Daclatasvir: The first of a new class of drugs targeted against hepatitis C virus NS5A

Current Medicinal Chemistry

Volumn 21, Issue 12, 2014, Pages 1391-1404

  Gentile, I ^a   Borgia, F ^a,b   Coppola, N ^c   Buonomo, A R ^a   Castaldo, G ^a,b   Borgia, G ^a  

^a UNIVERSITY OF NAPLES FEDERICO II   (Italy)

^b CEINGE BIOTECNOLOGIE AVANZATE   (Italy)

^c SECOND UNIVERSITY OF NAPLES   (Italy)

Author keywords

Combination therapy; Daclatasvir; Hepatitis C virus; Interferon free; Pegylated interferon; Polymerase inhibitors; Resistance; Ribavirin

Indexed keywords

AMINOTRANSFERASE; ANTIVIRUS AGENT; ASUNAPREVIR; BECLABUVIR; BILIRUBIN; DACLATASVIR; ETHINYLESTRADIOL PLUS NORGESTIMATE; HEMOGLOBIN; NONSTRUCTURAL PROTEIN 5A; PEGINTERFERON; PEGINTERFERON ALPHA; PEGINTERFERON ALPHA2A; PEGINTERFERON LAMBDA; PLACEBO; RIBAVIRIN; SOFOSBUVIR; VIRUS RNA;

ALOPECIA; AMINO ACID SUBSTITUTION; AMINOTRANSFERASE BLOOD LEVEL; ANEMIA; ANTIVIRAL ACTIVITY; ARTHRALGIA; BILIRUBIN BLOOD LEVEL; CONSTIPATION; DIARRHEA; DOSE RESPONSE; DRUG ABSORPTION; DRUG DOSE REDUCTION; DRUG EFFECT; DRUG EFFICACY; DRUG EXCRETION; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG RESPONSE; DRUG SAFETY; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; FATIGUE; FEVER; GASTROENTERITIS; GENE MUTATION; HEADACHE; HEMOGLOBIN BLOOD LEVEL; HEPATITIS C; HEPATITIS C VIRUS; HEPATITIS C VIRUS GENOTYPE 1; HEPATITIS C VIRUS GENOTYPE 2; HEPATITIS C VIRUS GENOTYPE 3; HEPATITIS C VIRUS GENOTYPE 4; HUMAN; HYPERBILIRUBINEMIA; HYPOCHONDRIASIS; IN VITRO STUDY; MONOTHERAPY; NAUSEA; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); RANDOMIZED CONTROLLED TRIAL (TOPIC); RELAPSE; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; SUSTAINED VIROLOGICAL RESPONSE; TREATMENT OUTCOME; VIRUS LOAD; VIRUS RESISTANCE;

ANTIVIRAL AGENTS; CLINICAL TRIALS AS TOPIC; DRUG COMBINATIONS; HEPACIVIRUS; HUMANS; IMIDAZOLES; VIRAL NONSTRUCTURAL PROTEINS;

EID: 84898439254     PISSN: 09298673     EISSN: 1875533X     Source Type: Journal    
DOI: 10.2174/0929867321666131228222215     Document Type: Review

References (101)

