Entecavir for the treatment of chronic hepatitis B virus infection

Clinical Therapeutics

Volumn 28, Issue 2, 2006, Pages 184-203

  Matthews, S James ^a  

^a NORTHEASTERN UNIVERSITY   (United States)

Author keywords

adverse events; entecavir; hepatitis B virus; pharmacokinetics; therapeutic use

Indexed keywords

ADEFOVIR; ALANINE AMINOTRANSFERASE; AMINOTRANSFERASE; ANTIVIRUS AGENT; BILIRUBIN; CYTOCHROME P450; ENTECAVIR; HEMOGLOBIN; IMMUNOSUPPRESSIVE AGENT; LAMIVUDINE; LIVER ENZYME; PLACEBO; PROBENECID; TENOFOVIR; VIRUS DNA;

ABNORMALLY HIGH SUBSTRATE CONCENTRATION IN BLOOD; ABNORMALLY LOW SUBSTRATE CONCENTRATION IN BLOOD; ALANINE AMINOTRANSFERASE BLOOD LEVEL; ARTICLE; BILIRUBIN BLOOD LEVEL; BIOSIS; BRANCHED DNA SIGNAL AMPLIFICATION ASSAY; CHRONIC HEPATITIS; CLINICAL TRIAL; COMORBIDITY; COUGHING; CYTOTOXICITY; DIARRHEA; DISEASE SEVERITY; DIZZINESS; DOSE CALCULATION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG COST; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INDICATION; DRUG INDUCED HEADACHE; DRUG INDUSTRY; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENTIATION; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG TREATMENT FAILURE; DRUG USE; DRUG WITHDRAWAL; ENZYME SUBSTRATE; FATIGUE; GLOMERULUS FILTRATION; GRAFT VERSUS HOST REACTION; GROUPS BY AGE; HEMOGLOBIN BLOOD LEVEL; HEPATITIS B; HEPATITIS B VIRUS; HEPATOMEGALY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INFORMATION RETRIEVAL; INSOMNIA; KIDNEY FUNCTION; KIDNEY TUBULE EXCRETION; LACTIC ACIDOSIS; LETHARGY; LIVER DISEASE; LIVER HISTOLOGY; LIVER TRANSPLANTATION; LONG TERM POTENTIATION; MAXIMUM TOLERATED DOSE; MEDLINE; NAUSEA; NEUTROPHIL COUNT; PATIENT CARE; PHOTOSENSITIVITY; POLYMERASE CHAIN REACTION; PROTHROMBIN TIME; PUBLICATION; REFERENCE DATABASE; RHINOPHARYNGITIS; SOMNOLENCE; STATISTICAL SIGNIFICANCE; STEATOSIS; TABLET; THROMBOCYTE COUNT; TITRIMETRY; TREATMENT DURATION; TREATMENT OUTCOME; TREATMENT RESPONSE; UNSPECIFIED SIDE EFFECT; UPPER ABDOMINAL PAIN; UPPER RESPIRATORY TRACT INFECTION; URINARY EXCRETION; VIRUS REPLICATION;

ANTIVIRAL AGENTS; CLINICAL TRIALS; DRUG INTERACTIONS; DRUG RESISTANCE, VIRAL; GUANINE; HEPATITIS B, CHRONIC; HIV INFECTIONS; HUMANS; LIVER TRANSPLANTATION; MOLECULAR STRUCTURE;

EID: 33646186755     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/j.clinthera.2006.02.012     Document Type: Article

References (63)

