Hepatitis C virus directly acting antivirals: Current developments with NS3/4A HCV serine protease inhibitors

Journal of Antimicrobial Chemotherapy

Volumn 65, Issue 10, 2010, Pages 2063-2069

  Naggie, Susanna ^a,b,c   Patel, Keyur ^a,b   McHutchison, John ^a,b  

^a DUKE CLINICAL RESEARCH INSTITUTE   (United States)

^b DUKE UNIVERSITY MEDICAL CENTER   (United States)

^c DURHAM VA MEDICAL CENTER   (United States)

Author keywords

Interferon; Polymerase inhibitors; Resistance; Ribavirin; STAT C; Targeted therapy

Indexed keywords

4' AZIDOCYTIDINE 2',3',5' TRIISOBUTYRATE; ABT 072; ABT 333; ACH 1625; BI 201335; BMS 650032; BOCEPREVIR; CILUPREVIR; GS 9190; GS 9256; IDX 184; ITMN 191; MK 3281; N [[[6 (2 CARBOXY 2,3 DIHYDRO 1H ISOINDOL 4 YL) 2,2 DIMETHYLHEXYL]OXY]CARBONYL] 3 METHYLVALYL 4 HYDROXYPROLYL 1 AMINO N (CYCLOPROPYLSULFONYL) 2 ETHYLCYCLOPROPANECARBOXAMIDE LACTONE; NONSTRUCTURAL PROTEIN 3; NONSTRUCTURAL PROTEIN 5B; PEGINTERFERON; PEGINTERFERON ALPHA; PSI 7851; R 7128; RIBAVIRIN; SERINE PROTEINASE INHIBITOR; TELAPREVIR; TMC 435350; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALOPICITABINE; VIRUS RNA; VX 222; VX 759; VX 985;

AMINO ACID SUBSTITUTION; ANEMIA; ANTIVIRAL ACTIVITY; ANTIVIRAL SUSCEPTIBILITY; ANTIVIRAL THERAPY; ARTICLE; CARDIOTOXICITY; CLINICAL TRIAL; DIARRHEA; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG ERUPTION; DRUG POTENTIATION; DRUG TOLERABILITY; DRUG WITHDRAWAL; DYSGEUSIA; ENZYME INHIBITION; HEPATITIS C; HEPATITIS C VIRUS; HUMAN; MONOTHERAPY; NAUSEA; NONHUMAN; PRURITUS; SINGLE NUCLEOTIDE POLYMORPHISM; TREATMENT DURATION; TREATMENT RESPONSE; VIRUS LOAD; VIRUS REPLICATION;

ANTIVIRAL AGENTS; CARRIER PROTEINS; CLINICAL TRIALS AS TOPIC; DRUG RESISTANCE, VIRAL; HEPATITIS C, CHRONIC; HUMANS; INTERFERON ALFA-2A; INTERFERON ALFA-2B; POLYETHYLENE GLYCOLS; RIBAVIRIN; SERPINS; VIRAL NONSTRUCTURAL PROTEINS; VIRAL PROTEINS; VIRUSES;

EID: 77957229293     PISSN: 03057453     EISSN: 14602091     Source Type: Journal    
DOI: 10.1093/jac/dkq284     Document Type: Article

References (36)

