Potency, safety, and pharmacokinetics of the NS3/4A protease inhibitor BI201335 in patients with chronic HCV genotype-1 infection

Journal of Hepatology

Volumn 54, Issue 6, 2011, Pages 1114-1122

  Manns, Michael P ^a   Bourlire, Marc ^b   Benhamou, Yves ^c   Pol, Stanislas ^d   Bonacini, Maurizio ^e   Trepo, Christian ^f   Wright, David ^g   Berg, Thomas ^h   Calleja, José L ⁱ   White, Peter W ^j   Stern, Jerry O ^k   Steinmann, Gerhard ^l   Yong, Chan Loi ^k   Kukolj, George ^j   Scherer, Joe ^k   Boecher, Wulf O ^l  

^a HANNOVER MEDICAL SCHOOL   (Germany)

^b HÔPITAL SAINT JOSEPH   (France)

^c PITIÉ SALPÊTRIÈRE HOSPITAL   (France)

^d Hopital Cochin ^*  (France)

^e CALIFORNIA PACIFIC MEDICAL CENTER   (United States)

^f HÔTEL DIEU   (France)

^g Central Texas Clinical Research   (United States)

^h CHARITÉ UNIVERSITÄTSMEDIZIN BERLIN   (Germany)

ⁱ HOSPITAL UNIVERSITARIO PUERTA DE HIERRO   (Spain)

^j BOEHRINGER INGELHEIM CANADA LTD   (Canada)

^k BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

^l BOEHRINGER INGELHEIM PHARMA GMBH AND CO KG   (Germany)

more..

Author keywords

Antiviral; Hepatitis C virus; Pegylated interferon; Resistant variants; Ribavirin

Indexed keywords

ALANINE AMINOTRANSFERASE; ALKALINE PHOSPHATASE; ANTIVIRUS AGENT; ASPARTATE AMINOTRANSFERASE; BI 201335; BILIRUBIN; GAMMA GLUTAMYLTRANSFERASE; HEMOGLOBIN; PEGINTERFERON ALPHA; PLACEBO; RIBAVIRIN; UNCLASSIFIED DRUG; VIRUS RNA;

ADULT; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ANEMIA; ANTIVIRAL THERAPY; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; ASTHENIA; CATARACT; COMBINATION CHEMOTHERAPY; DOSE RESPONSE; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG HALF LIFE; DRUG POTENCY; DRUG SAFETY; DRUG TOLERABILITY; ERYTHEMA; FATIGUE; FEMALE; GASTROINTESTINAL DISEASE; GENETIC VARIABILITY; GENOTYPE; HEADACHE; HEMOLYSIS; HEPATITIS C; HEPATITIS C VIRUS; HUMAN; HYPERBILIRUBINEMIA; LEUKOCYTE COUNT; LIMIT OF DETECTION; LIVER TOXICITY; MAJOR CLINICAL STUDY; MALE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; MULTICENTER STUDY; NAUSEA; PHOTOSENSITIVITY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RASH; SIDE EFFECT; STEADY STATE; THROMBOCYTE COUNT; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT DURATION; TREATMENT RESPONSE; VIRUS GENE; VIRUS LOAD; VIRUS RESISTANCE;

ADULT; ANTIVIRAL AGENTS; CARRIER PROTEINS; DOUBLE-BLIND METHOD; DRUG RESISTANCE, VIRAL; FEMALE; HEPACIVIRUS; HEPATITIS C; HUMANS; INTERFERON ALFA-2A; MALE; MIDDLE AGED; OLIGOPEPTIDES; POLYETHYLENE GLYCOLS; PROTEASE INHIBITORS; RIBAVIRIN; THIAZOLES; VIRAL LOAD; VIRAL NONSTRUCTURAL PROTEINS;

EID: 79953224799     PISSN: 01688278     EISSN: 01688278     Source Type: Journal    
DOI: 10.1016/j.jhep.2010.08.040     Document Type: Article

References (22)

