Antiviral treatment of chronic hepatitis B virus (HBV) infections

Viruses

Volumn 2, Issue 6, 2010, Pages 1279-1305

  de Clercq, Erik ^a   Férir, Geoffrey ^a   Kaptein, Suzanne ^a   Neyts, Johan ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

Antiviral therapy; HBV therapy; Nucleoside analogs; Viral hepatitis

Indexed keywords

ADEFOVIR DIPIVOXIL; ALPHA INTERFERON; ALPHA2B INTERFERON; ANTIVIRUS AGENT; CLEVUDINE; EMTRICITABINE; ENTECAVIR; HEPATITIS B CORE ANTIGEN; HEPATITIS B SURFACE ANTIGEN; HEPATITIS B(E) ANTIGEN; LAMIVUDINE; PEGINTERFERON ALPHA; PEGINTERFERON ALPHA2A; PEGINTERFERON ALPHA2B; PLACEBO; RECOMBINANT ALPHA2B INTERFERON; RIBAVIRIN; TELBIVUDINE; TENOFOVIR DISOPROXIL;

ANTIVIRAL ACTIVITY; ANTIVIRAL RESISTANCE; ANTIVIRAL SUSCEPTIBILITY; ANTIVIRAL THERAPY; COMBINATION CHEMOTHERAPY; DRUG ABSORPTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG MEGADOSE; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG STRUCTURE; DRUG TARGETING; DRUG TOLERABILITY; DRUG WITHDRAWAL; FLU LIKE SYNDROME; GENE MUTATION; HEPATITIS B; HEPATITIS B VIRUS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LACTIC ACIDOSIS; LIVER TOXICITY; MITOCHONDRIAL TOXICITY; MIXED INFECTION; MONOTHERAPY; MYOPATHY; NEPHROTOXICITY; NONHUMAN; REVIEW; SEROCONVERSION; VIRUS PARTICLE; VIRUS REPLICATION;

HEPATITIS B VIRUS;

EID: 79952094473     PISSN: None     EISSN: 19994915     Source Type: Journal    
DOI: 10.3390/v2061279     Document Type: Review

References (164)

1. Ganem, D; Prince, A.M. Hepatitis B virus infection - Natural history and clinical consequences. N. Engl. J. Med. 2004, 350, 1118-1129.
2. Beasley, R.P. Hepatitis B virus: the major etiology of hepatocellular carcinoma. Cancer 1988, 61, 1942-1956.
3. Chiaramonte, M.; Stroffolini, T.; Vian, A.; Stazi, M.A.; Floreani, A.; Lorenzoni, U.; Lobello, S.; Farinati, F.; Naccarato, R. Rate of incidence of hepatocellular carcinoma in patients with compensated viral cirrhosis. Cancer 1999, 85, 2132-2137.
4. Fattovich, G.; Pantalena, M.; Zagni, I.; Realdi, G.; Schalm, S.W.; Christensen, E. Effect of hepatitis B and C virus infections on the natural history of compensated cirrhosis: a cohort study of 297 patients. Am. J. Gastroenterol. 2002, 97, 2886-2895.
5. Yang, H.I.; Lu, S.N.; Liaw, Y.F.; You, S.L.; Sun, C.A.; Wang, L.Y.; Hsiao, C.K.; Chen, P.J.; Chen, D.S.; Chen, C.J. Hepatitis B e antigen and the risk of hepatocellular carcinoma. N. Engl. J. Med. 2002, 347, 168-174.
6. Zoulim, F. Antiviral therapy of chronic hepatitis B. Antiviral Res. 2006, 71, 206-215.
7. Keeffe, E.B.; Marcellin, P. New and emerging treatment of chronic hepatitis B. Clin. Gastroenterol. Hepatol. 2007, 5, 285-294.
8. Palumbo, E. New drugs for chronic hepatitis B: a review. Am. J. Therapeut. 2008, 15, 167-172.
9. Peng, J.; Zhao, Y.; Mai, J.; Pang, W.K.; Wei, X.; Zhang, P.; Xu, Y. Inhibition of hepatitis B virus replication by various RNAi constructs and their pharmacodynamic properties. J. Gen. Virol. 2005, 86, 3227-3234.
10. Ying, C.; De Clercq, E.; Neyts, J. Selective inhibition of hepatitis B virus replication by RNA interference. Biochem. Biophys. Res. Commun. 2003, 309, 482-484.
11. Chen, Y.; Cheng, G., Mahato, R.I. RNAi for treating hepatitis B viral infection. Pharm. Res. 2008, 25, 72-86.
12. McCaffrey, A.P.; Nakai, H.; Pandey, K.; Huang, Z.; Salazar, F.H.; Xu, H.; Wieland, S.F.; Marion, P.I.; Kay, M.A. Inhibition of hepatitis B virus in mice by RNA interference. Nat. Biotechnol. 2003, 21, 639-644.
13. Cheng, Y.C.; Ying, C.X.; Leung, C.H.; Li, Y. New targets and inhibitors of HBV replication to combat drug resistance. J. Clin. Virol. 2005, 34 Suppl. 1, S147-S150.
14. Ying, C.; Li, Y.; Leung, C.H.; Robek, M.D. Cheng, Y.C. Unique antiviral mechanism discovered in anti-hepatitis B virus research with a natural product analogue. Proc. Natl. Acad. Sci. USA 2007, 104, 8526-8531.
15. Deres, K.; Schröder, C.H.; Paessens, A.; Goldmann, S.; Hacker, H.J.; Weber, O.; Krämer, T.; Niewöhner, U.; Pleiss, U.; Stoltefuss, J.; Graef, E.; Koletzki, D.; Masantschek, R.N.; Reimann, A.; Jaeger, R.; Gross, R.; Beckermann, B.; Schlemmer, K.H.; Haebich, D.; Rübsamen-Waigmann, H. Inhibition of hepatitis B virus replication by drug-induced depletion of nucleocapsids. Science 2003, 299, 893-896.
16. Block, T.M.; Lu, X.; Mehta, A.S.; Blumberg, B.S.; Tennant, B.; Ebling, M.; Korba, B.; Lansky, D.M.; Jacob, G.S., Dwek, R.A. Treatment of chronic hepadnavirus infection in a woodchuck animal model with an inhibitor of protein folding and trafficking. Nat. Med. 1998, 4, 610-614.
17. Korba, B.E.; Montero, A.B.; Farrar, K.; Gaye, K.; Mukerjee, S.; Ayers, M.S.; Rossignol, J.F. Nitazoxanide, tizoxanide and other thiazolides are potent inhibitors of hepatitis B virus and hepatitis C virus replication. Antiviral Res. 2008, 77, 56-63.
18. Dougherty, A.M.; Guo, H.; Westby, G.; Liu, Y.; Simsek, E.; Guo, J.T.; Mehta, A.; Norton, P.; Gu, B.; Block, T.; Cuconati, A. A substituted tetrahydro-tetrazolo-pyrimidine is a specific and novel inhibitor of hepatitis B virus surface antigen secretion. Antimicrob. Agents Chemother. 2007, 51, 4427-4437.