1. Lavanchy D. The global burden of hepatitis C. Liver Int 2009; 29 Suppl s1: 74-81.
2. Viral Hepatitis Topics. http://www.cdc.gov/hepatitis/statistics.htm (27 May 2010, date last accessed).
3. Kim WR. The burden of hepatitis C in the United States. Hepatology 2002; 36: S30-4.
4. Dienstag JL, McHutchison JG. American Gastroenterological Association technical review on the management of hepatitis C. Gastroenterology 2006; 130: 231-64.
5. Ghany MG, Strader DB, Thomas DL et al. Diagnosis, management, and treatment of hepatitis C. Hepatology 2009; 49: 1335-74.
6. Muir AJ, Bornstein JD, Killenberg PG. Peginterferon alfa-2b and ribavirin for the treatment of chronic hepatitis C in blacks and non-hispanic whites. N Engl J Med 2004; 350: 2265-71.
7. Conjeevaram HS, Fried MW, Jeffers LJ et al. Peginterferon and ribavirin treatment in African American and Caucasian American patients with hepatitis C genotype 1. Gastroenterology 2006; 131: 470-7.
8. Rodriguez-Torres M, Jeffers LJ, Sheikh MY et al. Peginterferon alfa-2a and ribavirin in Latino and non-Latino whites with hepatitis C. N Engl J Med 2009; 360: 257-67.
9. Choo QL, Richman KH, Han JH et al. Genetic organization and diversity of the hepatitis C virus. Proc Natl Acad Sci USA 1991; 88: 2451-5.
10. Pawlotsky JM, Chevaliez S, McHutchison JG. The hepatitis C virus life cycle as a target for new antiviral therapies. Gastroenterology 2007; 132: 1979-98.
11. Thompson AJV, McHutchison JG. Review article: investigational agents for chronic hepatitis C. Aliment Pharmacol Ther 2009; 29: 689-705.
12. Lohmann V, Korner F, Koch J et al. Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line. Science 1999; 285: 110-3.
13. 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: 791-6.
14. Thimme R, Lohmann V, Weber F. A target on the move: innate and adaptive immune escape strategies of hepatitis C virus. Antiviral Res 2006; 69: 129-41.
15. Li K, Foy E, Ferreon JC et al. Immune evasion by hepatitis C virus NS3/4A protease-mediated cleavage of the Toll-like receptor 3 adaptor protein TRIF. Proc Natl Acad Sci USA 2005; 102: 2992-7.
16. Loo YM, Owen DM, Li K et al. Viral and therapeutic control of IFN-beta promoter stimulator 1 during hepatitis C virus infection. Proc Natl Acad Sci USA 2006; 103: 6001-6.
17. 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: 1347-55.
18. McHutchison JG, Everson GT, Gordon SC et al. Telaprevir with peginterferon and ribavirin for chronic HCV genotype 1 infection. N Engl J Med 2009; 360: 1827-38.
19. Hezode C, Forestier N, Dusheiko G et al. Telaprevir and peginteferon with or without ribavirin for chronic HCV infection. N Engl J Med 2009; 360: 1839-50.
20. Foster GR, Hezode C, Bronowicki JP et al. Activity of telaprevir alone or in combination with peginterferon alfa-2a and ribavirin in treatment-naïve genotype 2 and 3 hepatitis-C patients: interim results of study C209. J Hepatology 2009; 50: S22.
21. Benhamou Y, Moussali J, Ratziu V et al. Results of a proof of concept study (C210) of telaprevir monotherapy and in combination with peginterferon alpha-2A and ribavirin in treatment-naive genotype 4 HCV patients. J Hepatology 2009; 50: S6.
22. Kwo P, Lawitz EJ, McCone J et al. HCV SPRINT-1: boceprevir plus peginterferon alpha-2B/ribavirin for treatment of genotype 1 chronic hepatitis C in previously untreated patients. J Hepatology 2008; 48: S372.
23. Reesink HW, Zeuzem S, Weegink CJ et al. Rapid decline of viral RNA in hepatitis C patients treated with VX-950: a phase Ib, placebo-controlled, randomized study. Gastroenterology 2006; 131: 997-1002.
24. 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: 1767-77.
25. Forestier N, Reesink HW, Weegink CJ et al. Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C. Hepatology 2007; 46: 640-8.
26. Gane EJ, Roberts SK, Stedman CA et al. Combination therapy with a nucleoside polymerase (R7128) and protease (R7227/ITMN-191) inhibitor in HCV: safety, pharmacokinetics, and virologic results from INFORM-1. J Hepatology 2009; 50: S380.
27. Chu H, Zhou Y, Bartels D et al. Telaprevir (VX 950)-resistant variants exhibit reduced replication capacity compared to wild-type HCV in vivo and in vitro. J Hepatology 2007; 46: S230-1.
28. Pawlotsky JM, Dahari H, Neumann AU et al. Antiviral action of ribavirin in chronic hepatitis C. Gastroenterology 2004; 126: 703-14.
29. Bronowicki JP, Ouzan D, Asselah T et al. Effect of ribavirin in genotype 1 patients with hepatitis C responding to pegylated interferon alfa-2a plus ribavirin. Gastroenterology 2006; 131: 1040-8.
30. McHutchison JG, Manns MP, Muir A et al. Telaprevir for previously treated chronic HCV infection. New Engl J Med 2010; 362: 1292-303.
31. Schiff E, Poordad F, Jacobson I et al. Boceprevir (B) combination therapy in null responders (NR): response dependent on interferon responsiveness. J Hepatol 2008; 48: S46.
32. Ge D, Fellay J, Thompson AJ et al. Genetic variation in IL28B predicts hepatitis C treatment-induced viral clearance. Nature 2009; 461: 399-401.
33. Suppiah V, Moldovan M, Ahlenstiel G et al. IL28B is associated with response to chronic hepatitis C interferon-α and ribavirin therapy. Nature Genetics 2009; 41: 1100-4.
34. Tanaka Y, Nishida N, Sugiyama M et al. Genome-wide association of IL28B with response to pegylated interferon-a and ribavirin therapy for chronic hepatitis C. Nature Genetics 2009; 41: 1105-9.
35. Thomas DL, Thio CL, Martin MP et al. Genetic variation in IL28B and spontaneous clearance of hepatitis C virus. Nature 2009; 461: 798-802.
36. Thompson AJ, Muir AJ, Sulkowski MS et al. Interleukin-28B polymorphism improves viral kinetics and is the strongest pretreatment predictor of sustained virologic response in genotype 1 hepatitis C virus. Gastroenterology 2010; 139: 120-9.