Entecavir: A review of its use in the treatment of chronic hepatitis B in patients with decompensated liver disease

Drugs

Volumn 71, Issue 18, 2011, Pages 2511-2529

  Keating, Gillian M ^a   Buti, M ^b   Gadano, A ^c   Kao, J H ^d   Lee, C M ^e   Peng, C Y ^f   Schiff, E R ^g   Tanwandee, T ^h  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

^b INSTITUTO DE SALUD CARLOS III   (Spain)

^c HOSPITAL ITALIANO DE BUENOS AIRES   (Argentina)

^d NATIONAL TAIWAN UNIVERSITY HOSPITAL   (Taiwan)

^e CHANG GUNG MEMORIAL HOSPITAL   (Taiwan)

^f CHINA MEDICAL UNIVERSITY HOSPITAL   (Taiwan)

^g UNIVERSITY OF MIAMI MILLER SCHOOL OF MEDICINE   (United States)

^h MAHIDOL UNIVERSITY   (Thailand)

Author keywords

Adis Drug Evaluations; Entecavir; Hepatitis B

Indexed keywords

ADEFOVIR DIPIVOXIL; CREATININE; DNA POLYMERASE; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ENTECAVIR; LAMIVUDINE; PEGINTERFERON ALPHA; TELBIVUDINE; TENOFOVIR DISOPROXIL;

ABDOMINAL DISTENSION; ABDOMINAL PAIN; ALLERGIC REACTION; AMYLASE BLOOD LEVEL; ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ASCITES; ASTHENIA; CHRONIC HEPATITIS; CREATINE KINASE BLOOD LEVEL; CREATININE BLOOD LEVEL; DECOMPENSATED LIVER CIRRHOSIS; DIZZINESS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG DOSE REDUCTION; DRUG EXCRETION; DRUG FATALITY; DRUG METABOLISM; DRUG TOLERABILITY; FEVER; GLUCOSE URINE LEVEL; GYNECOMASTIA; HEPATIC ENCEPHALOPATHY; HEPATITIS B; HEPATORENAL SYNDROME; HERPES SIMPLEX VIRUS; HUMAN; HYPERAMYLASEMIA; HYPERSENSITIVITY; INFLUENZA VIRUS; LACTIC ACIDOSIS; LIVER CELL CARCINOMA; LIVER FAILURE; MYALGIA; NAUSEA; NAUSEA AND VOMITING; PERIPHERAL EDEMA; PRURITUS; RASH; REVIEW; SIDE EFFECT; TRIACYLGLYCEROL LIPASE BLOOD LEVEL; UPPER RESPIRATORY TRACT INFECTION; VARICELLA ZOSTER VIRUS;

EID: 82955172930     PISSN: 00126667     EISSN: 11791950     Source Type: Journal    
DOI: 10.2165/11208510-000000000-00000     Document Type: Review

References (76)