1. Lavanchy, D. Evolving epidemiology of hepatitis C virus. Clin. Microbiol. Infect., 2011, 17(2), 107-115.
2. Sagnelli, E.; Stroffolini, T.; Mele, A.; Almasio, P.; Coppola, N.; Ferrigno, L.; Scolastico, C.; Onofrio, M.; Imparato, M.; Filippini, P. The importance of HCV on the burden of chronic liver disease in Italy: a multicenter prevalence study of 9,997 cases. J. Med. Virol., 2005, 75(4), 522-527.
3. Petruzziello, A.; Coppola, N.; Diodato, A.M.; Iervolino, V.; Azzaro, R.; Di Costanzo, G.; Di Macchia, C.A.; Di Meo, T.; Loquercio, G.; Pasquale, G.; Cacciapuoti, C. Age and gender distribution of hepatitis C virus genotypes in the metropolitan area of Naples. Intervirology, 2013, 56(3), 206-212.
4. Gentile, I.; Di Flumeri, G.; Scarica, S.; Frangiosa, A.; Foggia, M.; Reynaud, L.; Borgia, G. Acute hepatitis C in patients undergoing hemodialysis: experience with high-dose interferon therapy. Minerva Urol. Nefrol., 2013, 65(1), 83-84.
5. Gentile, I.; De Stefano, A.; Di Flumeri, G.; Buonomo, A.R.; Carlomagno, C.; Morisco, F.; De Placido, S.; Borgia, G. Concomitant interferon-alpha and chemotherapy in hepatitis C and colorectal cancer: a case report. In Vivo, 2013, 27(4), 527-529.
6. Sagnelli, E.; Tonziello, G.; Pisaturo, M.; Sagnelli, C.; Coppola, N. Clinical applications of antibody avidity and immunoglobulin M testing in acute HCV infection. Antivir. Ther., 2012, 17(7 Pt B), 1453-1458.
7. Sagnelli, E.; Coppola, N.; Marrocco, C.; Coviello, G.; Battaglia, M.; Messina, V.; Rossi, G.; Sagnelli, C.; Scolastico, C.; Filippini, P. Diagnosis of hepatitis C virus related acute hepatitis by serial determination of IgM anti-HCV titres. J. Hepatol., 2005, 42(5), 646-651.
8. Coppola, N.; Pisapia, R.; Marrocco, C.; Martini, S.; Vatiero, L.M.; Messina, V.; Tonziello, G.; Sagnelli, C.; Filippini, P.; Piccinino, F.; Sagnelli, E. Anti-HCV IgG avidity index in acute hepatitis C. J. Clin. Virol., 2007, 40(2), 110-115.
9. Coppola, N.; Pisapia, R.; Tonziello, G.; Masiello, A.; Martini, S.; Pisaturo, M.; Messina, V.; Sagnelli, C.; Macera, M.; Signoriello, G.; Sagnelli, E. Improvement in the aetiological diagnosis of acute hepatitis C: a diagnostic protocol based on the anti-HCV-IgM titre and IgG Avidity Index. J. Clin. Virol., 2009, 46(3), 222-229.
10. Hoofnagle, J.H. Hepatitis C: the clinical spectrum of disease. Hepatology, 1997, 26(3 Suppl 1), 15S-20S.
11. Sagnelli, E.; Pisaturo, M.; Stanzione, M.; Messina, V.; Alessio, L.; Sagnelli, C.; Starace, M.; Pasquale, G.; Coppola, N. Presentation, Outcomes, and Response to Therapy Among Patients with Acute Exacerbation of Chronic Hepatitis C. Clin. Gastroenterol. Hepatol., 2013, 13(13), 00466-00467.
12. Gentile, I.; Coppola, N.; Pasquale, G.; Liuzzi, R.; D'Armiento, M.; Di Lorenzo, M.E.; Capoluongo, N.; Buonomo, A.R.; Sagnelli, E.; Morisco, F.; Caporaso, N.; Borgia, G. A simple noninvasive score based on routine parameters can predict liver cirrhosis in patients with chronic Hepatitis C. Hepatitis Monthly, 2013, 13(5), e8352.
13. Gentile, I.; Meola, M.; Buonomo, A.R.; Minei, G.; Coppola, N.; Foggia, M.; Ferruzzi, F.; Fratellanza, G.; Scarpato, N.; Borgia, G. Human platelet antigen-3 genotype predicts platelet count in patients with HCV infection. In Vivo, 2013, 27(6), 773-777.
14. Alazawi, W.; Cunningham, M.; Dearden, J.; Foster, G.R. Systematic review: outcome of compensated cirrhosis due to chronic hepatitis C infection. Aliment. Pharmacol. Ther., 2010, 32(3), 344-355.
15. Menzin, J.; White, L.A.; Nichols, C.; Deniz, B. The economic burden of advanced liver disease among patients with hepatitis C virus: a large state Medicaid perspective. BMC Health Serv. Res., 2012, 12(459), 1472-6963.
16. Ferri, C.; Antonelli, A.; Mascia, M.T.; Sebastiani, M.; Fallahi, P.; Ferrari, D.; Pileri, S.A.; Zignego, A.L. HCV-related autoimmune and neoplastic disorders: the HCV syndrome. Dig. Liver Dis., 2007, 39(1), S13-S21.
17. Fallahi, P.; Di Domenicantonio, A.; Mazzi, V.; Santini, F.; Fabiani, S.; Sebastiani, M.; Zignego, A.L.; Ferri, C.; Antonelli, A. Hepatitis C virus and type 1 diabetes. Clin. Ter., 2013, 164(5), 437-444.
