Simeprevir for the treatment of chronic hepatitis C genotype 1 infection

Expert Review of Anti-Infective Therapy

Volumn 12, Issue 8, 2014, Pages 909-917

  Takehara, Tetsuo ^a  

^a OSAKA UNIVERSITY GRADUATE SCHOOL OF MEDICINE   (Japan)

Author keywords

direct acting antiviral; hepatitis C virus; peginterferon; protease inhibitor; Simeprevir

Indexed keywords

BOCEPREVIR; PEGINTERFERON; PEGINTERFERON ALPHA2A PLUS RIBAVIRIN; PLACEBO; RIBAVIRIN; SIMEPREVIR; TELAPREVIR; ALPHA INTERFERON; ANTIVIRUS AGENT; FUSED HETEROCYCLIC RINGS; MACROGOL DERIVATIVE; PEGINTERFERON ALPHA2A; PEGINTERFERON ALPHA2B; RECOMBINANT PROTEIN; SULFONAMIDE; VIRUS RNA;

ANEMIA; ANTIVIRAL ACTIVITY; DRUG EFFICACY; DRUG ERUPTION; DRUG POTENTIATION; DRUG SAFETY; DRUG TOLERABILITY; GASTROINTESTINAL SYMPTOM; HEPATITIS C; HEPATITIS C VIRUS GENOTYPE 1; HUMAN; HYPERBILIRUBINEMIA; MONOTHERAPY; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); RASH; REVIEW; TREATMENT DURATION; VIROLOGY; BLOOD; CHEMICAL STRUCTURE; CHEMISTRY; CLINICAL TRIAL (TOPIC); DRUG ADMINISTRATION; DRUG COMBINATION; DRUG DESIGN; DRUG EFFECTS; DRUG SCREENING; GENETICS; GENOTYPE; HEPACIVIRUS; HEPATITIS C, CHRONIC; TREATMENT OUTCOME;

ANTIVIRAL AGENTS; CLINICAL TRIALS AS TOPIC; DRUG ADMINISTRATION SCHEDULE; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; DRUG THERAPY, COMBINATION; GENOTYPE; HEPACIVIRUS; HEPATITIS C, CHRONIC; HETEROCYCLIC COMPOUNDS, 3-RING; HUMANS; INTERFERON-ALPHA; MOLECULAR STRUCTURE; POLYETHYLENE GLYCOLS; RECOMBINANT PROTEINS; RIBAVIRIN; RNA, VIRAL; SULFONAMIDES; TREATMENT OUTCOME;

EID: 84903964582     PISSN: 14787210     EISSN: 17448336     Source Type: Journal    
DOI: 10.1586/14787210.2014.925800     Document Type: Review

References (28)