19. He, X.X.; Chen, T.; Lin, J.S.; Chang, Y.; Ye, B.X. Inhibition of the replication of hepatitis B virus in vitro by a novel 2,6-diaminopurine analog, beta-LPA. Biochem. Biophys. Res. Commun. 2008, 369, 513-518.
20. Kim, H.J.; Sharon, A.; Bal, C.; Wang, J.; Allu, M.; Huang, Z.; Murray, M.G.; Bassit, L.; Schinazi, R.F.; Korba, B.; Chu, C.K. Synthesis and anti-hepatitis B virus and anti-hepatitis C virus activities of 7-deazaneplanocin A analogues in vitro. J. Med. Chem. 2009, 52, 206-218.
21. Li, X.; Kuang, E.; Dai, W.; Zhou, B.; Yang, F. Efficient inhibition of hepatitis B virus replication by hammerhead ribozymes delivered by hepatitis delta virus. Virus. Res. 2005, 114, 126-132.
22. Dane, D.S.; Cameron, C.H.; Briggs, M. Virus-like particles in serum of patients with Australia-antigen-associated hepatitis. Lancet 1970, 1, 695-698.
23. Robinson, W.S.; Lutwick, L.I. The virus of hepatitis, type B (first of two parts). N. Engl. J. Med. 1976, 295, 1168-1175.
24. Gavilanes, F.; Gonzalez-Ros, J.M.; Peterson, D.L. Structure of hepatitis B surface antigen: Characterization of the lipid components and their association with the viral proteins. J. Biol. Chem. 1982, 257, 7770-7777.
25. Peterson, D.L. Isolation and characterization of the major protein and glycoprotein of hepatitis B surface antigen. J. Biol. Chem. 1981, 256, 6975-6983.
26. Peterson, D.L. The structure of hepatitis B surface antigen and its antigenic sites. Bioessays 1987, 6, 258-262.
27. Valenzuela, P.; Gray, P.; Quiroga, M.; Zaldivar, J.; Goodman, H.M.; Rutter, W.J. Nucleotide sequence of the gene coding for the major protein of hepatitis B virus surface antigen. Nature 1979, 280, 815-819.
28. Bartenschlager, R.; Schaller, H. The amino-terminal domain of the hepadnaviral P-gene encodes the terminal protein (genome linked protein) believed to prime reverse transcription. EMBO J. 1988, 7, 4185-4192.
29. Chang, L.J.; Hirsch, R.C.; Ganem, D.; Varmus, H.E. Effects of insertional and point mutations on the functions of the duck hepatitis B virus polymerase. J. Virol. 1990, 11, 5553-5558.
30. Radziwill, G.; Tucker, W.; Schaller, H. Mutational analysis of the hepatitis B virus P gene product: domain structure and RNase H activity. J. Virol. 1990, 2, 613-620.
31. Poch, O.; Sauvaget, I.; Delarue, M.; Tordo, N. Identification of four conserved motifs among the RNA-dependent polymerase encoding elements. EMBO J. 1989, 8, 3867-3874.
32. Tipples, G.A.; Ma, M.M.; Fischer, K.P.; Bain, V.G.; Kneteman, N.M.; Tyrrell, D.L.J. Mutation in HBV RNA-dependent DNA polymerase confers resistant to lamivudine in vivo. Hepatology 1996, 24, 714-717.
33. Ou, J.H.; Laub, O.; Rutter, W.J. Hepatitis B virus gene function: the pre-core region targets the core antigen to cellular membranes and causes the secretion of the e entigen. Proc. Natl. Acad. Sci. USA 1986, 83, 1578-1582.
34. Pasek, M.; Goto, T.; Gilbert, W.; Zink, B.; Schaller, H.; MacKay, P.; Leadbetter, G.; Murray, K. Hepatitis B virus genes and their expression in E. coli. Nature 1979, 282, 575-579.
35. Tuttleman, J.S.; Pourcel, C.; Summers, J. Formation of the pool of covalently closed circular viral DNA in hepadnavirus-infected cells. Cell 1986, 47, 451-460.
36. Will, H.; Reiser, W.; Weimer, T.; Pfaff, E.; Büscher, M.; Sprengel, R.; Cattaneo, R.; Schaller, H. Replication strategy of human hepatitis B virus. J. Virol. 1987, 61, 904-911.
37. Wong, D.K.; Yuen, M.F.; Poon, R.T.; Yuen, J.C.; Fung, J.; Lai, C.L. Quantification of hepatitis B virus covalently closed circular DNA in patients with hepatocellular carcinoma. J. Hepatol. 2006, 45, 553-559.
38. Pollack, J.R.; Ganem, D. Site-specific RNA binding by a hepatitis B virus reverse transcriptase initiates two distinct reactions: RNA packaging and DNA synthesis. J. Virol. 1994, 68, 5579-5587.
39. Hu, J.; Seeger, C. Hsp90 is required for the activity of a hepatitis B virus reverse transcriptase. Proc. Natl. Acad. Sci. USA 1996, 93, 1060-1064.
40. Seeger, C.; Mason, W.S. Hepatitis B virus biology. Microbiol. Mol. Biol. Rev. 2000, 64, 51-68.
41. Staprans, S.; Loeb, D.D.; Ganem, D. Mutations affecting hepadnavirus plus-strand DNA synthesis dissociate primer cleavage from translocation and reveal the origin of linear viral DNA. J. Virol. 1991, 65, 1255-1262.
42. Yang, W.; Mason, W.S.; Summers, J. Covalently closed circular viral DNA formed from two types of linear DNA in woodchuck hepatitis virus-infected liver. J. Virol. 1996, 70, 4567-4575.
43. Yang, W.; Summers, J. Illegitimate replication of linear hepadnavirus DNA through nonhomologous recombination. J. Virol. 1995, 69, 4029-4036.
44. Yang, W.; Summers J. Integration of hepadnavirus DNA in infected liver: evidence for a linear precursor. J. Virol. 1999, 73, 9710-9717.
45. Gong, S.S.; Jensen, A.D.; Chang, C.J.; Rogler, C.E. Double-stranded linear duck hepatitis B virus (DHBV) stably integrates at a higher frequency than wild-type DHBV in LMH chicken hepatoma cells. J. Virol. 1999, 73, 1492-1502.
46. Gong, S.S.; Jensen, A.D.; Wang, H.; Rogler, C.E. Duck hepatitis B virus integrations in LMH chicken hepatoma cells: identification and characterization of new episomally derived integrations. J. Virol. 1995, 69, 8102-8108.
47. Kamimura, T.; Yoshikawa, A.; Ichida, F.; Sasaki, H. Electron microscopic studies of Dane particles in hepatocytes with special reference to intracellular development of Dane particles and their relation with HBeAg in serum. Hepatology 1981, 1, 392-397.
