Adefovir dipivoxil in chronic hepatitis B: History and current uses

Expert Opinion on Pharmacotherapy

Volumn 13, Issue 2, 2012, Pages 245-254

  Segovia, Maria C ^a   Chacra, Wadih ^a   Gordon, Stuart C ^a,b  

^a HENRY FORD HEALTH SYSTEM   (United States)

^b WAYNE STATE UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

Adefovir dipivoxil; Antiviral resistance; Hepatitis B virus; Lamivudine

Indexed keywords

ADEFOVIR; ADEFOVIR DIPIVOXIL; ALPHA INTERFERON; CLEVUDINE; EMTRICITABINE; ENTECAVIR; LAMIVUDINE; PEGINTERFERON ALPHA2A; PEGINTERFERON ALPHA2B; PLACEBO; TELBIVUDINE; TENOFOVIR; TENOFOVIR DISOPROXIL;

ABDOMINAL DISCOMFORT; ACUTE PANCREATITIS; ADD ON THERAPY; ANTIVIRAL RESISTANCE; ANTIVIRAL THERAPY; CHRONIC HEPATITIS; DRUG ABSORPTION; DRUG CLEARANCE; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG SUBSTITUTION; DRUG TOLERABILITY; DRUG USE; DRUG WITHDRAWAL; FANCONI RENOTUBULAR SYNDROME; HEADACHE; HEPATITIS B; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; HYPOPHOSPHATEMIC RICKETS; KIDNEY FAILURE; LACTIC ACIDOSIS; LIVER TRANSPLANTATION; MIXED INFECTION; MYOPATHY; NEPHROTOXICITY; PHASE 3 CLINICAL TRIAL (TOPIC); RECOMMENDED DRUG DOSE; REVIEW; THROMBOCYTOPENIA; UNSPECIFIED SIDE EFFECT; VIRUS LOAD; WEAKNESS;

ADENINE; ANTIVIRAL AGENTS; DNA-DIRECTED DNA POLYMERASE; HEPATITIS B, CHRONIC; HUMANS; PHOSPHONIC ACIDS;

EID: 84855882090     PISSN: 14656566     EISSN: 17447666     Source Type: Journal    
DOI: 10.1517/14656566.2012.649727     Document Type: Review

References (90)