1. WHO. Available from: www.who.int/ mediacentre/factsheets/fs164/en/index. html
2. Hayashi N, Takehara T. Antiviral therapy for chronic hepatitis C: past, present, and future. J Gastroenterol 2006;41(1):17-27
3. Muir AJ. Telaprevir for the treatment of chronic hepatitis C infection. Expert Rev Anti Infect Ther 2011;9(12):1105-14
4. You DM, Pockros PJ. Simeprevir for the treatment of chronic hepatitis C. Expert Opin Pharmacother 2013;14(18):2581-9
5. Lohmann V, Körner F, Koch J, et al. Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line. Science 1999;285(5424):110-13
6. Kim JL, Morgenstern KA, Lin C, et al. Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide. Cell 1996; 87(2):343-55
7. 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):186-9
8. 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):832-5
9. Mauss S, Hueppe D, Alshuth U. Renal impairment is frequent in chronic hepatitis C patients under triple therapy with telaprevir or boceprevir. Hepatology 2014; 59(1):46-8
10. Raboisson P, de Kock H, Rosenquist A, et al. Structure-activity relationship study on a novel series of cyclopentane-containing macrocyclic inhibitors of the hepatitis C virus NS3/4A protease leading to the discovery of TMC435350. Bioorg Med Chem Lett 2008;18(17):4853-8
11. Lin TI, Lenz O, Fanning G, et al. In vitro activity and preclinical profile of TMC435350, a potent hepatitis C virus protease inhibitor. Antimicrob Agents Chemother 2009;53(4):1377-85
12. Lenz O, Verbinnen T, Lin TI, et al. In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435. Antimicrob Agents Chemother 2010;54(5): 1878-87
13. Reesink HW, Fanning GC, Farha KA, et al. Rapid HCV-RNA decline with once daily TMC435: a phase I study in healthy volunteers and hepatitis C patients. Gastroenterology 2010;138(3):913-21
14. Manns M, Reesink H, Berg T, et al. Rapid viral response of once-daily TMC435 plus pegylated interferon/ribavirin in hepatitis C genotype-1 patients: a randomized trial. Antivir Ther 2011;16(7):1021-33
15. Moreno C, Berg T, Tanwandee T, et al. Antiviral activity of TMC435 monotherapy in patients infected with HCV genotypes 2- 6: TMC435-C202, a phase IIa, open-label study. J Hepatol 2012;56(6):1247-53
16. Lenz O, Vijgen L, Berke JM, et al. Virologic response and characterisation of HCV genotype 2-6 in patients receiving TMC435 monotherapy (study TMC435- C202). J Hepatol 2013;58(3):445-51
17. Fried MW, Buti M, Dore GJ, et al. Once-daily simeprevir (TMC435) with pegylated interferon and ribavirin in treatment-naïve genotype 1 hepatitis C: the randomized PILLAR study. Hepatology 2013;58(6):1918-29
18. Hayashi N, Seto C, Kato M, et al. Once-daily simeprevir (TMC435) with peginterferon/ribavirin for treatment-naïve hepatitis C genotype 1-infected patients in Japan: the DRAGON study. J Gastroenterol 2014;49(1):138-47
19. Zeuzem S, Berg T, Gane E, et al. Simeprevir Increases Rate of Sustained Virologic Response Among Treatment-Experienced Patients With HCV Genotype-1 Infection: a Phase IIb Trial. Gastroenterology 2014;146(2):430-41
20. Jacobson GL, Dore GR, Foster MW, et al. Simeprevir (TMC435) with peginterferon/ ribavirin for chronic HCV genotype-1 infection in treatment-naïve patinets: results from QUEST-1, a phase III trial. EASL 2013, Late-braker #1425
21. Manns M, Marcellin P, Fred Poordad FP, et al. Simeprevir (TMC435) with peginterferon/ribavirin for treatment of chronic HCV genotype-1 infection in treatment-naïve patients: results from QUEST-1, a phase II trial. EASL 2013, Late-breaker #1413
22. Forns X, Lawitz E, Zeuzem S, et al. Simeprevir with peginterferon and ribavirin leads to high rates of SVR in patients with HCV genotype 1 who relapsed after previous therapy: a phase III trial. Gastroenterology 2014. [Epub ahead of print]
23. Hayashi N, Izumi N, Kumada H, et al. Simeprevir with peginterferon/ ribavirin for treatment-naïve hepatitis c genotype 1 patients in Japan: CONCERTO-1, a Phase III trial. J Hepatol 2014. [Epub ahead of print]
24. Izumi N, Hayashi N, Kumada H, et al. Once-daily simeprevir with peginterferon and ribavirin for treatment-experienced HCV genotype 1-infected patients in Japan: The CONCERTO-2 and -3 studies. J Gastroenterol 2014;49(5):941-53
25. Hiramatsu N, Takehara T, Hayashi N, et al. Pooled analysis of CONCERTO Studies: Simeprevir (TMC435) Combination Therapy for Genotype-1 HCV Infection (Poster). APASL; 2014
26. Lawitz E, Lalezari JP, Hassanein T, et al. Sofosbuvir in combination with peginterferon alfa-2a and ribavirin for non-cirrhotic, treatment-naive patients with genotypes 1, 2, and 3 hepatitis C infection: a randomised, double-blind, phase 2 trial. Lancet Infect Dis 2013;13(5):401-8
27. Chayama K, Takahashi S, Toyota J, et al. Dual therapy with the nonstructural protein 5A inhibitor, daclatasvir, and the nonstructural protein 3 protease inhibitor, asunaprevir, in hepatitis C virus genotype 1b-infected null responders. Hepatology 2012;55(3):742-8
28. Lawitz E, Poordad FF, Pang PS, et al. Sofosbuvir and ledipasvir fixed-dose combination with and without ribavirin in treatment-naive and previously treated patients with genotype 1 hepatitis C virus infection (LONESTAR): an open-label, randomised, phase 2 trial. Lancet 2014; 383(9916):515-23