1. Liaw Y-F, Brunetto MR, Hadziyannis S. The natural history of chronic HBV infection and geographical differences. Antivir Ther 2010; 15 Suppl. 3: 25-33
2. McMahon BJ. The natural history of chronic hepatitis B virus infection.Hepatology 2009 May; 49 (5 Suppl.): S45-55
3. Liaw Y-F, Leung N, Kao J-H, et al. Asian-Pacific consensus statement on the management of chronic hepatitis B: a 2008 update. Hepatol Int 2008 Sep; 2 (3): 263-83
4. Sorrell MF, Belongia EA, Costa J, et al. National Institutes of Health consensus development conference statement: management of hepatitis B. Hepatology 2009 May; 49 (5 Suppl.): S4-12
5. European Association for the Study of the Liver Clinical Practice Guidelines Panel. EASL clinical practice guidelines: management of chronic hepatitis B. J Hepatol 2009 Feb; 50 (2): 227-42
6. Lok ASF, McMahon BJ. Chronic hepatitis B: update 2009 [online]. Available from URL: http://www.aasld.org/practi ceguidelines/Documents/ Bookmarked%20Practice%20Gui delines/Chronic-Hep-B-Update-2009%208-24-2009.pdf [Accessed 2011 Sep 5]
7. Lai C-L, Shouval D, Lok AS, et al. Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. N Engl J Med 2006 Mar 9; 354 (10): 1011-20 (Pubitemid 43357805)
8. Chang T-T, Gish RG, de Man R, et al. A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. N Engl J Med 2006 Mar 9; 354 (10): 1001-10 (Pubitemid 43357804)
9. Yao G, Chen C, LuW, et al. Efficacy and safety of entecavir compared to lamivudine in nucleoside-na?̈ve patients with chronic hepatitis B: a randomized double-blind trial in China. Hepatol Int 2007 Sep; 1 (3): 365-72
10. Sherman M, Yurdaydin C, Sollano J, et al. Entecavir for treatment of lamivudine-refractory, HBeAg-positive chronic hepatitis B. Gastroenterology 2006 Jun; 130 (7): 2039-49 (Pubitemid 43816960)
11. Suzuki F, Toyoda J, Katano Y, et al. Efficacy and safety of entecavir in lamivudine-refractory patients with chronic hepatitis B: randomized controlled trial in Japanese patients. J Gastroenterol Hepatol 2008 Sep; 23 (9): 1320-6
12. Chang T-T, Gish RG, Hadziyannis SJ, et al. A dose-ranging study of the efficacy and tolerability of entecavir in lamivudine-refractory chronic hepatitis B patients. Gastroenterology 2005 Oct; 129 (4): 1198-209 (Pubitemid 41446860)
13. Chang T-T, Lai C-L, Kew Yoon S, et al. Entecavir treatment for up to 5 years in patients with hepatitis B e antigen-positive chronic hepatitis B. Hepatology 2010 Feb; 51 (2): 422-30
14. Schiff E, Simsek H, Lee WM, et al. Efficacy and safety of entecavir in patients with chronic hepatitis B and advanced hepatic fibrosis or cirrhosis. Am J Gastroenterol 2008 Nov; 103 (11): 2776-83
15. Schiff ER, Lee SS, Chao Y-C, et al. Long-term treatment with entecavir induces reversal of advanced fibrosis or cirrhosis in patients with chronic hepatitis B. Clin Gastroenterol Hepatol 2011 Mar; 9 (3): 274-6
16. Bristol-Myers Squibb. Baraclude(entecavir): US prescribing information [online]. Available from URL: http://packageinserts.bms.com/pi/pi-baraclude.pdf [Accessed 2011 Aug 26]
17. European Medicines Agency. Baraclude (entecavir): EU summary of product characteristics [online]. Available from URL: http://www.ema.europa.eu/docs/ enGB/docu ment-library/EPAR---Product-Information/human/0006 23/WC500051984.pdf [Accessed 2011 Aug 26]
18. Innaimo SF, Seifer M, Bisacchi GS, et al. Identification of BMS-200475 as a potent and selective inhibitor of hepatitis B virus. Antimicrob Agents Chemother 1997 Jul; 41 (7): 1444-8 (Pubitemid 27289665)
19. Langley DR, Walsh AW, Baldick CJ, et al. Inhibition of hepatitis B virus polymerase by entecavir. J Virol 2007 Apr; 81 (8): 3992-4001 (Pubitemid 46586894)
20. Tchesnokov EP, Obikhod A, Schinazi RF, et al. Delayed chain-termination protects the anti-HBV drug entecavir from excision by HIV-1 reverse transcriptase. J Biol Chem 2008 Dec 5; 283 (49): 34218-28
