Estimation of inhibitory quotient using a comparative equilibrium dialysis assay for prediction of viral response to hepatitis C virus inhibitors

Journal of Viral Hepatitis

Volumn 18, Issue 5, 2011, Pages 338-348

  Mo, H ^a   Yang, C ^a   Wang, K ^a   Wang, Y ^a   Huang, M ^b   Murray, B ^a   Qi, X ^a   Sun, S C ^a   Deshpande, M ^b   Rhodes, G ^a   Miller, M D ^a  

^a GILEAD SCIENCES   (United States)

^b Achillion Pharmaceuticals Inc   (United States)

Author keywords

comparative equilibrium dialysis; hepatitis C virus inhibitors; inhibitory quotient; viral response

Indexed keywords

ANTIVIRUS AGENT; BOCEPREVIR; CILUPREVIR; GS 9132; TELAPREVIR; UNCLASSIFIED DRUG;

ARTICLE; ASSAY; COMPARATIVE EQUILIBRIUM DIALYSIS ASSAY; CULTURE MEDIUM; DRUG MECHANISM; HEPATITIS C VIRUS; HUMAN; INHIBITORY QUOTIENT; MAXIMUM PLASMA CONCENTRATION; MEASUREMENT; NONHUMAN; PLASMA; PREDICTION; PRIORITY JOURNAL;

ANTIVIRAL AGENTS; BLOOD PROTEINS; CARBAMATES; CELL LINE; COMPARATIVE EFFECTIVENESS RESEARCH; DIALYSIS; HEPACIVIRUS; HEPATITIS C; HUMANS; INHIBITORY CONCENTRATION 50; MACROCYCLIC COMPOUNDS; MEMBRANES, ARTIFICIAL; OLIGOPEPTIDES; PHENYLTHIOUREA; PLASMA; PROLINE; PROTEASE INHIBITORS; PROTEIN BINDING; QUINOLINES; RNA, VIRAL; THIAZOLES; VIRAL LOAD;

EID: 79953846185     PISSN: 13520504     EISSN: 13652893     Source Type: Journal    
DOI: 10.1111/j.1365-2893.2010.01314.x     Document Type: Article

References (32)