48. Roingeard, P.; Lu, S.L.; Sureau, C.; Freschlin, M.; Arbeille, B.; Essex, M.; Romet-Lemonne, J.L. Immunocytochemical and electron microscopic study of hepatitis B virus antigen and complete particle production in hepatitis B virus DNA transfected HepG2 cells. Hepatology 1990, 11, 277-285.
49. Ganem, D.; Schneider, R.J. Hepadnaviridae: The viruses and their replication. In Fields Virology, 4th edition. Lippincott Williams & Wilkins: Philadelphia, PA, USA, 2001; pp. 2923-2969.
50. Cammack, N.; Rouse, P.; Marr, C.L.; Reid, P.J.; Boehme, R.E.; Coates, J.A.; Penn, C.R.; Cameron, J.M. Cellular metabolism of (-) enantiomeric 2'-deoxy-3'-thiacytidine. Biochem. Pharmacol. 1992, 43, 2059-2064.
51. Chang, C.N.; Skalski, V.; Zhou, J.H.; Cheng, Y.C. Biochemical pharmacology of (+)- and (-)-2',3'-dideoxy-3'-thiacytidine as anti-hepatitis B virus agents. J. Biol. Chem. 1992, 267, 22414-22420.
52. Lai, C.L.; Yuen, M.F. Profound suppression of hepatitis B virus replication with lamivudine. J. Med. Virol. 2000, 61, 367-373.
53. Dienstag, J.L.; Schiff, E.R.; Wright, T.L.; Perrillo, R.P.; Hann, H.W.; Goodman, Z.; Crowther, L.; Condreay, L.D.; Woessner, M.; Rubin, M.; Brown, N.A. Lamivudine as initial treatment for chronic hepatitis B in the United States. N. Engl. J. Med. 1999, 341, 1256-1263.
54. Lai, C.L.; Chine, R.W.; Leung, N.W.Y.; Chang, T.T.; Guan, R.; Tai, D.I.; Ng, K.Y.; Wu, P.C.; Dent, J.C.; Barber, J.; Stephenson, S.L.; Gray, F. A one year trial of lamivudine for chronic hepatitis B. N. Engl. J. Med. 1998, 339, 61-68.
55. Yuen, M.F.; Fong, D.Y.; Wong, D.K.; Yuen, J.C.; Fung, J.; Lai, C.L. Hepatitis B virus DNA levels at week 4 of lamivudine treatment predict the 5-year ideal response. Hepatology 2007, 46, 1695-1703.
56. Fung, S.K.; Wong, F.; Hussain, M.; Lok, A.S.F. Sustained response after a 2-year course of lamivudine treatment of hepatitis B e antigen-negative chronic hepatitis B. J. Viral. Hepatol. 2004, 11, 432-438.
57. Perry, C.M.; Faulds, D. Lamivudine. A review of its antiviral activity, pharmacokinetic properties and therapeutic efficacy in the management of HIV infection. Drugs 1997, 53, 657-680.
58. Schalm, S.W.; Heathcote, J.; Cianciara, J.; Farrell, G.; Sherman, M.; Willems, B.; Dhillon, A.; Moorat, A.; Barber, J.; Gray, D.F. Lamivudine and alpha interferon combination treatment of patients with chronic hepatitis B infection: a randomised trial. Gut 2000, 46, 562-568.
59. Yuen, M.F.; Seto, W.K.; Chow, D.H.; Tsui, K.; Wong, D.K.; Ngai, V.W.; Wong, B.C.; Fung, J.; Yuen, J.C.; Lai, C.L. Long-term lamivudine therapy reduces the risk of long-term complications of chronic hepatitis B infection even in patients without advanced disease. Antiviral Ther. 2007, 12, 1295-1303.
60. Lok, A.S.; Lai, C.L.; Leung, N.; Yao, G.B.; Cui, Z.Y.; Schiff, E.R.; Dienstag, J.L.; Heathcote, E.J.; Little, N.R.; Griffiths, D.A.; Gardner, S.D.; Castiglia, M. Long-term safety of lamivudine treatment in patients with chronic hepatitis B. Gastroenterology 2003, 125, 1714-1722.
61. Pawlotsky, J.M.; Dusheiko, G.; Hatzakis, A.; Lau, D.; Lau, G.; Liang, T.J.; Locarnini, S.; Martin, P.; Richman, D.D.; Zoulim, F. Virologic monitoring of hepatitis B virus therapy in clinical trials and practice: recommendations for a standardized approach. Gastroenterology 2008, 134, 405-415.
62. Das, K.; Xiong, X.; Yang, H.; Westland, C.E.; Gibbs, C.S.; Sarafianos, S.G.; Arnold, E. Molecular modeling and biochemical characterization reveal the mechanism of hepatitis B virus polymerase resistance to lamivudine (3TC) and emtricitabine (FTC). J. Virol. 2001, 75, 4771-4779.
63. Yatsuji, H.; Noguchi, C.; Hiraga, N.; Mori, N.; Tsuge, M.; Imamura, M.; Takahashi, S.; Iwao, E.; Fujimoto, Y.; Ochi, H.; Abe, H.; Maekawa, T.; Tateno, C.; Yoshizato, K.; Suzuki, F.; Kumada, H.; Chayama, K. Emergence of a novel lamivudine-resistant hepatitis B virus variant with a substitution outside the YMDD motif. Antimicrob. Agents Chemother. 2006, 50, 3867-3874.
64. Yang, H.; Qi, X.; Sabogal, A.; Miller, M.; Xiong, S.; Delaney, W.E. Cross-resistance testing of next-generation nucleoside and nucleotide analogues against lamivudine-resistant HBV. Antiviral Ther. 2005, 10, 625-633.
65. Karatayli, E.; Karayalçin, S.; Karaaslan, H.; Kayhan, H.; Türkyilmaz, A.R.; Sahin, F.; Yurdaydin, C.; Bozdayi, A.M. A novel mutation pattern emerging during lamivudine treatment shows cross-resistance to adefovir dipivoxil treatment. Antiviral Ther. 2007, 12, 761-768.
66. De Clercq, E.; Holý A.; Rosenberg, I.; Sakuma, T.; Balzarini, J.; Maudgal, P.C. A novel selective broad-spectrum anti-DNA virus agent. Nature 1986, 323, 464-467.
67. Merta, A.; Votruba, I.; Jindrich, J.; Holý, A.; Cihlár, T.; Rosenberg, I.; Otmar, M.; Herve, T.Y. Phosphorylation of 9-(2-phosphonomethoxyethyl)adenine and 9-(S)-(3-hydroxy-2-phosphonomethoxypropyl)adenine by AMP(dAMP) kinase from L1210 cells. Biochem. Pharmacol. 1992, 44, 2067-2077.
68. De Clercq, E. Antivirals and antiviral strategies. Nat. Rev. Microbiol. 2004, 2, 704-720.
69. Shen, Y.; Zhukovskaya, N.L.; Zimmer, M.I.; Soelaiman, S.; Bergson, P.; Wang, C.R.; Gibbs, C.S.; Tang, W.J. Selective inhibition of anthrax edema factor by adefovir, a drug for chronic hepatitis B virus infection. Proc. Natl. Acad. Sci. USA 2004, 101, 3242-3247.