18. Fusco, F.; D'Anzeo, G.; Rossi, A.; Sciorio, C.; Buonomo, A.R.; d'Emmanuele di Villa Bianca, R.; Borgia, G.; Mirone, V.; Gentile, I. Erectile dysfunction in patients with chronic viral hepatitis: a systematic review of the literature. Expert Opin. Pharmacother., 2013, 14(8), 2533-2544.
19. Morisco, F.; Granata, R.; Stroffolini, T.; Guarino, M.; Donnarumma, L.; Gaeta, L.; Loperto, I.; Gentile, I.; Auriemma, F.; Caporaso, N. Sustained virological response: A milestone in the treatment of chronic hepatitis C. World J. Gastroenterol., 2013, 19(18), 2793-2798.
20. Gentile, I.; Borgia, G. Surrogate endpoints and non-inferiority trials in chronic viral hepatitis. J. Hepatol., 2010, 52(5), 778.
21. Bruno, S.; Stroffolini, T.; Colombo, M.; Bollani, S.; Benvegnu, L.; Mazzella, G.; Ascione, A.; Santantonio, T.; Piccinino, F.; Andreone, P.; Mangia, A.; Gaeta, G.B.; Persico, M.; Fagiuoli, S.; Almasio, P.L. Sustained virological response to interferon-alpha is associated with improved outcome in HCV-related cirrhosis: a retrospective study. Hepatology, 2007, 45(3), 579-587.
22. Braks, R.E.; Ganne-Carrie, N.; Fontaine, H.; Paries, J.; Grando-Lemaire, V.; Beaugrand, M.; Pol, S.; Trinchet, J.C. Effect of sustained virological response on long-term clinical outcome in 113 patients with compensated hepatitis C-related cirrhosis treated by interferon alpha and ribavirin. World J. Gastroenterol., 2007, 13(42), 5648-5653.
23. Di Marco, V.; Almasio, P.L.; Ferraro, D.; Calvaruso, V.; Alaimo, G.; Peralta, S.; Di Stefano, R.; Craxi, A. Peg-interferon alone or combined with ribavirin in HCV cirrhosis with portal hypertension: a randomized controlled trial. J. Hepatol., 2007, 47(4), 484-491.
24. Backus, L.I.; Boothroyd, D.B.; Phillips, B.R.; Belperio, P.; Halloran, J.; Mole, L.A. A sustained virologic response reduces risk of all-cause mortality in patients with hepatitis C. Clin. Gastroenterol. Hepatol., 2011, 9(6), 509-516.
25. Ghany, M.G.; Strader, D.B.; Thomas, D.L.; Seeff, L.B. Diagnosis, management, and treatment of hepatitis C: an update. Hepatology, 2009, 49(4), 1335-1374.
26. Coppola, N.; Pisaturo, M.; Tonziello, G.; Sagnelli, C.; Sagnelli, E.; Angelillo, I.F. Efficacy of Pegylated interferon alpha-2a and alpha-2b in patients with genotype 1 chronic hepatitis C: a meta-analysis. BMC Infect. Dis., 2012, 12(357), 1471-2334.
27. Venkatraman, S.; Bogen, S.L.; Arasappan, A.; Bennett, F.; Chen, K.; Jao, E.; Liu, Y.T.; Lovey, R.; Hendrata, S.; Huang, Y.; Pan, W.; Parekh, T.; Pinto, P.; Popov, V.; Pike, R.; Ruan, S.; Santhanam, B.; Vibulbhan, B.; Wu, W.; Yang, W.; Kong, J.; Liang, X.; Wong, J.; Liu, R.; Butkiewicz, N.; Chase, R.; Hart, A.; Agrawal, S.; Ingravallo, P.; Pichardo, J.; Kong, R.; Baroudy, B.; Malcolm, B.; Guo, Z.; Prongay, A.; Madison, V.; Broske, L.; Cui, X.; Cheng, K.C.; Hsieh, Y.; Brisson, J.M.; Prelusky, D.; Korfmacher, W.; White, R.; Bogdanowich-Knipp, S.; Pavlovsky, A.; Bradley, P.; Saksena, A.K.; Ganguly, A.; Piwinski, J.; Girijavallabhan, V.; Njoroge, F.G. Discovery of (1R,5S)-N-[3-amino-1- (cyclobutylmethyl)-2,3- dioxopropyl]- 3-[2(S)-[[[(1,1-dimethylethyl)amino] carbonyl]amino]- 3,3-dimethyl-1-oxobutyl]- 6,6-dimethyl-3-azabicyclo[3.1.0] hexan- 2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor: a potential therapeutic agent for the treatment of hepatitis C infection. J. Med. Chem., 2006, 49(20), 6074-6086.
28. Tong, X.; Chase, R.; Skelton, A.; Chen, T.; Wright-Minogue, J.; Malcolm, B.A. Identification and analysis of fitness of resistance mutations against the HCV protease inhibitor SCH 503034. Antiviral Res., 2006, 70(2), 28-38.
29. Lin, C.; Kwong, A.D.; Perni, R.B. 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.
30. Ghany, M.G.; Nelson, D.R.; Strader, D.B.; Thomas, D.L.; Seeff, L.B. 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, 2011, 54(4), 1433-1444.
31. Borgia, G.; Reynaud, L.; Gentile, I.; Borrelli, F.; Cerini, R.; Ciampi, R.; Piazza, M. Pernicious anemia during IFN-alpha treatment for chronic hepatitis C. J. Interferon Cytokine Res., 2003, 23(1), 11-12.