21. Mazzucco CE, Hamatake RK, Colonno RJ, et al. Entecavir for treatment of hepatitis B virus displays no in vitro mitochondrial toxicity or DNA polymerase gamma inhibition. Antimicrob Agents Chemother 2008 Feb; 52 (2): 598-605 (Pubitemid 351170833)
22. Baldick CJ, Eggers BJ, Fang J, et al. Hepatitis B virus quasispecies susceptibility to entecavir confirms the relationship between genotypic resistance and patient virologic response. J Hepatol 2008 Jun; 48 (6): 895-902
23. Suh DJ, Um SH, Herrmann E, et al. Early viral kinetics of telbivudine and entecavir: results of a 12-week randomized exploratory study with patients with HBeAg-positive chronic hepatitis B. Antimicrob Agents Chemother 2010 Mar; 54 (3): 1242-7
24. Wolters LMM, Hansen BE, Niesters HGM, et al. Viral dynamics during and after entecavir therapy in patients with chronic hepatitis B. J Hepatol 2002 Jul; 37 (1): 137-44 (Pubitemid 34713065)
25. McMahon MA, Jilek BL, Brennan TP, et al. The HBV drug entecavir: effects on HIV-1 replication and resistance. N Engl J Med 2007 Jun 21; 356 (25): 2614-21 (Pubitemid 46961006)
26. Jain MK, Zoellner CL. Entecavir can select for M184 V of HIV-1: a case of an HIV/hepatitis B (HBV) naive patient treated for chronic HBV [letter]. AIDS 2007 Nov 12; 21 (17): 2365-6 (Pubitemid 350287474)
27. Jakobsen MR, Arildsen H, Krarup HB, et al. Entecavir therapy induces de novo HIV reverse-transcriptase M184 V mutation in an antiretroviral therapy-naive patient. Clin Infect Dis 2008 May 1; 46 (9): e88-91 (Pubitemid 351589966)
28. Castel H, Bocket L, Tamalet C, et al. Entecavir monotherapy selects M184V mutation in lamivudine-naive and lamivudine experienced HIV-HBV co-infected patients [abstract no. 938]. Hepatology 2008 Oct; 48 (4 Suppl.): 728
29. Tenney DJ, Rose RE, Baldick CJ, et al. Long-term monitoring shows hepatitis B virus resistance to entecavir in nucleoside-naïve patients is rare through 5 years of therapy. Hepatology 2009 May; 49 (5): 1503-14
30. Tenney DJ, Pokornowski KA, Rose RE, et al. Entecavir maintains a high genetic barrier to HBV resistance through 6 years in naive patients [abstract no. 20]. J Hepatol 2009 Apr; 50 Suppl. 1: S10
31. Colonno RJ, Rose R, Baldick CJ, et al. Entecavir resistance is rare in nucleoside naive patients with hepatitis B. Hepatology 2006 Dec; 44 (6): 1656-65 (Pubitemid 44953670)
32. YuenM-F, SetoW-K, Fung J, et al. Three years of continuous entecavir therapy in treatment-naïve chronic hepatitis B patients: viral suppression, viral resistance, and clinical safety. Am J Gastroenterol 2011 Jul; 106 (7): 1264-71
33. Baldick CJ, Tenney DJ,Mazzucco CE, et al. Comprehensive evaluation of hepatitis B virus reverse transcriptase substitutions associated with entecavir resistance. Hepatology 2008 May; 47 (5): 1473-82
34. Tenney DJ. Genotypic determinants and phenotypic properties of antiviral-resistant HBV variants: insight from entecavir resistance studies. Antivir Ther 2010; 15 (3 Pt B): 529-35
35. Walsh AW, Langley DR, Colonno RJ, et al. Mechanistic characterization and molecular modeling of hepatitis B virus polymerase resistance to entecavir. PLoS One 2010 Feb; 5 (2): e9195
36. Tenney DJ, Rose RE, Baldick CJ, et al. Two-year assessment of entecavir resistance in lamivudine-refractory hepatitis B virus patients reveals different clinical outcomes depending on the resistance substitutions present. Antimicrob Agents Chemother 2007 Mar; 51 (3): 902-11 (Pubitemid 46355274)
37. Jardi R, Rodriguez-Frias F, Tabernero D, et al. Use of the novel INNO-LiPA line probe assay for detection of hepatitis B virus variants that confer resistance to entecavir therapy. J Clin Microbiol 2009 Feb; 47 (2): 485-8
38. Guo J-J, Li Q-L, Shi X-F, et al. Dynamics of hepatitis B virus resistance to entecavir in a nucleoside/nucleotidenai ̈ve patient. Antiviral Res 2009 Feb; 81 (2): 180-3
39. Liaw Y-F, Raptopoulou-Gigi M, Cheinquer H, et al. Efficacy and safety of entecavir versus adefovir in chronic hepatitis B patients with hepatic decompensation: a randomized, open-label study. Hepatology 2011 Jul; 54 (1): 91-100