70. Werle-Lapostolle, B.; Bowden, S.; Locarnini, S.; Wursthorn, K.; Petersen, J.; Lau, G.; Trepo, C.; Marcellin, P.; Goodman, Z.; Delaney, W.E. 4th; Xiong, S.; Brosgart, C.L.; Chen, S.S.; Gibbs, CS; Zoulim, F. Persistence of cccDNA during the natural history of chronic hepatitis B and decline during adefovir dipivoxil therapy. Gastroenterology 2004, 126, 1750-1758.
71. Hadziyannis, S.J.; Tassopoulos, N.C.; Heathcote, E.J.; Chang, T.T.; Kitis, G.; Rizzetto, M.; Marcellin, P.; Lim, S.G.; Goodman, Z.; Wulfsohn, M.S.; Xiong, S.; Fry, J.; Brosgart, C.L. Adefovir dipivoxil for the treatment of hepatitis B e antigen-negative chronic hepatitis B. N. Engl. J. Med. 2003, 348, 800-807.
72. Marcellin, P.; Chang, T.T.; Lim, S.G.; Tong, M.J.; Sievert, W.; Shiffman, M.L.; Jeffers, L.; Goodman, Z.; Wulfsohn, M.S.; Xiong, S.; Fry, J.; Brosgart, C.L. Adefovir dipivoxil 437 study group. Adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. N. Engl. J. Med. 2003, 348, 848-850.
73. Hadziyannis, S.J.; Tassopoulos, N.C.; Heathcote, E.J.; Chang, T.T.; Kitis, G.; Rizzetto, M.; Marcellin, P.; Lim, S.G.; Goodman, Z.; Ma, J.; Arterburn, S.; Xiong, S.; Currie, G.; Brosgart, C.L. Long-term therapy with adefovir dipivoxil for HBeAg-negative chronic hepatitis B. N. Engl. J. Med. 2005, 352, 2673-2681.
74. Carrouée-Durantel, S.; Durantel, D.; Werle-Lapostolle, B.; Pichoud, C.; Naesens, L.; Neyts, J.; Trépo, C.; Zoulim, F. Suboptimal response to adefovir dipivoxil therapy for chronic hepatitis B in nucleoside-naive patients is not due to pre-existing drug-resistant mutants. Antiviral Ther. 2008, 13, 381-388.
75. Hadziyannis, S.J.; Tassopoulos, N.C.; Heathcote, E.J.; Chang, T.T.; Kitis, G.; Rizzetto, M.; Marcellin, P.; Lim, S.G.; Goodman, Z.; Ma, J.; Brosgart, C.L.; Borroto-Esoda, K.; Arterburn, S.; Chuck, S.L.; Adefovir Dipivoxil 438 Study Group. Long-term therapy with adefovir dipivoxil for HBeAg-negative chronic hepatitis B for up to 5 years. Gastroenterology 2006, 131, 1743-1751.
76. Schiff, E.; Lai, C.L.; Hadziyannis, S.; Neuhaus, P.; Terrault, N.; Colombo, M.; Tillmann, H.; Samuel, D.; Zeuzem, S.; Villeneuve, J.P.; Arterburn, S.; Borroto-Esoda, K.; Brosgart, C.; Chuck, S. Adefovir dipivoxil for wait-listed and post-liver transplantation patients with lamivudine-resistant hepatitis B: final long-term results. Liver Transpl. 2007, 13, 349-360.
77. Marcellin, P.; Asselah, T. Resistance to adefovir: a new challenge in the treatment of chronic hepatitis B. J. Hepatol. 2005, 43, 920-923.
78. Borroto-Esoda, K.; Miller, M.D.; Arterburn, S. Pooled analysis of amino acid changes in the HBV polymerase in patients from four major adefovir dipivoxil clinical trials. J. Hepatol. 2007, 47, 492-498
79. Gallego, A.; Sheldon, J.; García-Samaniego, J.; Margall, N.; Romero, M.; Hornillos, P.; Soriano, V.; Enrĺquez, J. Evaluation of initial virological response to adefovir and development of adefovir-resistant mutations in patients with chronic hepatitis B. J. Viral Hepat. 2008, 15, 392-398.
80. Lacombe, K.; Ollivet, A.; Gozlan, J.; Durantel, S.; Tran, N.; Girard, P.M.; Zoulim, F. A novel hepatitis B virus mutation with resistance to adefovir but not to tenofovir in an HIV-hepatitis B virus-co-infected patient. AIDS 2006, 20, 2229-2231.
81. Osiowy, C.; Villeneuve, J.P.; Heathcote, E.J.; Giles, E.; Borlang, J. Detection of rtN236T and rtA181V/T mutations associated with resistance to adefovir dipivoxil in samples from patients with chronic hepatitis B virus infection by the INNO-LiPA HBV DR Line Probe Assay (version 2). J. Clin. Microbiol. 2006, 44, 1994-1997.
82. Lee, Y.S.; Suh, D.J.; Lim, Y.S.; Jung, S.W.; Kim, K.M.; Lee, H.C.; Chung, Y.H.; Lee, Y.S.; Yoo, W.; Kim, S.O. Increased risk of adefovir resistance in patients with lamivudine-resistant chronic hepatitis B after 48 weeks of adefovir dipivoxil monotherapy. Hepatology 2006, 43, 1385-1391.
83. Schildgen, O.; Sirma, H.; Funk, A.; Olotu, C.; Wend, U.C.; Hartmann, H.; Helm, M.; Rockstroh, J.K.; Willems, W.R.; Will, H.; Gerlich, W.H. Variant of hepatitis B virus with primary resistance to adefovir. N. Engl. J. Med. 2006, 354, 1807-1812.
84. Villeneuve, J.P.; Durantel, D.; Durantel, S.; Westland, C.; Xiong, S.; Brosgart, C.L.; Gibbs, C.S.; Parvaz, P.; Werle, B.; Trépo, C.; Zoulim, F. Selection of a hepatitis B virus strain resistant to adefovir in a liver transplantation patient. J. Hepatol. 2003, 39, 1085-1089.
85. Fung, S.K.; Andreone, P.; Han, S.H.; Reddy, K.R.; Regev, A.; Keeffe, E.B.; Hussain, M.; Cursaro, C.; Richtmyer, P.; Marrero, J.A.; Lok, A.S.F. Adefovir-resistant hepatitis B can be associated with viral rebound and hepatic decompensation. J. Hepatol. 2005, 43, 937-943.
86. Fung, S.K.; Chae, H.B.; Fontana, R.J.; Conjeevaral, H.; Marrero, J.; Oberhelman, K.; Hussain, M.; Lok, A.S.F. Virologic response and resistance to adefovir in patients with chronic hepatitis B. J. Hepatol. 2006, 44, 283-290.