32. Borgia, G.; Reynaud, L.; Gentile, I.; Cerini, R.; Ciampi, R.; Dello Russo, M.; Piazza, M. Myasthenia gravis during low-dose IFNalpha therapy for chronic hepatitis C. J. Interferon Cytokine Res., 2001, 21(7), 469-470.
33. Gentile, I.; Viola, C.; Reynaud, L.; Borrelli, F.; Cerini, R.; Ciampi, R.; Piazza, M.; Borgia, G. Hemolytic anemia during pegylated IFN-alpha2b plus ribavirin treatment for chronic hepatitis C: ribavirin is not always the culprit. J. Interferon Cytokine Res., 2005, 25(5), 283-285.
34. Yoshida, T.; Kondoh, M.; Yagi, K. Promising targets for antihepatitis C virus agents. Curr. Med. Chem., 2011, 18(8), 1239-1244.
35. Carloni, G.; Crema, A.; Valli, M.B.; Ponzetto, A.; Clementi, M. HCV infection by cell-to-cell transmission: choice or necessity? Curr. Mol. Med., 2012, 12(1), 83-95.
36. Gentile, I.; Borgia, F.; Buonomo, A.R.; Castaldo, G.; Borgia, G. A novel promising therapeutic option against hepatitis C virus: an oral nucleotide NS5B polymerase inhibitor sofosbuvir. Curr. Med. Chem., 2013, 20(30), 3733-3742.
37. Stedman, C.A.M. Current prospects for interferon-free treatment of hepatitis C in 2012. Clin. Gastroenterol. Hepatol., 2013, 28(1), 38-45.
38. Yi, G.; Deval, J.; Fan, B.; Cai, H.; Soulard, C.; Ranjith-Kumar, C.T.; Smith, D.B.; Blatt, L.; Beigelman, L.; Kao, C.C. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob. Agents. Chemother., 2012, 56(2), 830-837.
39. Tong, X.; Le Pogam, S.; Li, L.; Haines, K.; Piso, K.; Baronas, V.; Yan, J.M.; So, S.S.; Klumpp, K.; Najera, I. In Vivo Emergence of a Novel Mutant L159F/L320F in the NS5B Polymerase Confers Low-Level Resistance to the HCV Polymerase Inhibitors Mericitabine and Sofosbuvir. J. Infect. Dis., 2013, 11, 11.
40. Fridell, R.A.; Qiu, D.; Valera, L.; Wang, C.; Rose, R.E.; Gao, M. Distinct functions of NS5A in hepatitis C virus RNA replication uncovered by studies with the NS5A inhibitor BMS-790052. J. Virol., 2011, 85(14), 7312-7320.
41. Perni, R.B.; Almquist, S.J.; Byrn, R.A.; Chandorkar, G.; Chaturvedi, P.R.; Courtney, L.F.; Decker, C.J.; Dinehart, K.; Gates, C.A.; Harbeson, S.L.; Heiser, A.; Kalkeri, G.; Kolaczkowski, E.; Lin, K.; Luong, Y.P.; Rao, B.G.; Taylor, W.P.; Thomson, J.A.; Tung, R.D.; Wei, Y.; Kwong, A.D.; Lin, C. Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease. Antimicrob. Agents Chemother., 2006, 50(3), 899-909.
42. Sarrazin, C.; Hezode, C.; Zeuzem, S.; Pawlotsky, J.M. Antiviral strategies in hepatitis C virus infection. J. Hepatol., 2012, 56(1), 60010-60015.
43. Lange, C.M.; Zeuzem, S. Perspectives and challenges of interferonfree therapy for chronic hepatitis C. J. Hepatol., 2013, 58(3), 583-592.
44. O'Boyle, D.R., 2nd; Nower, P.T.; Sun, J.H.; Fridell, R.; Wang, C.; Valera, L.; Gao, M. A 96-well based analysis of replicon elimination with the HCV NS5A replication complex inhibitor daclatasvir. J. Virol. Methods, 2013, 193(1), 68-76.
45. Zhang, H.; Zhou, L.; Amblard, F.; Shi, J.; Bobeck, D.R.; Tao, S.; McBrayer, T.R.; Tharnish, P.M.; Whitaker, T.; Coats, S.J.; Schinazi, R.F. Synthesis and evaluation of novel potent HCV NS5A inhibitors. Bioorg. Med. Chem. Lett., 2012, 22(14), 4864-4868.
46. Suk-Fong Lok, A. HCV NS5A inhibitors in development. Clin. Liver Dis., 2013, 17(1), 111-121.
47. Gao, M.; Nettles, R.E.; Belema, M.; Snyder, L.B.; Nguyen, V.N.; Fridell, R.A.; Serrano-Wu, M.H.; Langley, D.R.; Sun, J.H.; O'Boyle, D.R., 2nd; Lemm, J.A.; Wang, C.; Knipe, J.O.; Chien, C.; Colonno, R.J.; Grasela, D.M.; Meanwell, N.A.; Hamann, L.G. Chemical genetics strategy identifies an HCV NS5A inhibitor with a potent clinical effect. Nature, 2010, 465(7294), 96-100.
48. Lee, C. Daclatasvir: potential role in hepatitis C. Drug Des. Devel. Ther., 2013, 7, 1223-1233.
49. Herbst, D.A.; Reddy, K.R. NS5A inhibitor, daclatasvir, for the treatment of chronic hepatitis C virus infection. Expert Opin. Investig. Drugs, 2013, 22(10), 1337-1346.
50. Simmonds, P. Genetic diversity and evolution of hepatitis C virus - 15 years on. J. Gen. Virol., 2004, 85(Pt 11), 3173-3188.