1. Lok ASF, McMahon BJ. Chronic hepatitis B: update 2009. Hepatology 2009;50:661-2
2. Centers for Disease Control and Prevention. Hepatitis B Information for Health Professionals. Available from: http://www.cdc.gov/hepatitis/HBV/HBVfaq. htm#overview [Last accessed 26 August 2011]
3. EASL Clinical Practice Guidelines: management of chronic hepatitis B. European Association for the Study of the Liver. J Hepatol 2009;50(2):227-42
4. 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;2:263-83
5. Jafri S-MR, Lok AS-F. Antiviral therapy for chronic hepatitis B. Clin Liver Dis 2010;14:425-38
6. Yoo BC, Kim JH, Chung Y-H, et al. Twenty-four-week clevudine therapy showed potent and sustained antiviral activity in HBeAg-positive chronic hepatitis B. Hepatology 2007;45:1172-8 (Pubitemid 46775779)
7. Yoo BC, Kim JH, Kim T-H, et al. Clevudine is highly efficacious in hepatitis B e antigen-negative chronic hepatitis B with durable off-therapy viral suppression. Hepatology 2007;46:1041-8 (Pubitemid 350144769)
8. Yoon EL, Yim HJ, Lee HJ, et al. Comparison of clevudine and entecavir for treatment-naive patients with chronic hepatitis B virus infection: two year follow-up data. J Clin Gastroenterol 2011;45:893-9. Available from: http://www.ncbi.nlm.nih.gov/pubmed/21617542 [Last accessed 25 August 2011]
9. Shin SR, Yoo BC, Choi MS, et al. A comparison of 48-week treatment efficacy between clevudine and entecavir in treatment-naive patients with chronic hepatitis B. Hepatol Int 2011;5:664-70
10. Gilead Sciences. Highlights of prescribing information for hepsera (adefovir dipivoxil). Available from: www.gilead. com/pdf/hepsera-pi.pdf [Last accessed 26 August 2011]
11. Kahn J, Lagakos S, Wulfsohn M, et al. Efficacy and safety of adefovir dipivoxil with antiretroviral therapy: a randomized controlled trial. JAMA 1999;282:2305-12 (Pubitemid 30013061)
12. Mellors JW. Adefovir for the treatment of HIV infection: if not now, when? JAMA 1999;282:2355-6 (Pubitemid 30013069)
13. Gilead Sciences. Gilead Sciences announces termination of its U.S. development program for adefovir dipivoxil for HIV. Available from: http://www.gilead.com/pr-944254502 [Last accessed 26 August 2011]
14. Ray AS, Vela JE, Olson L, et al. Effective metabolism and long intracellular half life of the anti-hepatitis B agent adefovir in hepatic cells. Biochem Pharmacol 2004;68:1825-31 (Pubitemid 39278505)
15. Marcellin P, Chang T-T, Lim SG, et al. Adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. N Engl J Med 2003;348:808-16 (Pubitemid 36245757)
16. Marcellin P, Chang T-T, Lim SGL, et al. Long-term efficacy and safety of adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. Hepatology 2008;48:750-8
17. Hadziyannis SJ, Tassopoulos NC, Heathcote EJ, et al. Adefovir dipivoxil for the treatment of hepatitis B e antigen-negative chronic hepatitis B. Engl J Med 2003;348:800-7 (Pubitemid 36245756)
18. Westland C, Delaney W IV, Yang H, et al. Hepatitis B virus genotypes and virologic response in 694 patients in phase III studies of adefovir dipivoxil1. Gastroenterology 2003;125:107-16 (Pubitemid 36799112)
19. Perrillo R, Schiff E, Yoshida E, et al. Adefovir dipivoxil for the treatment of lamivudine-resistant hepatitis B mutants. Hepatology 2000;32:129-34 (Pubitemid 30432377)
20. Perrillo R, Hann H-W, Mutimer D, et al. Adefovir dipivoxil added to ongoing lamivudine in chronic hepatitis B with YMDD mutant hepatitis B virus. Gastroenterology 2004;126:81-90 (Pubitemid 38040726)
21. Peters MG, Hann H, Martin P, et al. Adefovir dipivoxil alone or in combination with lamivudine in patients with lamivudine-resistant chronic hepatitis B. Gastroenterology 2004;126:91-101 (Pubitemid 38040727)
22. Rapti I, Dimou E, Mitsoula P, et al. Adding-on versus switching-to adefovir therapy in lamivudine-resistant HBeAg-negative chronic hepatitis B. Hepatology 2007;45:307-13 (Pubitemid 46374587)
23. Vassiliadis TG, Giouleme O, Koumerkeridis G, et al. Adefovir plus lamivudine are more effective than adefovir alone in lamivudine-resistant HBeAg- chronic hepatitis B patients: a 4-year study. J Gastroenterol Hepatol 2010;25:54-60
24. Lee JM, Park JY, Kim DY, et al. Long-term adefovir dipivoxil monotherapy for up to 5 years in lamivudine-resistant chronic hepatitis B. Antivir Ther (Lond) 2010;15:235-41
25. Chung GE, Kim W, Lee KL, et al. Add-on adefovir is superior to a switch to entecavir as rescue therapy for Lamivudine-resistant chronic hepatitis B. Dig Dis Sci 2011;56:2130-6
26. Westland CE, Yang H, Delaney WE IV, et al. Week 48 resistance surveillance in two phase III clinical studies of adefovir dipivoxil for chronic hepatitis B. Hepatology 2003;38:96-103 (Pubitemid 36775800)
27. Lee Y-S, Suh DJ, Lim Y-S, et al. Increased risk of adefovir resistance in patients with lamivudine-resistant chronic hepatitis B after 48 weeks of adefovir dipivoxil monotherapy. Hepatology 2006;43:1385-91 (Pubitemid 43980117)
28. Yeon JE, Yoo W, Hong SP, et al. Resistance to adefovir dipivoxil in lamivudine resistant chronic hepatitis B patients treated with adefovir dipivoxil. Gut 2006;55:1488-95 (Pubitemid 44476796)
29. Fung SK, Chae HB, Fontana RJ, et al. Virologic response and resistance to adefovir in patients with chronic hepatitis B. J Hepatol 2006;44:283-90 (Pubitemid 43069209)
30. Chen C-H, Wang J-H, Lu S-N, et al. Characteristics of adefovir resistance in patients with or without lamivudine-resistant hepatitis B virus treated with adefovir: a 4-year experience. Liver Int 2011;31:206-14