87. Zoulim F, Parvaz P, Marcellin P, Zarski JP, Beaugrand M, Benhamou Y, Bailly F, Maynard M, Trepo C, Trylesinski A, Monchecourt F. Adefovir dipivoxil is effective for the treatment of cirrhotic patients with lamivudine failure. Liver Int. 2009, 29, 420-426.
88. Yamanaka, G.; Wilson, T.; Innaimo, S.; Bisacchi, G.S.; Egli, P.; Rinehart, J.K.; Zahler, R.; Colonno, R.J. Metabolic studies on BMS-200475, a new antiviral compound active against hepatitis B virus. Antimicrob. Agents Chemother. 1999, 43, 190-193.
89. Zoulim, F. Entecavir: a new treatment option for chronic hepatitis B. J. Clin. Virol. 2006, 36, 8-12.
90. Seifer, M.; Hamatake, R.K.; Colonno, R.J.; Standring, D.N. In vitro inhibition of hepadnavirus polymerases by the triphosphates of BMS-200475 and lobucavir. Antimicrob. Agents Chemother. 1998, 42, 3200-3208.
91. Tchesnokov, E.P.; Obikhod, A.; Schinazi, R.F.; Götte, M. Delayed chain termination protects the anti-hepatitis B virus drug entecavir from excision by HIV-1 reverse transcriptase. J. Biol. Chem. 2008, 283, 34218-34228.
92. Colonno, R.J.; Genovesi, E.V.; Medina, I.; Lamb, L.; Durham, S.K.; Huang, M.L.; Corey, L.; Littlejohn, M.; Locarnini, S.; Tennant, B.C.; Rose, B.; Clark, J.M. Long-term entecavir treatment results in sustained antiviral efficacy and prolonged life span in the woodchuck model of chronic hepatitis infection. J. Infect. Dis. 2001, 184, 1236-1245.
93. Chang, T.T.; Gish, R.G.; de Man, R.; Gadano, A.; Sollano, J.; Chao, Y.C.; Lok, A.S.; Han, K.H.; Goodman, Z.; Zhu, J.; Cross, A.; DeHertogh, D.; Wilber, R.; Colonno, R.; Apelian, D. A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. N. Engl. J. Med. 2006, 354, 1001-1010.
94. Lai, C.L.; Shouval, D.; Lok, A.S.; Chang, T.T.; Cheinquer, H.; Goodman, Z.; DeHertogh, D.; Wilber, R.; Zink, R.C.; Cross, A.; Colonno, R.; Fernandes, L. Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. N. Engl. J. Med. 2006, 354, 1011-1020.
95. Sherman, M.; Yurdaydin, C.; Simsek, H.; Silva, M.; Liaw, Y.F.; Rustgi, V.K.; Sette, H.; Tsai, N.; Tenney, D.J.; Vaughan, J.; Kreter, B.; Hindes, R. Entecavir therapy for lamivudine-refractory chronic hepatitis B: improved virologic, biochemical, and serology outcomes through 96 weeks. Hepatology 2008, 48, 99-108.
96. Yao, G. Entecavir is a potent anti-HBV drug superior to lamivudine: experience from clinical trials in China. J. Antimicrob. Chemother. 2007, 60, 201-205.
97. Reijnders, J.G.P., Pas, S.D., Schutten, M., de Man, R.A., Janssen, H.L.A. Entecavir shows limited efficacy in HBeAg-positive hepatitis B patients with a partial virologic response to adefovir therapy. J. Hepatol. 2009, 50, 674-683.
98. Tenney, D.J.; Levine, S.M.; Rose, R.E.; Walsh, A.W.; Weinheimer, S.P.; Discotto, L.; Plym, M.; Pokornowski, K.; Yu, C.F.; Angus, P.; Ayres, A.; Bartholomeusz, A.; Sievert, W.; Thompson, G.; Warner, N.; Locarnini, S.; Colonno, R.J. Clinical emergence of entecavir-resistant hepatitis B virus requires additional substitutions in virus already resistant to lamivudine. Antimicrob. Agents Chemother. 2004, 48, 3498-3507.
99. Baldick CJ, Tenney DJ, Mazzucco CE, Eggers BJ, Rose RE, Pokornowski KA, Yu CF, Colonno RJ. Comprehensive evaluation of hepatitis B virus reverse transcriptase substitutions associated with entecavir resistance. Hepatology 2008, 47, 1473-1482.
100. Baldick, C.J., Eggers, B.J., Fang, J., Levine, S.M., Pokornowski, K.A., Rose, R.E., Yu, C.-F., Tenney, D.J., Colonno, R.J. Hepatitis B virus quasispecies susceptibility to entecavir confirms the relationship between genotypic resistance and patient virologic response. J. Hepatol. 2008, 48, 895-902.
101. Nagasaki, F.; Niitsuma, H.; Ueno, Y.; Inoue, J.; Kogure, T.; Fukushima, K.; Shimosegawa, T. The high incidence of the emergence of entecavir-resistant mutants among patients infected with lamivudine-resistant hepatitis B virus. Tohoku J. Exp. Med. 2007, 213, 181-186.
102. Tenney, D.J.; Rose, R.E.; Baldick, C.J.; Pokornowski, K.A.; Eggers, B.J.; Fang, J.; Wichroski, M.J.; Xu, D.; Yang, J.; Wilber, R.B.; Colonno, R.J. Long-term monitoring shows hepatitis B virus resistance to entecavir in nucleoside-naïve patients is rare through 5 years of therapy. Hepatology 2009, 49, 1503-1514.
103. McMahon, M.A.; Jilek, B.L.; Brennan, T.P.; Shen, L.; Zhou, Y.; Wind-Rotolo, M.; Xing, S.; Bhat, S.; Hale, B.; Hegarty, R.; Chong, C.R.; Liu, J.O.; Siliciano, R.F.; Thio, C.L. The HBV drug entecavir - effects on HIV-1 replication and resistance. N. Engl. J. Med. 2007, 356, 2614-2621.
104. Jain, M.K.; Zoellner, C.L. Entecavir can select for M184V of HIV-1: a case of an HIV/hepatitis B (HBV) naïve patient treated for chronic HBV. AIDS 2007, 21, 2365-2366.
105. Sasadeusz, J. The anti-HIV antiviral activity of entecavir: the loss of a trusted friend? J. Hepatol. 2007, 47, 872-874.
106. Lin, P.F.; Nowicka-Sans, B.; Terry, B.; Zhang, S.; Wang, C.; Fan, L.; Dicker, I.; Gali, V.; Higley, H.; Parkin, N.; Tenney, D.; Krystal, M.; Colonno, R. Entecavir exhibits inhibitory activity against human immunodeficiency virus under conditions of reduced viral challenge. Antimicrob. Agents Chemother. 2008, 52, 1759-1767.
107. Zhu M, Bifano M, Xu X, Wang Y, LaCreta F, Grasela D, Pfister M. Lack of an effect of human immunodeficiency virus coinfection on the pharmacokinetics of entecavir in hepatitis B virus-infected patients. Antimicrob. Agents Chemother. 2008, 52, 2836-2841.