51. Gentile, I.; Viola, C.; Borgia, F.; Castaldo, G.; Borgia, G. Telaprevir: a promising protease inhibitor for the treatment of hepatitis C virus infection. Curr. Med. Chem., 2009, 16(9), 1115-1121.
52. Parfieniuk, A.; Jaroszewicz, J.; Flisiak, R. Specifically targeted antiviral therapy for hepatitis C virus. World J. Gastroenterol., 2007, 13(43), 5673-5681.
53. Wolk, B.; Sansonno, D.; Krausslich, H.G.; Dammacco, F.; Rice, C.M.; Blum, H.E.; Moradpour, D. Subcellular localization, stability, and trans-cleavage competence of the hepatitis C virus NS3-NS4A complex expressed in tetracycline-regulated cell lines. J. Virol., 2000, 74(5), 2293-2304.
54. Elazar, M.; Cheong, K.H.; Liu, P.; Greenberg, H.B.; Rice, C.M.; Glenn, J.S. Amphipathic helix-dependent localization of NS5A mediates hepatitis C virus RNA replication. J. Virol., 2003, 77(10), 6055-6061.
55. Tellinghuisen, T.L.; Marcotrigiano, J.; Rice, C.M. Structure of the zinc-binding domain of an essential component of the hepatitis C virus replicase. Nature, 2005, 435(7040), 374-379.
56. Lohmann, V.; Hoffmann, S.; Herian, U.; Penin, F.; Bartenschlager, R. Viral and cellular determinants of hepatitis C virus RNA replication in cell culture. J. Virol., 2003, 77(5), 3007-3019.
57. Appel, N.; Zayas, M.; Miller, S.; Krijnse-Locker, J.; Schaller, T.; Friebe, P.; Kallis, S.; Engel, U.; Bartenschlager, R. Essential role of domain III of nonstructural protein 5A for hepatitis C virus infectious particle assembly. PLoS Pathog., 2008, 4(3), 1000035.
58. Tripathi, L.P.; Kambara, H.; Chen, Y.A.; Nishimura, Y.; Moriishi, K.; Okamoto, T.; Morita, E.; Abe, T.; Mori, Y.; Matsuura, Y.; Mizuguchi, K. Understanding the Biological Context of NS5A Host Interactions in HCV Infection: A Network-Based Approach. J. Proteome Res., 2013, 12(6), 2537-2551.
59. Martell, M.; Esteban, J.I.; Quer, J.; Genesca, J.; Weiner, A.; Esteban, R.; Guardia, J.; Gomez, J. Hepatitis C virus (HCV) circulates as a population of different but closely related genomes: quasispecies nature of HCV genome distribution. J. Virol., 1992, 66(5), 3225-3229.
60. Pawlotsky, J.M. Hepatitis C virus population dynamics during infection. Curr. Top. Microbiol. Immunol., 2006, 299, 261-284.
61. Fridell, R.A.; Wang, C.; Sun, J.H.; O'Boyle, D.R., 2nd; Nower, P.; Valera, L.; Qiu, D.; Roberts, S.; Huang, X.; Kienzle, B.; Bifano, M.; Nettles, R.E.; Gao, M. Genotypic and phenotypic analysis of variants resistant to hepatitis C virus nonstructural protein 5A replication complex inhibitor BMS-790052 in humans: in vitro and in vivo correlations. Hepatology, 2011, 54(6), 1924-1935.
62. Tellinghuisen, T.L.; Foss, K.L.; Treadaway, J.C.; Rice, C.M. Identification of residues required for RNA replication in domains II and III of the hepatitis C virus NS5A protein. J. Virol., 2008, 82(3), 1073-1083.
63. Guedj, J.; Dahari, H.; Rong, L.; Sansone, N.D.; Nettles, R.E.; Cotler, S.J.; Layden, T.J.; Uprichard, S.L.; Perelson, A.S. Modeling shows that the NS5A inhibitor daclatasvir has two modes of action and yields a shorter estimate of the hepatitis C virus half-life. Proc. Natl. Acad. Sci. U S A, 2013, 110(10), 3991-3996.
64. Guedj, J.; Dahari, H.; Uprichard, S.L.; Perelson, A.S. The hepatitis C virus NS5A inhibitor daclatasvir has a dual mode of action and leads to a new virus half-life estimate. Expert Rev. Gastroenterol. Hepatol., 2013, 7(5), 397-399.
65. Wang, C.; Valera, L.; Jia, L.; Kirk, M.J.; Gao, M.; Fridell, R.A. In vitro activity of daclatasvir on hepatitis C virus genotype 3 NS5A. Antimicrob. Agents Chemother., 2013, 57(1), 611-613.
66. Wang, C.; Jia, L.; Huang, H.; Qiu, D.; Valera, L.; Huang, X.; Sun, J.H.; Nower, P.T.; O'Boyle, D.R., 2nd; Gao, M.; Fridell, R.A. In vitro activity of BMS-790052 on hepatitis C virus genotype 4 NS5A. Antimicrob. Agents Chemother., 2012, 56(3), 1588-1590.
67. Lemm, J.A.; O'Boyle, D., 2nd; Liu, M.; Nower, P.T.; Colonno, R.; Deshpande, M.S.; Snyder, L.B.; Martin, S.W.; St Laurent, D.R.; Serrano-Wu, M.H.; Romine, J.L.; Meanwell, N.A.; Gao, M. Identification of hepatitis C virus NS5A inhibitors. J. Virol., 2010, 84(1), 482-491.