40. Liaw Y-F, Sheen I-S, Lee C-M, et al. Tenofovir disoproxil fumarate (TDF), emtricitabine/TDF, and entecavir in patients with decompensated chronic hepatitis B liver disease. Hepatology 2011 Jan; 53 (1): 62-72
41. Mukaide M, Tanaka Y, Shin-I T, et al. Mechanism of entecavir resistance of hepatitis B virus with viral breakthrough as determined by long-term clinical assessment and molecular docking simulation. Antimicrob Agents Chemother 2010 Feb; 54 (2): 882-9
42. Yan J-H, Bifano M, Olsen S, et al. Entecavir pharmacokinetics, safety, and tolerability after multiple ascending doses in healthy subjects. J Clin Pharmacol 2006 Nov; 46 (11): 1250-8 (Pubitemid 44564354)
43. Yoshitsugu H, Sakurai T, Ishikawa H, et al. Pooled modelbased approach to compare the pharmacokinetics of entecavir between Japanese and non-Japanese chronic hepatitis B patients. Diagn Microbiol Infect Dis 2011; 70 (1): 91-100
44. Zhu M, Bifano M, Xu X, et al. Lack of an effect of human immunodeficiency virus coinfection on the pharmacokinetics of entecavir in hepatitis B virus-infected patients. Antimicrob Agents Chemother 2008 Aug; 52 (8): 2836-41
45. Bifano M, Yan J-H, Smith RA, et al. Absence of a pharmacokinetic interaction between entecavir and adefovir. J Clin Pharmacol 2007 Oct; 47 (10): 1327-34 (Pubitemid 47459664)
46. Cheinquer H, Raptopoulou-Gigi M, Sarin SK, et al. Efficacy and safety of entecavir versus adefovir in chronic hepatitis B patients with evidence of hepatic decompensation: week 96 results [poster]. 21st Conference of the Asian Pacific Association for the Study of the Liver; 2011 Feb 17-20; Bangkok
47. Shim JH, Lee HC, Kim KM, et al. Efficacy of entecavir in treatment-naïve patients with hepatitis B virus-related decompensated cirrhosis. J Hepatol 2010 Feb; 52 (2): 176-82
48. Liaw Y-F, Raptopoulou-Gigi M, Cheinquer H, et al. Risk and predictors of mortality or hepatocellular carcinoma among entecavir-or adefovir-treated chronic hepatitis B patients with evidence of hepatic decompensation [abstract no. 1011]. J Hepatol 2010 Apr; 52 Suppl. 1: S390-391
49. GlaxoSmithKline. Epivir-HBV (lamivudine): US prescribing information [online]. Available from URL: http://www. accessdata.fda.gov/drugsatfda docs/label/2011/021003s013, 021004s013lbl.pdf [Accessed 2011 Sep 5]
50. Gilead Sciences, Inc.Viread (tenofovir disoproxil fumarate) tablets: US prescribing information [online]. Available from URL: http://www.accessdata.fda. gov/drugsatfda docs/lab el/2010/021356s035lbl.pdf [Accessed 2011 Sep 5]
51. Novartis. Tyzeka (telbivudine): US prescribing information [online]. Available from URL: http://www.pharma.us.no vartis.com/product/pi/pdf/tyzeka.pdf [Accessed 2011 Sep 5]
52. Gilead Sciences, Inc. Hepsera (adefovir dipivoxil) tablets: US prescribing information [online]. Available from URL: http://www.accessdata.fda. gov/drugsatfda docs/label/2009/021449s016lbl.pdf [Accessed 2011 Sep 5]
53. European Medicines Agency. Sebivo (telbivudine): EU summary of product characteristics [online]. Available from URL: http://www.ema.europa.eu/docs/ enGB/document-library/EPAR---Product-Information/human/000713/WC 500049337.pdf [Accessed 2011 Sep 5]
54. European Medicines Agency. Viread (tenofovir disoproxil fumarate): EU summary of product characteristics [online]. Available from URL: http://www.ema.europa.eu/docs/enGB/document-library/EPAR---Product-Information/ hu man/000419/WC500051737.pdf [Accessed 2011 Sep 5]
55. European Medicines Agency. Hepsera (adefovir dipivoxil): EU summary of product characteristics [online]. Available from URL: http://www.ema.europa.eu/ docs/enGB/docu ment-library/EPAR---Product-Information/human/0004 85/WC500048079.pdf [Accessed 2011 Sep 5]
56. European Medicines Agency. Zeffix (lamivudine): EU summary of product characteristics [online]. Available from URL: http://www.ema.europa.eu/docs/ enGB/document-library/EPAR---Product-Information/human/000242/WC 500048387.pdf [Accessed 2011 Sep 5]