1. Available at. US Food and Drug Administration approves Baraclude (entecavir) for treatment of chronic Hepatitis B. Accessed October 3, 2005. http://www.bms.com/news/press/data/fg_press_release_5480.html
2. Baraclude [package insert] (March 2005), Bristol-Myers Squibb Company, Princeton, NJ
3. [published corrections appear in N Engl J Med. 2005;352:740 and N Engl J Med. 2005;352:2362]. Poland G., and Jacobson R. Clinical practice: Prevention of hepatitis B with the hepatitis B vaccine. N Engl J Med 351 (2004) 2832-2838
4. Available at. World Health Organization. Hepatitis B vaccines. Weekly Epidemiological Record 79 (2004) 255-263. http://www.who.int/wer/2004/wer7928/en/
5. Alter M., and Mast E. The epidemiology of viral hepatitis in the United States. Gastroenterol Clin North Am. 23 (1994) 437-455
6. Lok A., McMahon B., Practice Guidelines Committee, and American Association for the Study of Liver Diseases (AASLD). Chronic hepatitis B: Update of recommendations. Hepatology 39 (2004) 857-861
7. Cooksley W., Piratvisuth T., Lee S., et al. Peginterferon alpha-2a (40 kDa): An advance in the treatment of hepatitis B e antigen-positive hepatitis B. J Viral Hepat. 10 (2003) 298-305
8. Marcellin P., Lau G., Bonino F., et al., the Peginterferon Alfa-2a HBeAg-Negative Chronic Hepatitis B Study Group. Peginterferon alfa-2a alone, lamivudine alone, and the two in combination in patients with HBeAg-negative chronic hepatitis B. N Engl J Med 351 (2004) 1206-1217
9. Chan H., Leung N., Hui A., et al. A randomized, controlled trial of combination therapy for chronic hepatitis B: Comparing pegylated interferon-alpha2b and lamivudine with lamivudine alone. Ann Intern Med 142 (2005) 240-250
10. Janssen H., van Zonneveld M., Senturk H., et al., the HBV 99-01 Study Group and the Rotterdam Foundation for Liver Research. Pegylated interferon alfa-2b alone or in combination with lamivudine for HBeAg-positive chronic hepatitis B: A randomised trial. Lancet 365 (2005) 123-129
11. Lau G., Piratvisuth T., Luo K., et al., the Peginterferon Alfa-2a HBeAg-Positive Chronic Hepatitis B Study Group. Peginterferon alfa-2a, lamivudine, and the combination for HBeAg-positive chronic hepatitis B. N Engl J Med 352 (2005) 2682-2695
12. Lai C., Chien R., Leung N., et al., the Asia Hepatitis Lamivudine Study Group. A one-year trial of lamivudine for chronic hepatitis B. N Engl J Med 339 (1998) 61-68
13. Liaw Y., Leung N., Chang T., et al., the Asia Hepatitis Lamivudine Study Group. Effects of extended lamivudine therapy in Asian patients with chronic hepatitis B. Gastroenterology 119 (2000) 172-180
14. Leung N., Lai C., Chang T., et al., the Asia Hepatitis Lamivudine Study Group. Extended lamivudine treatment in patients with chronic hepatitis B enhances hepatitis B e antigen seroconversion rates: Results after 3 years of therapy. Hepatology 33 (2001) 1527-1532
15. Gaia S., Marzano A., Smedile A., et al. Four years of treatment with lamivudine: Clinical and virological evaluations in HBe antigen-negative chronic hepatitis B. Aliment Pharmacol Ther. 20 (2004) 281-287
16. Dando T., and Plosker G. Adefovir dipivoxil: A review of its use in chronic hepatitis B. Drugs 63 (2003) 2215-2234
17. Lai C., Dienstag J., Schiff E., et al. Prevalence and clinical correlates of YMDD variants during lamivudine therapy for patients with chronic hepatitis B. Clin Infect Dis. 36 (2003) 687-696
18. Abstract 187. Guan R., Lai C., Liaw Y., et al. Efficacy and safety of 5 years lamivudine treatment of Chinese patients with chronic hepatitis B. J Gastroenterol Hepatol 16 Suppl 1 (2001) A60
19. Moskovitz D., Osiowy C., Giles E., et al. Response to long-term lamivudine treatment (up to 5 years) in patients with severe chronic hepatitis B, role of genotype and drug resistance. J Viral Hepat. 12 (2005) 398-404
20. Thio C. Hepatitis B in the human immunodeficiency virus-infected patient: Epidemiology, natural history, and treatment. Semin Liver Dis. 23 (2003) 125-136
21. de Franchis, Hadengue A., Lau G., et al., the EASL Jury. Suppl 1. EASL International Consensus Conference on Hepatitis B. 13-14 September, 2002 Geneva, Switzerland. J Hepatol 39 (2003) S3-S25 Consensus statement (long version)
22. Ide T., Kumashiro R., Kuwahara R., et al., the Hepatitis B Study Group. Clinical course of patients with chronic hepatitis B with viral breakthrough during long-term lamivudine treatment. J Gastroenterol 40 (2005) 625-630
23. Abstract 1141. Yang H., Westland C., Delaney IV W., et al. Complete genotypic and phenotypic analyses of HBV mutations identified in HBeAg-negative chronic hepatitis B patients receiving 96 weeks of adefovir dipivoxil (ADV). Hepatology 38 Suppl 1 (2003) 705A