1. Zeuzem S, Buti M, Ferenci P, et al. Efficacy of 24 weeks treatment with peginterferon alfa-2b plus ribavirin in patients with chronic hepatitis C infected with genotype 1 and low pretreatment viremia. J Hepatol 2006; 44 (1): 97-103. (Pubitemid 41772522)
2. Schalm SW, Weiland O, Hansen BE, et al. Interferon-ribavirin for chronic hepatitis C with and without cirrhosis: analysis of individual patient data of six controlled trials. Eurohep Study Group for Viral Hepatitis. Gastroenterology 1999; 117 (2): 408-413. (Pubitemid 29352950)
3. McHutchison JG,. Hepatitis C advances in antiviral therapy: what is accepted treatment now? J Gastroenterol Hepatol 2002; 17 (4): 431-441.
4. Sarrazin C, Rouzier R, Wagner F, et al. SCH 503034, a novel hepatitis C virus protease inhibitor, plus pegylated interferon alpha-2b for genotype 1 nonresponders. Gastroenterology 2007; 132 (4): 1270-1278. (Pubitemid 46627577)
5. Roberts SK, Cooksley G, Dore GJ, et al. Robust antiviral activity of R1626, a novel nucleoside analog: a randomized, placebo-controlled study in patients with chronic hepatitis C. Hepatology (Baltimore, MD) 2008; 48 (2): 398-406.
6. Kieffer TL, Sarrazin C, Miller JS, et al. Telaprevir and pegylated interferon-alpha-2a inhibit wild-type and resistant genotype 1 hepatitis C virus replication in patients. Hepatology (Baltimore, MD) 2007; 46 (3): 631-639. (Pubitemid 47436107)
7. 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 (5): 1347-1355. (Pubitemid 39457761)
8. Yang W, Zhao Y, Fabrycki J, et al. Selection of replicon variants resistant to ACH-806, a novel hepatitis C virus inhibitor with no cross-resistance to NS3 protease and NS5B polymerase inhibitors. Antimicrob Agents Chemother 2008; 52 (6): 2043-2052. (Pubitemid 351758541)
9. 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): 186-189. (Pubitemid 37442587)
10. Herrmann E, Zeuzem S, Sarrazin C, et al. Viral kinetics in patients with chronic hepatitis C treated with the serine protease inhibitor BILN 2061. Antivir Ther 2006; 11 (3): 371-376. (Pubitemid 43823556)
11. 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 (4): 997-1002. (Pubitemid 44498690)
12. Forestier N, Reesink HW, Weegink CJ, et al. Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C. Hepatology (Baltimore, MD) 2007; 46 (3): 640-648. (Pubitemid 47436108)
13. Seiwert S, Hong J, Lim S, Tan H, Kossen K, Blatt L,. Sequence variation of NS3 and NS4A in hepatitic C virus (HCV) replicons following exposure ti ITMN-191 concentrations likely to encompass those achieved in human liver following clinical dosing. Reviews in Antiviral Therapy, 1st int Workshop Hepatitis C Resistance and New Compounds, Boston, MA abstr 2 2007; 1: 56-57.
14. Pottage JCJ, Lawitz E, Mazur D, et al. Short-term antiviral activity and safety of ACH-806 (GS-9132), an NS4A antagonist, in HCV genotype 1 infected individuals. Presentation at EASL 2007-42nd Annual Meeting, Barcelona, Spain. J Hepatol Suppl 2007; 46: A783.
15. Ellner PD, Neu HC,. The inhibitory quotient. A method for interpreting minimum inhibitory concentration data. JAMA 1981; 246 (14): 1575-1578. (Pubitemid 11000076)
16. Gatti G, Castelli-Gattinara G, Cruciani M, et al. Pharmacokinetics and pharmacodynamics of nelfinavir administered twice or thrice daily to human immunodeficiency virus type 1-infected children. Clin Infect Dis 2003; 36 (11): 1476-1482. (Pubitemid 36702882)
17. Hsu A, Isaacson J, Brun S, et al. Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2003; 47 (1): 350-359. (Pubitemid 36070384)
18. Gatti G, Vigano A, Sala N, et al. Indinavir pharmacokinetics and pharmacodynamics in children with human immunodeficiency virus infection. Antimicrob Agents Chemother 2000; 44 (3): 752-755. (Pubitemid 30117973)
19. Hoefnagel JG, Koopmans PP, Burger DM, Schuurman R, Galama JM,. Role of the inhibitory quotient in HIV therapy. Antivir Ther 2005; 10 (8): 879-892. (Pubitemid 43076339)
20. Fischl MA, Richman DD, Saag M, et al. Safety and antiviral activity of combination therapy with zidovudine, zalcitabine, and two doses of interferon-alpha2a in patients with HIV. AIDS Clinical Trials Group Study 197. J Acquir Immune Defic Syndr Hum Retrovirol 1997; 16 (4): 247-253.
21. Bilello JA, Drusano GL,. Relevance of plasma protein binding to antiviral activity and clinical efficacy of inhibitors of human immunodeficiency virus protease. J Infect Dis 1996; 173 (6): 1524-1526. (Pubitemid 26286824)
22. Molla A, Vasavanonda S, Kumar G, et al. Human serum attenuates the activity of protease inhibitors toward wild-type and mutant human immunodeficiency virus. Virology 1998; 250 (2): 255-262. (Pubitemid 28489625)
23. Gatti G, Di Biagio A, Casazza R, et al. The relationship between ritonavir plasma levels and side-effects: implications for therapeutic drug monitoring. AIDS (London, England) 1999; 13 (15): 2083-2089. (Pubitemid 29509585)
24. Vrolijk JM, Kwekkeboom J, Janssen LLA, et al. Pretreatment intrahepatic CD8+ cell count correlates with virological response to antiviral therapy in chronic hepatitis C virus infection. J Infect Dis 2003; 188 (10): 1528-1532. (Pubitemid 37523938)
25. Zeuzem S, Sarrazin C, Tarral A, et al. Anti-viral activity of SCH 503034, a HCV protease inhibitor, administered as monotherapy in hepatitis C genotype -1(HCV-1) patients refractory to pegylated interferon (PEG-IFN-alpha), Presentation at 45th AASLD, November 11-15, 2005, San Francisco, Abstract 94. Hepatology 2005; 42 (4) (suppl1): 233A.
26. Lu L, Pilot-Matias TJ, Stewart KD, et al. Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro. Antimicrob Agents Chemother 2004; 48 (6): 2260-2266. (Pubitemid 38691627)
27. Lin C, Gates CA, Rao BG, et al. In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061. J Biol Chem 2005; 280 (44): 36784-36791. (Pubitemid 41587758)
28. Lin C, Kwong AD, Perni RB,. Discovery and development of VX-950, a novel, covalent, and reversible inhibitor of hepatitis C virus NS3.4A serine protease. Infect Disord Drug Targets 2006; 6 (1): 3-16. (Pubitemid 43796632)
29. Malcolm BA, Liu R, Lahser F, et al. SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells. Antimicrob Agents Chemother 2006; 50 (3): 1013-1020. (Pubitemid 43327807)
30. 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 (Baltimore, MD) 2005; 41 (4): 832-835. (Pubitemid 40462946)
31. Barrail-Tran A, Morand-Joubert L, Poizat G, et al. Predictive values of the human immunodeficiency virus phenotype and genotype and of amprenavir and lopinavir inhibitory quotients in heavily pretreated patients on a ritonavir-boosted dual-protease-inhibitor regimen. Antimicrob Agents Chemother 2008; 52 (5): 1642-1646. (Pubitemid 351614655)
32. Hickman D, Vasavanonda S, Nequist G, et al. Estimation of serum-free 50-percent inhibitory concentrations for human immunodeficiency virus protease inhibitors lopinavir and ritonavir. Antimicrob Agents Chemother 2004; 48 (8): 2911-2917. (Pubitemid 38989155)