Zhang E et al. Natural prevalence of HCV variants with decreased sensitivity to NS3-4A protease inhibitors in treatment-naive subjects. J. Infect. Dis. 198, 800-807 (2008).
49. Kuntzen T, Timm J, Berical A et al. Naturally occurring dominant resistance mutations to HCV protease and polymerase inhibitors in treatment-naive patients. Hepatology 48, 1769-1778 (2008).
50. Gaudieri S, Rauch A, Pfafferott K et al. Hepatitis C virus drug resistance and immune-driven adaptations: Relevance to new antiviral therapy. Hepatology 49, 1069-1082 (2009).
51. Sun S, Bae A, Qi X et al. Natural variation in drug susceptibility to HCV polymerase inhibitors in treatment-naive HCV patient isolates. J. Viral. Hepat. (18), 861-870 (2011).
52. Trimoulet P, Belzunce C, Faure M et al. HCV protease variability and anti-HCV protease inhibitor resistance in HIV/HCV-coinfected patients. HIV Med. 12, 506-509 (2011).
53. Treviño A, de Mendoza C, Parra P et al. Natural polymorphisms associated with resistance to new antivirals against hepatitis C virus (HCV) in newly diagnosed HIV/HCV-coinfected patients in Spain. Antivir. Ther. 16, 413-416 (2011). n Assesses the prevalence of natural polymorphisms to HCV protease and polymerase inhibitors in newly diagnosed HIV/HCV-coinfected population.
54. Plaza Z, Soriano V, Gonzalez MM et al. Impact of antiretroviral therapy on the variability of the HCV NS5B polymerase in HIV/HCV co-infected patients. J. Antimicrob. Chemother. 66, 2838-2842 (2011). n Evaluates the potential impact of antiretroviral therapy against HIV infection on the variability of HCV NS5B polymerase inhibitors in HIV/HCV-coinfected patients.
55. Plaza Z, Soriano V, Vispo E et al. Prevalence of natural polymorphisms at the Hepatitis C virus NS5A gene associated with resistance to daclatasvir, a NS5A inhibitor. Antivir. Ther. (2012) (In Press).
56. Bae A, Sun S, Qi X et al. Susceptibility of treatment-naive HCV clinical isolates to HCV protease inhibitors. Antimicrob. Agents Chemother. 54, 5288-5297 (2010).
57. Fridell R, Qiu D, Wang C, Valera L, Gao M. Resistance analysis of the hepatitis C virus NS5A inhibitor BMS-790052 in an in vitro replicon system. Antimicrob. Agents Chemother. 54, 3641-3650 (2010).
58. McCown M, Rajyaguru S, Kular S, Cammack N, Najera I. GT-1a or GT-1b subtype-specific resistance profiles for hepatitis C virus inhibitors telaprevir and HCV-796. Antimicrob. Agents Chemother. 53, 2129-2132 (2009).
59. Kieffer T, De Meyer S, Bartels D et al. Clinical virology findings from treatment-naive and treatment-experienced genotype 1 HCV patients receiving telaprevir/peginterferon/ribavirin in Phase 3 clinical trials. Antivir. Ther. 16(Suppl. 1), A27 (2011).
60. Graham D, Acosta A, Guo Z et al. MK-5172, a second generation HCV NS3/4a protease inhibitor is active against common resistance associated variants (RAVS) and exhibits cross-genotype activity. Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). SanFrancisco, CA, USA, 5-8 November 2011.
61. Barnad R, Strizki J, Miller M et al. The association of boceprevir (BOC) resistance-associated amino acid variants (RAVs) detected at baseline and treatment outcomes in patients from the SPRINT-2 and RESPOND-2 clinical studies. Antivir. Ther. 16(Suppl. 1), A26 (2011).
62. Chevaliez S, Rodriguez C, Soulier et al. Molecular characteriztion of HCV resistance to telaprevir by means of UDPS: Pre-existing resistant variants and dynamics of resistant populations. Antivir. Ther. 16(Suppl. 1), A31 (2011).
63. Margeridon-Thermet S, Le Pogam S, Liu T et al. Ultra-deep sequencing of the NS3 and NS5B regions detects pre-existing resistant variants to direct acting antivirals (DAA) in HCV genotype 1 infected patients naive. Antivir. Ther. 16(Suppl. 1), A33 (2011).
64. Lam A, Espiritu C, Bansal S et al. HCV replicon resistance for PSI-352938 and PSI-353661, prodrugs of 2'-a-F2'-b-C-methylguanosine, is mediated through multiple amino acid changes. Antivir. Ther. 16(Suppl. 1), A23 (2011).
65. Schinazi R, Zhang H, Zhou L et al. Synthesis and characterization of picomolar inhibitors of HCV NS5A in hepatocytes. Antivir. Ther. 16(Suppl. 1), A22 (2011).
66. Soriano V, Perelson A, Zoulim F. Why different dynamics of selection of drug resistance in HIV, hepatitis B and C viruses? J. Antimicrob. Chemother. 62, 1-4 (2008).
67. Sarrazin C, Kieffer T, Bartels D et al. Dynamic hepatitis C virus genotypic and phenotypic changes in patients treated with the protease inhibitor telaprevir. Gastroenterology 132, 1767-1777 (2007).
68. Sarrazin C, Reesink H, Zeuzem S et al. Re-treatment with telaprevir/peg-IFN/RBV after a short exposure to telaprevir in phase I studies: Interim results from a phase IIIB rollover trial (C219). Presented at: 62nd Annual Meeting of the American Association for the Study of Liver Diseases (AASLD). SanFrancisco, CA, USA, 5-8 November 2011.
69. Ghany M, Nelson D, Strader D et al. An update on treatment of genotype 1 chronic hepatitis C virus infection: 2011 practice guideline by the American Association for the Study of Liver Diseases. Hepatology 54, 1433-1444 (2011). n Practice guideline approved by the American Association for the Study of Liver Diseases, which provides clinical recommendations for the treatment of genotype 1 chronic HCV infection with direct-acting antivirals.