24. Hadziyannis S., Tassopoulos N., Heathcote E., et al., the Adefovir Dipivoxil 438 Study Group. Longterm therapy with adefovir dipivoxil for HBeAg-negative chronic hepatitis B. N Engl J Med 352 (2005) 2673-2681
25. Available at. Locarnini S., Qi X., Arterburn S., et al. Incidence and predictors of emergence of HBV mutations associated with ADV resistance during 4 years of ADV therapy for patients with chronic HBV. Presented at: 40th Annual Meeting of the European Association for the Study of the Liver. Paris, France (April 13-17, 2005). http://www.natap.org/2005/EASL/easl_14.htm
26. Yamanaka G., Wilson T., Innaimo S., et al. Metabolic studies on BMS-200475, a new antiviral compound active against hepatitis B virus. Antimicrob Agents Chemother 43 (1999) 190-193
27. Innaimo S., Seifer M., Bisacchi G., et al. Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother 41 (1997) 1444-1448
28. Seifer M., Hamatake R., Colonno R., and Standring D. In vitro inhibition of hepadnavirus polymerases by the triphosphates of BMS-200475 and lobucavir. Antimicrob Agents Chemother 42 (1998) 3200-3208
29. Abstract 102. Slusarchyk W., Field A., Greytok J., et al. 4-Hydroxy-3-(hydroxymethyl)-2-methylcyclopentyl purines and pyrimidines, a novel class of antiherpesvirus agents. Antivir Res 17 Suppl 1 (1992) 98
30. Delaney IV W., Yang H., Miller M., et al. Combinations of adefovir with nucleoside analogs produce additive antiviral effects against hepatitis B virus in vitro. Antimicrob Agents Chemother 48 (2004) 3702-3710
31. Stuyver L., Locarnini S., Lok A., et al. Nomenclature for antiviral-resistant human hepatitis B virus mutations in the polymerase region. Hepatology 33 (2001) 751-757
32. Li M., Hou W., Wo J., and Liu K. Character of HBV (hepatitis B virus) polymerase gene rtM204V/I and rtL180M mutation in patients with lamivudine resistance. J Zhejiang Univ Sci B 6 (2005) 664-667
33. Ono S., Kato N., Shiratori Y., et al. The polymerase L528M mutation cooperates with nucleotide binding-site mutations, increasing hepatitis B virus replication and drug resistance. J Clin Invest 107 (2001) 449-455
34. Levine S., Hernandez D., Yamanaka G., et al. Efficacies of entecavir against lamivudine-resistant hepatitis B virus replication and recombinant polymerases in vitro. Antimicrob Agents Chemother 46 (2002) 2525-2532
35. Sherman M., Yurdaydin C., Sollano J., et al. Entecavir is superior to continued lamivudine for the treatment of lamivudine-refractory, HBeAg(+) chronic hepatitis B: Results of the Phase III study ETV-026. Presented at: 55th Annual Meeting of the American Association for the Study of Liver Diseases. October 29-November 2, 2004 (1941), Poster, Boston, Mass.
36. Brunelle M., Jacquard A., Pichoud C., et al. Susceptibility to antivirals of a human HBV strain with mutations conferring resistance to both lamivudine and adefovir. Hepatology 41 (2005) 1391-1398
37. Abstract 478. Colonno R., Rose R., Levine S., et al. Entecavir (ETV) resistance is not observed in nucleoside-naive subjects and is observed infrequently by week 48 in lamivudine-refractory subjects with chronic HBV infection. J Hepatol 42 Suppl 2 (2005) 173
38. Tenney D., Levine S., Rose R., et al. Clinical emergence of entecavir-resistant hepatitis B virus requires additional substitutions in virus already resistant to lamivudine. Antimicrob Agents Chemother 48 (2004) 3498-3507
39. Poster 1202. Bifano M., Yan J., Zhang D., et al. Hepatic impairment does not alter single-dose pharmacokinetics and safety of entecavir. Presented at: 55th Annual Meeting of the American Association for the Study of Liver Diseases. Boston, Mass. (October 29-November 2, 2004)
40. Poster 1253. Bifano M., Yan J., Xie J., et al. Lack of a pharmacokinetic interaction when entecavir is co-administered with lamivudine, adefovir, or tenofovir. Presented at: 40th Annual Meeting of the European Association for the Study of the Liver. Paris, France (April 13-17, 2005)
41. Abstract 86. Yan J., Bifano M., Nichola P., et al. Entecavir pharmacokinetics after multiple doses in healthy subjects. J Clin Pharmacol 42 Suppl 1 (2002) 1070
42. Poster 537. Yan J., Bifano M., Xie J., et al. Effects of renal impairment on single-dose pharmacokinetics of entecavir. Presented at: 40th Annual Meeting of the European Association for the Study of the Liver. Paris, France (April 13-17, 2005)
43. Abstract 43. Yan J., Bifano M., Xie J., et al. Effect of age and gender on single-dose pharmacokinetics of entecavir in healthy subjects. Antivir Ther. 9 (2004) H23
44. Abstract PI-45. LaCreta F., Mould D., Bifano M., and Grasela D. Simulation-based support of dose recommendations of entecavir for renally impaired subjects. Clin Pharmacol Ther. 77 (2005) P20