108. Keam, S.J. Telbivudine. Drugs 2007, 67, 1917-1929.
109. Nash, K. Telbivudine in the treatment of chronic hepatitis B. Adv. Ther. 2009, 26, 155-169.
110. Ruiz-Sancho, A.; Sheldon, J.; Soriano, V. Telbivudine: a new option for the treatment of chronic hepatitis B. Exp. Opin. Biol. Ther. 2007, 7, 751-761.
111. Bryant, M.L.; Bridges, E.G.; Placidi, L.; Faraj, A.; Loi, A.G.; Pierra, C.; Dukhan, D.; Gosselin, G.; Imbach, J.L.; Hernandez, B.; Juodawlkis, A.; Tennant, B.; Korba, B.; Cote, P.; Marion, P.; Cretton-Scott, E.; Schinazi, R.F.; Sommadossi, J.P. Antiviral L-nucleosides specific for hepatitis B virus infection. Antimicrob Agents Chemother 2001, 45, 229-235.
112. Hernandez-Santiago, B.; Placidi, L.; Cretton-Scott, E.; Faraj, A.; Bridges, E.G.; Bryant, M.L.; Rodriguez-Orengo, J.; Imbach, J.L.; Gosselin, G.; Pierra, C.; Dukhan, D.; Sommadossi, J.P. Pharmacology of beta-L-thymidine and beta-L-2'-deoxycytidine in HepG2 cells and primary human hepatocytes: relevance to chemotherapeutic efficacy against hepatitis B virus. Antimicrob Agents Chemother 2002, 46, 1728-1733.
113. Kim, J.W.; Park, S.H.; Louie, S.G. Telbivudine: A novel nucleoside analog for chronic hepatitis B. Ann Pharmacother 2006, 40, 472-478.
114. Lai, C.L.; Lim, S.G.; Brown, N.A.; Zhou, X.J.; Lloyd, D.M.; Lee, Y.M.; Yuen, M.F.; Chao, G.C.; Myers, M.W. A dose-finding study of once-daily oral telbivudine in HBeAg-positive patients with chronic hepatitis B virus infection. Hepatology 2004, 40, 719-726.
115. Lai, C.L.; Leung, N.; Teo, E.K.; Tong, M.; Wong, F.; Hann, H.W.; Han, S.; Poynard, T.; Myers, M.; Chao, G.; Lloyd, D.; Brown, N.A. A 1-year trial of telbivudine, lamivudine, and the combination in patients with hepatitis B e antigen-positive chronic hepatitis B. Gastroenterology 2005, 129, 528-536.
116. Chan, H.L.; Heathcote, E.J.; Marcellin, P.; Lai, C.L.; Cho, M.; Moon, Y.M.; Chao, Y.C.; Myers, R.P.; Minuk, G.Y.; Jeffers, L.; Sievert, W.; Bzowej, N.; Harb, G.; Kaiser, R.; Qiao, X.J.; Brown, N.A. Treatment of hepatitis B e antigen positive chronic hepatitis with telbivudine or adefovir: a randomized trial. Ann. Intern. Med. 2007, 147, 745-754.
117. Lai, C.L.; Gane, E.; Liaw, Y.F.; Hsu, C.W.; Thongsawat, S.; Wang, Y.; Chen, Y.; Heathcote, E.J.; Rasenack, J.; Bzowej, N.; Naoumov, N.V.; Di Bisceglie, A.M.; Zeuzem, S.; Moon, Y.M.; Goodman, Z.; Chao, G.; Constance, B.F.; Brown, N.A. Telbivudine versus lamivudine in patients with chronic hepatitis B. N. Engl. J. Med. 2007, 357, 2576-2588.
118. Hou, J.; Yin, Y.K.; Xu, D.; Tan, D.; Niu, J.; Zhou, X.; Wang, Y.; Zhu, L.; He, Y.; Ren, H.; Wan, M.; Chen, C.; Wu, S.; Chen, Y.; Xu, J.; Wang, Q.; Wei, L.; Chao, G.; Constance, B.F.; Harb, G.; Brown, N.A.; Jia, J. Telbivudine versus lamivudine in Chinese patients with chronic hepatitis B: Results at 1 year of a randomized, double-blind trial. Hepatology 2008, 47, 447-454.
119. Zeuzem, S.; Gane, E.; Liaw, Y.F.; Lim, S.G.; DiBisceglie, A.; Buti, M.; Chutaputti, A.; Rasenack, J.; Hou, J.; O'Brien, C.; Nguyen, T.T.; Jia, J.; Poynard, T.; Belanger, B.; Bao, W.; Naoumov, N.V. Baseline characteristics and early on-treatment response predict the outcomes of 2 years of telbivudine treatment of chronic hepatitis B. J. Hepatol. 2009, 51, 11-20.
120. Liaw, Y.F.; Gane, E.; Leung, N.; Zeuzem, S.; Wang, Y.; Lai, C.L.; Heathcote, E.J.; Manns, M.; Bzowej, N.; Niu, J.; Han, S.H.; Hwang, S.G.; Cakaloglu, Y.; Tong, M.J.; Papatheodoridis, G.; Chen, Y.; Brown, N.A.; Albanis, E.; Galil, K.; Naoumov, N.V. 2-Year GLOBE trial results: telbivudine Is superior to lamivudine in patients with chronic hepatitis B. Gastroenterology 2009, 136, 486-495.
121. Zhou, X.J.; Fielman, B.A.; Lloyd, D.M.; Chao, G.C.; Brown, N.A. Pharmacokinetics of telbivudine in healthy subjects and absence of drug interaction with lamivudine or adefovir dipivoxil. Antimicrob. Agents Chemother. 2006, 50, 2309-2315.
122. Seifer, M.; Patty, A.; Serra, I.; Li, B.; Standring, D.N. Telbivudine, a nucleoside analog inhibitor of HBV polymerase, has a different in vitro cross-resistance profile than the nucleotide analog inhibitors adefovir and tenofovir. Antiviral Res. 2009, 81, 147-155.
123. Thomas, H.; Foster, G.; Platis, D. Mechanisms of action of interferon and nucleoside analogues. J. Hepatol. 2003, 39, S1, S93-98.
124. Lok, A.S.F.; McMahon, B.J. Chronic hepatitis B. Hepatology 2007, 45, 507-539.
125. Lau, G.K.; Piratvisuth, T.; Luo, K.X.; Marcellin, P.; Thongsawat, S.; Cooksley, G.; Gane, E.; Fried, M.W.; Chow, W.C.; Paik, S.W.; Chang, W.Y.; Berg, T.; Flisiak, R.; McCloud, P.; Pluck, N. Peginterferon Alfa-2a, lamivudine, and the combination for HBeAg-positive chronic hepatitis B. N. Engl. J. Med. 2005, 352, 2682-2695.