68. Nettles, R.E.; Gao, M.; Bifano, M.; Chung, E.; Persson, A.; Marbury, T.C.; Goldwater, R.; DeMicco, M.P.; Rodriguez-Torres, M.; Vutikullird, A.; Fuentes, E.; Lawitz, E.; Lopez-Talavera, J.C.; Grasela, D.M. Multiple ascending dose study of BMS-790052, a nonstructural protein 5A replication complex inhibitor, in patients infected with hepatitis C virus genotype 1. Hepatology, 2011, 54(6), 1956-1965.
69. Kiser, J.J.; Burton, J.R., Jr.; Everson, G.T. Drug-drug interactions during antiviral therapy for chronic hepatitis C. Nat. Rev. Gastroenterol. Hepatol., 2013, 10(10), 596-606.
70. Bifano, M.; Sevinsky, H.; Persson, A.; Chung, E.; Wind-Rotolo, M.; Hwang, C.; Nettles, R.; Grasela, D.M.; Marbury, T.C.; DeMicco, M.P.; Bertz, R.J. Single-dose pharmacokinetics of bms-790052 in subjects with hepatic impairment compared with healthy subjects. Hepatology, 2011, 54, 1004A-1004A.
71. Bifano, M.; Sevinsky, H.; Persson, A.; Hwang, C.; Kandoussi, H.; Jiang, H.; Grasela, D.M.; Bertz, R.J. BMS-790052 has no effect on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and norgestimate in healthy female subjects. Hepatology, 2011, 54, 991A-992A.
72. Bifano, M.; Sevinsky, H.; Bedford, B.R.; Coumbis, J.J.; Huang, S.- P.; Grasela, D.M.; Eley, T.; Bertz, R.J.; Medlock, M. Coadministration of BMS-790052 and BMS-650032 does not result in a clinically meaningful pharmacokinetic interaction in healthy subjects. Hepatology, 2010, 52(4), 719A-719A.
73. Pasquinelli, C.; McPhee, F.; Eley, T.; Villegas, C.; Sandy, K.; Sheridan, P.; Persson, A.; Huang, S.P.; Hernandez, D.; Sheaffer, A.K.; Scola, P.; Marbury, T.; Lawitz, E.; Goldwater, R.; Rodriguez-Torres, M.; Demicco, M.; Wright, D.; Charlton, M.; Kraft, W.K.; Lopez-Talavera, J.C.; Grasela, D.M. Single- and multiple-ascending-dose studies of the NS3 protease inhibitor asunaprevir in subjects with or without chronic hepatitis C. Antimicrob. Agents Chemother., 2012, 56(4), 1838-1844.
74. McPhee, F.; Friborg, J.; Levine, S.; Chen, C.; Falk, P.; Yu, F.; Hernandez, D.; Lee, M.S.; Chaniewski, S.; Sheaffer, A.K.; Pasquinelli, C. Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir. Antimicrob. Agents Chemother., 2012, 56(7), 3670-3681.
75. Chayama, K.; Takahashi, S.; Toyota, J.; Karino, Y.; Ikeda, K.; Ishikawa, H.; Watanabe, H.; McPhee, F.; Hughes, E.; Kumada, H. 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), 742-748.
76. Pol, S.; Ghalib, R.H.; Rustgi, V.K.; Martorell, C.; Everson, G.T.; Tatum, H.A.; Hezode, C.; Lim, J.K.; Bronowicki, J.P.; Abrams, G.A.; Brau, N.; Morris, D.W.; Thuluvath, P.J.; Reindollar, R.W.; Yin, P.D.; Diva, U.; Hindes, R.; McPhee, F.; Hernandez, D.; Wind-Rotolo, M.; Hughes, E.A.; Schnittman, S. Daclatasvir for previously untreated chronic hepatitis C genotype-1 infection: a randomised, parallel-group, double-blind, placebo-controlled, dosefinding, phase 2a trial. Lancet Infect. Dis., 2012, 12(9), 671-677.
77. Lok, A.S.; Gardiner, D.F.; Lawitz, E.; Martorell, C.; Everson, G.T.; Ghalib, R.; Reindollar, R.; Rustgi, V.; McPhee, F.; Wind-Rotolo, M.; Persson, A.; Zhu, K.; Dimitrova, D.I.; Eley, T.; Guo, T.; Grasela, D.M.; Pasquinelli, C. Preliminary study of two antiviral agents for hepatitis C genotype 1. N. Engl. J. Med., 2012, 366(3), 216-224.
78. Coppola, N.; Marrone, A.; Pisaturo, M.; Starace, M.; Signoriello, G.; Gentile, I.; Adinolfi, L.E.; Sagnelli, E.; Zampino, R. Role of interleukin 28-B in the spontaneous and treatment-related clearance of HCV infection in patients with chronic HBV/HCV dual infection. Eur. J. Clin. Microbiol. Infect. Dis., [Online early access] DOI: 10.1007/s10096-013-1985-7. Published Online: October 1, 2013. PMID: 24081499.
79. Lok, A.; Gardiner, D.; Hezode, C.; Lawitz, E.; Bourliere, M.; Everson, G.; Marcellin, P.; Rodriguez-Torres, M.; Pol, S.; Serfaty, L.; Eley, T.; Huang, S.P.; Wind-Rotolo, M.; McPhee, F.; Grasela, D.; Pasquinelli, C. Confirmation that quadruple therapy with daclatasvir (ns5a inhibitor), asunaprevir (ns3 inhibitor) and peginterferon/ribavirin results in high rate of svr4 in hcv genotype 1 null responders. J. Hepatol., 2012, 56, S557-S557.