45. de Man R., Wolters L., Nevens F., et al. Safety and efficacy of oral entecavir given for 28 days in patients with chronic hepatitis B virus infection. Hepatology 34 (2001) 578-582
46. Abstract 1152. Yao G., Xu D., and Wang B. A phase II study in China of the safety and antiviral activity of entecavir in adults with chronic hepatitis B infection. Hepatology 38 Suppl 1 (2003) 711A
47. Lai C., Rosmawati M., Lao J., et al. Entecavir is superior to lamivudine in reducing hepatitis B virus DNA in patients with chronic hepatitis B infection. Gastroenterology 123 (2002) 1831-1838
48. Chang T., Gish R., Hadziyannis S., et al., the BEHoLD Study Group. A dose-ranging study of the efficacy and tolerability of entecavir in lamivudine-refractory chronic hepatitis B patients. Gastroenterology 129 (2005) 1198-1209
49. Abstract 1170. Yao G., Zhou X., Xu D., et al. A randomized, placebo-controlled study (ETV-56) in China of the efficacy and safety of entecavir in chronic hepatitis B patients who have failed lamivudine. Hepatology 40 Suppl 1 (2004) 674A
50. Abstract 70. Chang T., Gish R., de Man R., et al. Entecavir is superior to lamivudine for the treatment of HBeAG+ chronic hepatitis B: Results of Phase III study ETV-022 in nucleoside-naive patients. Hepatology 40 Suppl 1 (2004) 193A
51. Poster HB38. Lai C., Chang T., Chao Y., et al. Entecavir demonstrates superior histologic and virologic efficacy over lamivudine in nucleoside-naive HBeAg(-) chronic hepatitis B: Results of Phase III study ETV-027. Presented at: 14th Biennial Conference of the Asian Pacific Association for the Study of the Liver. New Delhi, India (December 11-15, 2004)
52. Poster 490. Gish R., de Man R., Pedersen C., et al. Sustained response off-treatment to entecavir and lamivudine after 48 weeks of treatment in nucleoside-naive, HBeAg(+) patients: 24-Week follow-up results of phase 3 study ETV-022. Presented at: 40th Annual Meeting of the European Association for the Study of the Liver. Paris, France (April 13-17, 2005)
53. Abstract 540. Yurdaydin C., Gish R., Chang T., et al. Alanine aminotransferase (ALT) flares are uncommon both on and post-treatment in entecavir treated HBeAg(+) patients. J Hepatol 42 Suppl 2 (2005) 196
54. Abstract 1136. Rosmawati M., Schiff E., Parana R., et al. Entecavir is superior to lamivudine at reducing HBV DNA in patients with chronic hepatitis B regardless of baseline alanine aminotransferase levels. Hepatology 40 Suppl 1 (2004) 656A
55. Lai C., Chang T., Chao Y., et al. Sustained response off-treatment to entecavir and lamivudine in nucleoside-naive, HBeAg-negative patients: 24-Week follow-up results of phase 3 study-027. Presented at: 15th Biennial Conference of the Asian Pacific Association for the Study of the Liver. Bali, Indonesia (August 18-21, 2005)
56. Available at. Comparative trial of entecavir versus adefovir in the treatment of chronic hepatitis B infection. Accessed September 5, 2005. http://www.clinicaltrials.gov/ct/show/NCT00096785
57. Available at. Comparison of entecavir to adefovir in chronic hepatitis B virus (HBV) patients with hepatic decomposition. Accessed September 9, 2005. http://www.clinicaltrials.gov/ct/show/NCT00065507
58. Abstract 123. Available at. Pessoa W., Gazzard B., Huang A., et al. Entecavir in HIV/HBV-co-infected patients: Safety and efficacy in a Phase II study (ETV-038). Presented at: 12th Conference on Retroviruses and Opportunistic Infection. Boston, Mass. (February 22-25, 2005). http://www.retroconference.org/Search_Abstract_2005/default.aspx
59. Abstract 433. Shakil A., Lilly L., Angus P., et al. Entecavir significantly reduces viral load in liver transplant recipients failing lamivudine therapy for chronic hepatitis B infection. J Hepatol 36 Suppl 1 (2002) 122
60. Poster 2020. Sollano J., Schiff E., Carrilho F., et al. Entecavir is well-tolerated for the treatment of HBeAg-positive chronic hepatitis B: Phase III safety analysis in nucleoside-naive and lamivudine-refractory patients. Presented at: 55th Annual Meeting of the American Association for the Study of Liver Diseases. Boston, Mass. (October 29-November 2, 2004)
61. Abstract 511. Manns M., Raptopoulou-Gigi M., Sollano J., et al. Entecavir is well tolerated for the treatment of nucleoside-naive and lamivudine-refractory chronic hepatitis B: Phase II/III safety results. J Hepatol 42 Suppl 2 (2005) 185
62. Gerschenson M., and Brinkman K. Mitochondrial dysfunction in AIDS and its treatment. Mitochondrion 4 (2004) 763-777
63. Entecavir (baraclude) for chronic hepatitis B. Med Lett Drugs Ther 47 (2005) 47-48