126. Brunetto, M.R.; Moriconi, F.; Bonino, F.; Lau, G.K.; Farci, P.; Yurdaydin, C.; Piratvisuth, T.; Luo, K.; Wang, Y.; Hadziyannis, S.; Wolf, E.; McCloud, P.; Batrla, R.; Marcellin, P. Hepatitis B virus surface antigen levels: a guide to sustained response to peginterferon alfa-2a in HBeAg-negative chronic hepatitis B. Hepatology 2009, 49, 1141-1150.
127. Janssen, H.L.; van Zonneveld, M.; Senturk, H.; Zeuzem, S.; Akarca, U.S.; Cakaloglu, Y.; Simon, C.; So, T.M.; Gerken, G.; de Man, R.A.; Niesters, H.G, Zondervan, P.; Hansen, B.; Schalm, S.W. Pegylated interferon alpha-2b alone or in combination with lamivudine for HBeAg-positive chronic hepatitis B: a randomised trial. Lancet 2005, 365, 123-129.
128. Liu, C.J.; Lai, M.Y.; Chao, Y.C.; Liao, L.Y.; Yang, S.S, Hsiao TJ, Hsieh TY, Lin CL, Hu JT, Chen CL, Chen PJ, Kao JH, Chen DS. Interferon alpha-2b with and without ribavirin in the treatment of hepatitis B e antigen-positive chronic hepatitis B: a randomized study. Hepatology 2006, 43, 742-749.
129. Wursthorn, K.; Lutgehetmann, M.; Dandri, M.; Volz, T.; Buggisch, P.; Zollner, B.; Longerich, T.; Schirmacher, P.; Metzler, F.; Zankel, M.; Fischer, C.; Currie, G.; Brosgart, C.; Petersen, J. Peginterferon alpha-2b plus adefovir induce strong cccDNA decline and HBsAg reduction in patients with chronic hepatitis B. Hepatology 2006, 44, 675-684.
130. Buster, E.H.; Hansen, B.E.; Buti, M.; Delwaide, J.; Niederau, C.; Michielsen, P.P.; Flisiak, R.; Zondervan, P.E.; Schalm, S.W.; Janssen, H.L. Peginterferon alpha-2b is safe and effective in HBeAg-positive chronic hepatitis B patients with advanced fibrosis. Hepatology 2007, 46, 388-394.
131. Benhamou, Y.; Fleury, H.; Trimoulet, P.; Pellegrin, I.; Urbinelli, R.; Katlama, C.; Rozenbaum, W.; Le Teuff, G.; Trylesinski, A.; Piketty, C. Anti-hepatitis B virus efficacy of tenofovir disoproxil fumarate in HIV-infected patients. Hepatology 2006, 43, 548-555.
132. Zhu Y.; Curtis, M.; Qi, X.; Miller, M.D.; Borroto-Esoda, K. Anti-hepatitis B virus activity in vitro of combinations of tenofovir with nucleoside/nucleotide analogues. Antiviral Chem. Chemother. 2009, 19, 165-176.
133. Delaney, W.E. 4th; Ray, A.S.; Yang, H.; Qi, X.; Xiong, S.; Zhu, Y.; Miller, M.D. Intracellular metabolism and in vitro activity of tenofovir against hepatitis B virus. Antimicrob. Agents Chemother. 2006, 50, 2471-2477.
134. Birkus, G.; Hajek, M.; Kramata, P.; Votruba, I.; Holý, A.; Otova, B. Tenofovir diphosphate is a poor substrate and a weak inhibitor of rat DNA polymerases alpha, delta, and epsilon*. Antimicrob. Agents Chemother. 2002, 46, 1610-1613.
135. Delaney, W.E. 4th; Borroto-Esoda, K. Therapy of chronic hepatitis B: trends and developments. Curr. Opin. Pharmacol. 2008, 8, 532-540.
136. Marcellin, P.; Heathcote, E.J.; Buti, M.; Gane, E.; de Man, R.A.; Krastev, Z.; Germanidis, G.; Lee, S.S.; Flisiak, R.; Kaita, K.; Manns, M.; Kotzev, I.; Tchernev, K.; Buggisch, P.; Weilert, F.; Kurdas, O.O.; Shiffman, M.L.; Trinh, H.; Washington, M.K.; Sorbel, J.; Anderson, J.; Snow-Lampart, A.; Mondou, E.; Quinn, J.; Rousseau, F. Tenofovir disoproxil fumarate versus adefovir dipivoxil for chronic hepatitis B. N. Engl. J. Med. 2008, 359, 2442-2455.
137. Lacombe, K.; Gozlan, J.; Boyd, A.; Boelle, P.Y.; Bonnard, P.; Molina, J.M.; Miailhes, P.; Lascoux-Combe, C.; Serfaty, L.; Zoulim, F.; Girard, P.M. Comparison of the antiviral activity of adefovir and tenofovir on hepatitis B virus in HIV-HBV-coinfected patients. Antiviral Ther. 2008, 13, 705-713.
138. Del Poggio, P.; Zaccanelli, M.; Oggionni, M.; Colombo, S.; Jamoletti, C.; Puhalo, V. Low-dose tenofovir is more potent than adefovir and is effective in controlling HBV viremia in chronic HBeAg-negative hepatitis B. World J. Gastroenterol. 2007, 13, 4096-4099.
139. Tan, J.; Degertekin, B.; Wong, S.N.; Husain, M.; Oberhelman, K.; Lok, A.S. Tenofovir monotherapy is effective in hepatitis B patients with antiviral treatment failure to adefovir in the absence of adefovir-resistant mutations. J. Hepatol. 2008, 48, 391-398.
140. Leemans, W.F.; Janssen, H.L.; Niesters, H.G.; de Man, R.A. Switching patients with lamivudine resistant chronic hepatitis B virus from tenofovir to adefovir results in less potent HBV-DNA suppression. J. Viral Hepat. 2008, 15, 108-114.
141. Gutiérrez, S.; Guillemi, S.; Jahnke, N.; Montessori, V.; Harrigan, P.R.; Montaner, J.S. Tenofovir-based rescue therapy for advanced liver disease in 6 patients coinfected with HIV and hepatitis B virus and receiving lamivudine. Clin. Infect. Dis. 2008, 46, e28-30.
142. Menne, S.; Cote, P.J.; Korba, B.E.; Butler, S.D.; George, A.L.; Tochkov, I.A.; Delaney, W.E. 4th; Xiong, S.; Gerin, J.L.; Tennant, B.C. Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob. Agents Chemother. 2005, 49, 2720-2728.
143. Sheldon, J.; Camino, N.; Rodés, B.; Bartholomeusz, A.; Kuiper, M.; Tacke, F.; Núñez, M.; Mauss, S.; Lutz, T.; Klausen, G.; Locarnini, S.; Soriano, V. Selection of hepatitis B virus polymerase mutations in HIV-coinfected patients treated with tenofovir. Antiviral Ther. 2005, 10, 727-734.