1. M.P. Manns, J.G. McHutchison, S.C. Gordon, V.K. Rustgi, M. Shiffman, and R. Reindollar Peginterferon alfa-2b plus ribavirin compared with interferon alfa-2b plus ribavirin for initial treatment of chronic hepatitis C: a randomised trial Lancet 358 2001 958 965 (Pubitemid 32913521)
2. M.W. Fried, M.L. Shiffman, K.R. Reddy, C. Smith, G. Marinos, and F.L. Gonales Jr. Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection N Engl J Med 347 2002 975 982
3. M.P. Manns, G.R. Foster, J.K. Rockstroh, S. Zeuzem, F. Zoulim, and M. Houghton The way forward in HCV treatment - finding the right path Nat Rev Drug Discov 6 2007 991 1000 (Pubitemid 350201789)
4. M.P. Manns, K.L. Lindsay, S.C. Gordon, P.J. Pockros, D. Haeussinger, and S. Hadziyiannis Sustained virologic response after peginterferon alfa-2b and ribavirin treatment predicts long-term clearance of HCV at 5-year follow-up J Hepatol 48 2008 S300
5. M.G. Ghany, D.B. Strader, D.L. Thomas, and L.B. Seeff Diagnosis, management, and treatment of hepatitis C: an update Hepatology 49 2009 1335 1374
6. D. Lamarre, P.C. Anderson, M. Bailey, P. Beaulieu, G. Bolger, and P. Bonneau An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus Nature 426 2003 186 189 (Pubitemid 37442587)
7. H. Hinrichsen, Y. Benhamou, H. Wedemeyer, M. Reiser, R.E. Sentjens, and J.L. Calleja Short-term antiviral efficacy of BILN 2061, a hepatitis C virus serine protease inhibitor, in hepatitis C genotype 1 patients Gastroenterology 127 2004 1347 1355 (Pubitemid 39457761)
8. M. Reiser, H. Hinrichsen, Y. Benhamou, H.W. Reesink, H. Wedemeyer, and C. Avendano Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C Hepatology 41 2005 832 835 (Pubitemid 40462946)
9. J.G. McHutchison, G.T. Everson, S.C. Gordon, I.M. Jacobson, M. Sulkowski, and R. Kauffman Telaprevir with peginterferon and ribavirin for chronic HCV genotype 1 infection N Engl J Med 360 2009 1827 1838
10. C. Hézode, N. Forestier, G. Dusheiko, P. Ferenci, S. Pol, and T. Goeser Telaprevir and peginterferon with or without ribavirin for chronic HCV infection N Engl J Med 360 2009 1839 1850
11. P. Kwo, E. Lawitz, J. McCone, E. Schiff, J. Vierling, and D. Pound Interim results from HCV SPRINT 1: RVR/EVR from phase 2 study of boceprevir plus Pegintron (peginterferon alfa-2b)/ribavirin in treatment - naive subjects with HCV genotype 1 CHC J Hepatol 48 2008 S372
12. Struble K. Invited lecture on bridging studies. 4th International Workshop on Clinical Pharmacology of Hepatitis Therapy. Boston, MA; 2009.
13. H.W. Reesink, S. Zeuzem, C.J. Weegink, N. Forestier, A. van Vliet, and J. de Rooij Rapid decline of viral RNA in hepatitis C patients treated with VX-950: a phase 1b, placebo-controlled randomized study Gastroenterology 131 2006 997 1002 (Pubitemid 44498690)
14. S. Zeuzem, C. Sarrarin, R. Rouzier, A. Tarral, N. Brion, and N. Forestier Anti-viral activity of SCH 503034, a HCV protease inhibitor, administered as monotherapy in hepatitis C genotype-1 patients refractory to pegylated interferon (PEGIFN-alfa) Hepatology 42 2005 233A
15. C. Sarrazin, T.L. Kieffer, D. Bartels, B. Hanzelka, U. Müh, and M. Welker Dynamic hepatitis C virus genotypic and phenotypic changes in patients treated with the protease inhibitor telaprevir Gastroenterology 132 2007 1767 1777 (Pubitemid 46677938)
16. C. Lin, C.A. Gates, B.G. Rao, D.L. Brennan, J.R. Fulghum, and Y.P. Luong In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061 J Biol Chem 280 2005 36784 36791 (Pubitemid 41587758)
17. Y.S. Tsantrizos TMC-435, an NS3/4A protease inhibitor for the treatment of HCV infection Curr Opin Investig Drugs 10 2009 871 881
18. J.G. McHutchison, E.J. Lawitz, M.L. Shiffman, A.J. Muir, G.W. Galler, and J. McCone Peginterferon alfa-2b or alfa-2a with ribavirin for treatment of hepatitis C infection N Engl J Med 361 2009 580 593
19. M.S. Sulkowski, P. Ferenci, C. Emanoil, T. Asselah, F. Caruntu, and J. Lalezari SILEN-C1: early antiviral activity and safety of BI 201335 combined with peginterferon alfa-2a and ribavirin in treatment-naïve patients with chronic genotype 1 HCV infection Hepatology 50 2009 2A
20. M.S. Sulkowski, M. Bourliere, J.-P. Bronowicki, A. Streinu-Cercel, L. Preotescu, and T. Asselah SILEN-C2: early antiviral activity and safety or BI 201335 combined with peginterferon alfa-2a and ribavirin (PegIFN/RBV) in chronic HCV genotype-1 patients with non-response to PegIFN/RBV J Hepatol 52 2010 S462
21. D. Zhang, T.J. Chando, D.W. Everett, C.J. Patten, S.S. Dehal, and W.G. Humphreys In vitro inhibition of UDP glucuronosyltransferases by atazanavir and other HIV protease inhibitors and the relationship of this property to in vivo bilirubin glucuronidation Drug Metab Dispos 33 2005 1729 1739 (Pubitemid 41539973)
22. T.O. Lankisch, U. Moebius, M. Wehmeier, G. Behrens, M.P. Manns, and R.E. Schmidt Gilbert's disease and atazanavir: from phenotype to UDP- glucuronosyltransferase haplotype Hepatology 44 2006 1324 1332 (Pubitemid 44748383)