80. Hezode, C.; Hirschfield, G.M.; Ghesquiere, W.; Sievert, W.; Rodriguez-Torres, M.; Shafran, S.D.; Thuluvath, P.J.; Tatum, H.A.; Waked, I.; Esmat, G.E.; Lawitz, E.; Rustgi, V.K.; Pol, S.; Weis, N.; Pockros, P.; Bourliere, M.; Serfaty, L.; Vierling, J.M.; Fried, M.W.; Weiland, O.; Brunetto, M.R.; Everson, G.T.; Zeuzem, S.; Kwo, P.Y.; Sulkowski, M.S.; Brau, N.; Wind-Rotolo, M.; Liu, Z.; Hughes, E.A.; Schnittman, S.M.; Yin, P.D. Daclatasvir, an NS5A Replication Complex Inhibitor, Combined With Peginterferon Alfa-2a and Ribavirin in Treatment-Naive HCV-Genotype 1 or 4 Subjects: Phase 2b COMMAND-1 SVR12 Results. Hepatology, 2012, 56, 553A-554A.
81. Dore, G.J.; Lawitz, E.; Hezode, C.; Shafran, S.; Ramji, A.; Tatum, H.; Taliani, G.; Tran, A.; Brunetto, M.; Zaltron, S.; Strasser, S.; Weis, N.; Ghesquiere, W.; Lee, S.; Larrey, D.; Pol, S.; Harley, H.; George, J.; Fung, S.; de Ledinghen, V.; Hagens, P.; Cohen, D.; Cooney, E.; Noviello, S.; Hughes, E. Daclatasvir combined with peginterferon alfa-2a and ribavirin for 12 or 16 weeks in patients with hcv genotype 2 or 3 infection: command gt2/3 study. J. Hepatol., 2013, 58, S570-S571.
82. Ratziu, V.; Gadano, A.; Pol, S.; Hezode, C.; Ramji, A.; Cheng, W.; Sulkowsk, M.; Everson, G.; Diva, U.; McPhee, F.; Wind-Rotolo, M.; Hughes, E.A.; Yin, P.D.; Schnittman, S.; Investigators, C. Triple therapy with daclatasvir (DCV; BMS-790052), peginterferon alfa-2a and ribavirin in hcv-infected prior null and partial responders: 12-week results of phase 2b command-2 trial. J. Hepatol., 2012, 56, S478-S479.
83. Izumi, N.; Asahina, Y.; Yokosuka, O.; Imazeki, F.; Kawada, N.; Tamori, A.; Osaki, Y.; Kimura, T.; Yamamoto, K.; Takaki, A.; Sata, M.; Ide, T.; Ishikawa, H.; Ueki, T.; Yang, R.; McPhee, F.; Hughes, E.A. combination therapy of treatment-naive and nonresponder patients with hcv genotype 1 infection with BMS- 790052, an ns5a replication complex inhibitor, in combination with peginterferon alfa-2a and ribavirin. Hepatology, 2011, 54, 1439A-1440A.
84. Izumi, N.; LaTaillade, M.; Chayama, K.; Toyota, J.; Mochida, S.; Kawada, N.; Ishikawa, H.; Hosokawa, E.; Imai, J.; Scricca, R.; Cohen, D.S.; Xu, D.; Horga, A.; Srinivasan, S.; Kumada, H.; Lopez-Talavera, J.C. First Report of Peginterferon Lambda/Ribavirin in Combination With Either Daclatasvir or Asunaprevir in HCV Genotype 1 Japanese Subjects: Early Sustained Virologic Response (SVR4) Results From the D-LITE Japanese Sub-Study. Hepatology, 2012, 56, 310A-310A.
85. Sofia, M.J.; Bao, D.; Chang, W.; Du, J.; Nagarathnam, D.; Rachakonda, S.; Reddy, P.G.; Ross, B.S.; Wang, P.; Zhang, H.R.; Bansal, S.; Espiritu, C.; Keilman, M.; Lam, A.M.; Steuer, H.M.; Niu, C.; Otto, M.J.; Furman, P.A. Discovery of a beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-C-methyluridine nucleotide prodrug (PSI-7977) for the treatment of hepatitis C virus. J. Med. Chem., 2010, 53(19), 7202-7218.
86. Sulkowski, M.S.; Gardiner, D.F.; Rodriguez-Torres, M.; Reddy, K.R.; Hassanein, T.; Jacobson, I.M.; Lawitz, E.; Lok, A.S.; Hinestrosa, F.; Thuluvath, P.J.; Schwartz, H.; Nelson, D.R.; Eley, T.; Wind-Rotolo, M.; Huang, S.-P.; Gao, M.; McPhee, F.; Sherman, D.; Hindes, R.; Symonds, W.T.; Pasquinelli, C.; Grasela, D.M. High Rate of Sustained Virologic Response with the All-Oral Combination of Daclatasvir (NS5A Inhibitor) Plus Sofosbuvir (Nucleotide NS5B Inhibitor), With or Without Ribavirin, in Treatment-Naive Patients Chronically Infected With HCV Genotype 1, 2, or 3. Hepatology, 2012, 56(6), 1516-1517.
87. Everson, G.T.; Sims, K.D.; Rodriguez-Torres, M.; Hezode, C.; Lawitz, E.; Bourliere, M.; Loustaud-Ratti, V.; Rustgi, V.; Schwartz, H.; Tatum, H.; Marcellin, P.; Pol, S.; Thuluvath, P.J.; Eley, T.; Wang, X.; Huang, S.P.; McPhee, F.; Wind-Rotolo, M.; Chung, E.; Pasquinelli, C.; Grasela, D.M.; Gardiner, D.F. Interim analysis of an interferon (IFN)- and ribavirin (RBV)-free regimen of daclatasvir (DCV), asunaprevir (ASV), and BMS-791325 in treatment-naive, hepatitis c virus genotype 1-infected patients. J. Hepatol., 2013, 58, S573-S573.