144. Amini-Bavil-Olyaee, S.; Herbers, U.; Sheldon, J.; Luedde, T.; Trautwein, C.; Tacke, F. The rtA194T polymerase mutation impacts viral replication and susceptibility to tenofovir in hepatitis B e antigen-positive and hepatitis B e antigen-negative hepatitis B virus strains. Hepatology 2009, 49, 1158-1165.
145. van Bömmel, F.; Zöllner, B.; Sarrazin, C.; Spengler, U.; Hüppe, D.; Möller, B.; Feucht, H.H.; Wiedenmann, B.; Berg, T. Tenofovir for patients with lamivudine-resistant hepatitis B virus (HBV) infection and high HBV DNA level during adefovir therapy. Hepatology 2006, 44, 318-325.
146. Korba, B.E.; Schinazi, R.F.; Cote, P.; Tennant, B.C.; Gerin, J.L. Effect of oral administration of emtricitabine on woodchuck hepatitis virus replication in chronically infected woodchucks. Antimicrob. Agents Chemother. 2000, 44, 1757-1760.
147. Gish, R.G.; Trinh, H.; Leung, N.; Chan, F.K.; Fried, M.W.; Wright, T.L.; Wang, C.; Anderson, J.; Mondou, E.; Snow, A.; Sorbel, J.; Rousseau, F.; Corey, L. Safety and antiviral activity of emtricitabine (FTC) for the treatment of chronic hepatitis B infection: a two-year study. J. Hepatol. 2005, 43, 60-66.
148. Lim, S.G.; Krastev, Z.; Ng, T.M.; Mechkov, G.; Kotzev, I.A.; Chan, S.; Mondou, E.; Snow, A.; Sorbel, J.; Rousseau, F. Randomized, double-blind study of emtricitabine (FTC) plus clevudine versus FTC alone in treatment of chronic hepatitis B. Antimicrob. Agents Chemother. 2006, 50, 1642-1648.
149. Marcellin, P.; Mommeja-Marin, H.; Sacks, S.L.; Lau, G.K.; Sereni, D.; Bronowicki, J.P.; Conway, B.; Trepo, C.; Blum, M.R.; Yoo, B.C.; Mondou, E.; Sorbel, J.; Snow, A.; Rousseau, F.; Lee, H.S. A phase II dose-escalating trial of clevudine in patients with chronic hepatitis B. Hepatology 2004, 40, 140-148.
150. Goulis, I.; Dalekos, G.N. Entecavir monotherapy for lamivudine-refractory chronic hepatitis B. Expert Rev. Anti Infect. Ther. 2008, 6, 855-859.
151. Yoo, B.C.; Kim, J.H.; Chung, Y.H.; Lee, K.S.; Paik, S.W.; Ryu, S.H.; Han, B.H.; Han, J.Y.; Byun, K.S.; Cho, M.; Lee, H.J.; Kim, T.H.; Cho, S.H.; Park, J.W.; Um, SH.; Hwang, S.G.; Kim, Y.S.; Lee, Y.J.; Chon, C.Y.; Kim, B.I.; Lee, Y.S.; Yang, J.M.; Kim, H.C.; Hwang, J.S.; Choi, S.K.; Kweon, Y.O.; Jeong, S.H.; Lee, M.S.; Choi, J.Y.; Kim, D.G.; Kim, Y.S.; Lee, H.Y.; Yoo, K.; Yoo, H.W.; Lee, H.S. Twenty-four-week clevudine therapy showed potent and sustained antiviral activity in HBeAg-positive chronic hepatitis B. Hepatology 2007, 45, 1172-1178.
152. Yoo, B.C.; Kim, J.H.; Kim, T.H.; Koh, K.C.; Um, S.H.; Kim, Y.S.; Lee, K.S.; Han, B.H.; Chon, C.Y.; Han, J.Y.; Ryu, S.H.; Kim, H.C.; Byun, K.S.; Hwang, S.G.; Kim, B.I.; Cho, M.; Yoo, K.; Lee, H.J.; Hwang, J.S.; Kim, Y.S.; Lee, Y.S.; Choi, S.K.; Lee, Y.J.; Yang, J.M.; Park, J.W.; Lee, M.S.; Kim, D.G.; Chung, Y.H.; Cho, S.H.; Choi, J.Y.; Kweon, Y.O.; Lee, H.Y.; Jeong, S.H.; Yoo, H.W.; Lee, H.S. Clevudine is highly efficacious in hepatitis B e antigen-negative chronic hepatitis B with durable off-therapy viral suppression. Hepatology 2007, 46, 1041-1048.
153. Kim, B.K.; Oh, J.; Kwon, S.Y.; Choe, W.H.; Ko, S.Y.; Rhee, K.H.; Seo, T.H.; Lim, S.D.; Lee, C.H. Clevudine myopathy in patients with chronic hepatitis B. J. Hepatol. 2009; 51, 829-834.
154. Seok, J.I.; Lee, D.K.; Lee, C.H.; Park, M.S.; Kim, S.Y.; Kim, H.S.; Jo, H.Y.; Lee, C.H.; Kim, D.S. Long-term therapy with clevudine for chronic hepatitis B can be associated with myopathy characterized by depletion of mitochondrial DNA. Hepatology 2009, 49, 2080-2086
155. European Association for the Study of the Liver. EASL Clinical practice guidelines: management of chronic hepatitis B. J. Hepatol. 2009, 50, 227-242.
156. Lok, A.S.F.; McMahon, B.J. AASLD Practice guidelines. Chronic hepatitis B: update 2009. Hepatology 2009, 50, 1-36.
157. Liaw, Y.-F.; Suh, D.J.; Omata, M. APASL guidelines for HBV management. Presented at the APASL Annual Meeting, Seoul, Korea, 2008
158. Piratvisuth, T. Reviews for APASL guidelines: immunomodulatory therapy of chronic hepatitis B. Hepatol. Int. 2008, 2, 140-146.
159. Zoulim F.; Perrillo, R. Hepatitis B reflections on the current approach to antiviral therapy. J. Hepatol. 2008, 48 (Suppl. 1), S2-S19.
160. Lampertico, P.; Vigano, M.; Manenti, E.; Iavarone, M.; Colombo, M. Add-on adefovir prevents the emergence of adefovir resistance in lamivudine-resistant patients: a 4-year study. J. Hepatol. 2008, 48, S259.
161. Fournier, C.; Zoulim, F. Antiviral therapy of chronic hepatitis B prevention of drug resistance. Clin. Liver Dis. 2007, 11, 869-892.
162. Papatheodoridis, G.V.; Manolakopoulos, S.; Dusheiko, G.; Archimandritis, A.J. Therapeutic strategies in the management of patients with chronic hepatitis B virus infection. Lancet Infect. Dis. 2008, 8, 167-178.
163. Lampertico, P.; Colombo, M. HBeAg-negative chronic hepatitis B: why do I treat my patients with nucleos(t)ide analogues. Liver Int. 2009, 29, 130-132.
164. Liaw, Y.F. On-treatment outcome prediction and adjustment during chronic hepatitis B therapy: now and future. Antiviral Ther. 2009, 14, 13-22.