57. Lange CM, Bojunga J, Hofmann WP, et al. Severe lactic acidosis during treatment of chronic hepatitis B with entecavir in patients with impaired liver function. Hepatology 2009 Dec; 50 (6): 2001-6
58. Lange CM, Sprinzl K, Vermehren J, et al. Prospective observation of lactate values during treatment of chronic hepatitis B with nucleos(t)ide analogues in patients with decompensated liver disease [abstract plus poster]. 116th Congress of theGerman Society of Internal Medicine; 2010 Apr 9-14; Wiesbaden
59. Marzano A, Marengo A, Marietti M, et al. Lactic acidosis during entecavir treatment in decompensated hepatitis B virus-related cirrhosis [letter]. Dig Liver Dis. Epub 2011 Jul 20
60. Yuen M-F, Lai CL. Treatment of chronic hepatitis B: evolution over two decades. JGastroenterol Hepatol 2011 Jan; 26 Suppl. 1: 138-43
61. Keeffe EB, Dieterich DT, Han S-H, et al. A treatment algorithm for the management of chronic hepatitis B virus infection in the United States: 2008 update. Clin Gastroenterol Hepatol 2008 Dec; 6 (12): 1315-41
62. Dienstag JL. Drug therapy: hepatitis B virus infection. New Eng J Med 2008 Oct 2; 359 (14): 1486-500
63. Dienstag JL. Benefits and risks of nucleoside analog therapy for hepatitis B. Hepatology 2009May; 49 (5 Suppl.): S112-121
64. Fontana RJ. Side effects of long-term oral antiviral therapy for hepatitis B. Hepatology 2009 May; 49 (5 Suppl.): S185-195
65. Shin SR, Yoo BC, Choi MS, et al. A comparison of 48-week treatment efficacy between clevudine and entecavir in treatment-naïve patients with chronic hepatitis B. Hepatol Int 2011; 5 (2): 664-70
66. Gilead Sciences, Inc. Truvada (emtricitabine/tenofovir disoproxil fumarate) tablets: US prescribing information [online]. Available from URL: http://www.accessdata. fda.gov/drugsatfda docs/label/2011/021752s027lbl.pdf [Accessed 2011 Sep 6]
67. European Medicines Agency. Truvada (emtricitabine/tenofovir disoproxil fumarate): EU summary of product characteristics [online]. Available from URL: http://www. ema.europa.eu/docs/enGB/document-library/EPAR---Product-Information/ human/000594/WC500043718.pdf [Accessed 2011 Sep 6]
68. Pellicelli AM, Barbaro G, Barbarini G, et al. Efficacy of entecavir as rescue therapy in lamivudine-resistant patients with HBV liver cirrhosis and waiting for orthotopic liver transplantation [abstract no. 885]. Hepatology 2008; 48 (4 Suppl.): 701-702A
69. Pellicelli AM, Barbarini G, Romano M, et al. Entecavir therapy for lamivudine resistant HBV cirrhotic patients waiting for OLT: viral and biochemical outcomes at one year [abstract no. 441]. Hepatology 2009 Oct; 50 (4 Suppl.): 514A
70. Fontana RJ. Entecavir in decompensated HBV cirrhosis: the future is looking brighter. JHepatol 2010 Feb; 52 (2): 147-9
71. Asan Medical Center. Lactic acidosis during entecavir (ETV) treatment [ClinicalTrials.gov identifierNCT01354652]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://www.clinicaltrials.gov [Accessed 2011 Oct 17]
72. Bristol-Myers Squibb. US commitment studies [online]. Available from URL: http://www.bms.com/clinical-trials/pmc/Pages/US-Commitment-Studies.aspx [Accessed 2011 Oct 17]
73. Wong VW-S, Wong GL-H, Yiu KK-L, et al. Entecavir treatment in patients with severe acute exacerbation of chronic hepatitis B. J Hepatol 2011 Feb; 54 (2): 236-42
74. Chen T, He Y, Liu X, et al. Nucleoside analogues improve the short-term and long-term prognosis of patients with hepatitis B virus-related acute-on-chronic liver failure. Clin Exp Med. Epub 2011 Oct 15
75. Peters MG. Special populations with hepatitis B virus infection. Hepatology 2009 May; 49 (5 Suppl.): S146-155
76. Amarapurkar D. Efficacy of combination of entecavir and tenofovir treatment in hepatitis B related decompensated chronic liver disease: pilot study [abstract no. 901]. J Hepatol 2009 Apr; 50 Suppl. 1: S327