88. Suzuki, Y.; Ikeda, K.; Suzuki, F.; Toyota, J.; Karino, Y.; Chayama, K.; Kawakami, Y.; Ishikawa, H.; Watanabe, H.; Hu, W.; Eley, T.; McPhee, F.; Hughes, E.; Kumada, H. Dual oral therapy with daclatasvir and asunaprevir for patients with HCV genotype 1b infection and limited treatment options. J. Hepatol., 2013, 58(4), 655-662.
89. Sulkowski, M.S.; Gardiner, D.F.; Rodriguez-Torres, M.; Reddy, K.R.; Hassanein, T.; Jacobson, I.; Lawitz, E.; Lok, A.S.; Hinestrosa, F.; Thuluvath, P.J.; Schwartz, H.; Nelson, D.R.; Everson, G.T.; Eley, T.; Wind-Rotolo, M.; Huang, S.P.; Gao, M.; McPhee, F.; Hernandez, D.; Sherman, D.; Hindes, R.; Symonds, W.; Pasquinelli, C.; Grasela, D.M.; Grp, A.I.S. Sustained virologic response with daclatasvir plus sofosbuvir +/- ribavirin (RBV) in chronic HCV genotype (GT) 1-infected patients who previously failed telaprevir (TVR) or boceprevir (BOC). J. Gastroenterol. Hepatol., 2013, 28, 155-155.
90. Fontana, R.J.; Hughes, E.A.; Bifano, M.; Appelman, H.; Dimitrova, D.; Hindes, R.; Symonds, W.T. Sofosbuvir and daclatasvir combination therapy in a liver transplant recipient with severe recurrent cholestatic hepatitis C. Am. J. Transplant., 2013, 13(6), 1601-1605.
91. McPhee, F.; Hernandez, D.; Yu, F.; Ueland, J.; Chayama, K.; Toyota, J.; Izumi, N.; Yokosuka, O.; Kawada, N.; Osaki, Y.; Hughes, E.; Watanabe, H.; Ishikawa, H.; Kumada, H. A description of virologic escape in hcv genotype 1-infected patients treated with daclatasvir (BMS-790052) in combination with ribavirin and peginterferon alfa-2a or peginterferon alfa-2b. J. Hepatol., 2012, 56, S473-S473.
92. Galmozzi, E.; Aghemo, A.; Colombo, M. Low rates of naturally occurring resistant variants to the NS5A inhibitor daclatasvir in HCV-1 null responders. Hepatology, 2013, 57(5), 2087.
93. Wang, C.; Sun, J.H.; O'Boyle, D.R., 2nd; Nower, P.; Valera, L.; Roberts, S.; Fridell, R.A.; Gao, M. Persistence of resistant variants in hepatitis C virus-infected patients treated with the NS5A replication complex inhibitor daclatasvir. Antimicrob. Agents Chemother., 2013, 57(5), 2054-2065.
94. Karino, Y.; Toyota, J.; Ikeda, K.; Suzuki, F.; Chayama, K.; Kawakami, Y.; Ishikawa, H.; Watanabe, H.; Hernandez, D.; Yu, F.; McPhee, F.; Kumada, H. Characterization of virologic escape in hepatitis C virus genotype 1b patients treated with the direct-acting antivirals daclatasvir and asunaprevir. J. Hepatol., 2013, 58(4), 646-654.
95. Aghemo, A.; Colombo, M. Selection of resistant-associated variants to the NS5A inhibitor daclatasvir: revenge of the hepatitis C virus. Gastroenterology, 2013, 145(1), 247-249.
96. McPhee, F.; Hernandez, D.; Yu, F.; Ueland, J.; Monikowski, A.; Carifa, A.; Falk, P.; Wang, C.; Fridell, R.; Eley, T.; Zhou, N.; Gardiner, D. Resistance analysis of hepatitis C virus genotype 1 prior treatment null responders receiving daclatasvir and asunaprevir. Hepatology, 2013, 58(3), 902-911.
97. McPhee, F.; Hernandez, D.; Zhou, N.; Ueland, J.; Monikowski, A.; Tanveen, T.; Wind-Rotolo, M.; Hughes, E.A.; Cooney, E.L. Characterization of HCV NS5A Resistance Variants in Naive Patients Infected with Genotypes 2 and 3 Receiving Short-Term Treatment of Daclatasvir in Combination with Pegylated Interferon-Alfa and Ribavirin. Hepatology, 2012, 56, 579A-580A.
98. Claxton, A.J.; Cramer, J.; Pierce, C. A systematic review of the associations between dose regimens and medication compliance. Clin. Ther., 2001, 23(8), 1296-1310.
99. Pelosi, L.A.; Voss, S.; Liu, M.; Gao, M.; Lemm, J.A. Effect on hepatitis C virus replication of combinations of direct-acting antivirals, including NS5A inhibitor daclatasvir. Antimicrob. Agents Chemother., 2012, 56(10), 5230-5239.
100. Friborg, J.; Levine, S.; Chen, C.; Sheaffer, A.K.; Chaniewski, S.; Voss, S.; Lemm, J.A.; McPhee, F. Combinations of lambda interferon with direct-acting antiviral agents are highly efficient in suppressing hepatitis C virus replication. Antimicrob. Agents Chemother., 2013, 57(3), 1312-1322.
101. Alisi, A.; Della Corte, C.; Comparcola, D.; Sartorelli, M.R.; Nobili, V. Daclatasvir: a promising triple therapy for children with chronic hepatitis C. Lancet Infect. Dis., 2013, 13(1), 17-18.