31. Tan J, Degertekin B, Wong SN, et al. Tenofovir monotherapy is effective in hepatitis B patients with antiviral treatment failure to adefovir in the absence of adefovir-resistant mutations. J Hepatol 2008;48:391-8
32. Berg T, Marcellin P, Zoulim F, et al. Tenofovir is effective alone or with emtricitabine in adefovir-treated patients with chronic-hepatitis B virus infection. Gastroenterology 2010;139:1207-17
33. van Bommel F, de Man RA, Wedemeyer H, et al. Long-term efficacy of tenofovir monotherapy for hepatitis B virus-monoinfected patients after failure of nucleoside/nucleotide analogues. Hepatology 2010;51:73-80
34. Hadziyannis SJ, Tassopoulos NC, Heathcote EJ, et al. Long-term therapy with adefovir dipivoxil for HBeAg-negative chronic hepatitis B for up to 5 years. Gastroenterology 2006;131:1743-51 (Pubitemid 44958517)
35. Hui C-K, Zhang H-Y, Bowden S, et al. 96 weeks combination of adefovir dipivoxil plus emtricitabine vs. adefovir dipivoxil monotherapy in the treatment of chronic hepatitis B. J Hepatol 2008;48:714-20
36. Wursthorn K, Lutgehetmann M, Dandri M, et al. Peginterferon alpha-2b plus adefovir induce strong cccDNA decline and HBsAg reduction in patients with chronic hepatitis B. Hepatology 2006;44:675-84 (Pubitemid 44433724)
37. Lutgehetmann M, Volzt T, Quaas A, et al. Sequential combination therapy leads to biochemical and histological improvement despite low ongoing intrahepatic hepatitis B virus replication. Antivir Ther (Lond) 2008;13:57-66 (Pubitemid 351541674)
38. Moucari R, Boyer N, Ripault M-P, et al. Sequential therapy with adefovir dipivoxil and pegylated interferon alfa-2a for HBeAg-negative patients. J Viral Hepat 2011;18:580-6
39. Cao Z, Yu H, Ma L, et al. Peginterferon alfa-2a (40kD) plus adefovir for 96 weeks in HBeAg-negative CHB results in high rates of HBsAg clearance/seroconvesion. J Hepatol 2011;54(Suppl 1):S283
40. Cao Z, Zhang Y, Ma L, et al. Treatment of HBeAg-positive CHB infection with peginterferon alfa-2a [40kD] plus lamivudine or adefovir for 96 weeks results in high rates of HBsAg clearance/seroconversion. Hepatology 2010;52(Suppl S1):507A
41. Chen X, Cao Z, Liu Y, et al. A Potent HBsAg response to treatment of HBeAg-positive chronic hepatitis B with interferon alpha plus a nucleos(t)ide analogue. J Gastroenterol Hepatol 2011;Epub 2011 Nov 18. Available from: http://www.ncbi.nlm.nih.gov/pubmed/22098411 [Last accessed 28 November 2011]
42. Marcellin P, Heathcote EJ, Buti M, et al. Tenofovir disoproxil fumarate versus adefovir dipivoxil for chronic hepatitis B. N Engl J Med 2008;359:2442-55
43. Heathcote EJ, Marcellin P, Buti M, et al. Three-year efficacy and safety of tenofovir disoproxil fumarate treatment for chronic hepatitis B. Gastroenterology 2011;140:132-43
44. 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;54:91-100
45. Ryu HJ, Lee JM, Ahn SH, et al. Efficacy of adefovir add-on lamivudine rescue therapy compared with switching to entecavir monotherapy in patients with lamivudine-resistant chronic hepatitis B. J Med Virol 2010;82:1835-42
46. Sokal EM, Kelly D, Wirth S, et al. The pharmacokinetics and safety of adefovir dipivoxil in children and adolescents with chronic hepatitis B virus infection. J Clin Pharmacol 2008;48:512-17 (Pubitemid 351389107)
47. Jonas MM, Kelly D, Pollack H, et al. Safety, efficacy, and pharmacokinetics of adefovir dipivoxil in children and adolescents (age 2 to (Pubitemid 351945554)
48. Benhamou Y, Bochet M, Thibault V, et al. Safety and efficacy of adefovir dipivoxil in patients co-infected with HIV-1 and lamivudine-resistant hepatitis B virus: an open-label pilot study. Lancet 2001;358:718-23 (Pubitemid 32823401)
49. Benhamou Y, Thibault V, Vig P, et al. Safety and efficacy of adefovir dipivoxil in patients infected with lamivudine-resistant hepatitis B and HIV-1. J Hepatol 2006;44:62-7 (Pubitemid 41772517)
50. Hannon H, Bagnis CI, Benhamou Y, et al. The renal tolerance of low-dose adefovir dipivoxil by lamivudine-resistant individuals co-infected with hepatitis B and HIV. Nephrol Dial Transplant 2004;19:386-90 (Pubitemid 38195988)
51. Peters MG, Andersen J, Lynch P, et al. Randomized controlled study of tenofovir and adefovir in chronic hepatitis B virus and HIV infection: ACTG A5127. Hepatology 2006;44:1110-16 (Pubitemid 44748362)
52. Lacombe K, Gozlan J, Boyd A, et al. Comparison of the antiviral activity of adefovir and tenofovir on hepatitis B virus in HIV-HBV-coinfected patients. Antivir Ther (Lond) 2008;13:705-13
53. Ingiliz P, Valantin M-A, Thibault V, et al. Efficacy and safety of adefovir dipivoxil plus pegylated interferon-alpha2a for the treatment of lamivudine-resistant hepatitis B virus infection in HIV-infected patients. Antivir Ther (Lond) 2008;13:895-900
54. Department of Health and Human Services Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Available from: www. aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf [Last accessed 26 August 2011]
55. Sheldon JA, Corral A, Rodes B, et al. Risk of selecting K65R in antiretroviral-naive HIV-infected 47. individuals with chronic hepatitis B treated with adefovir. AIDS 2005;19:2036-8 (Pubitemid 41669031)
56. Delaugerre C, Marcelin A-G, Thibault V, et al. Human immunodeficiency virus (HIV) type 1 reverse transcriptase resistance mutations in hepatitis B virus (HBV)- HIV-coinfected patients treated for HBV chronic infection once daily with 10 milligrams of adefovir dipivoxil combined with lamivudine. Antimicrob Agents Chemother 2002;46:1586-8 (Pubitemid 34415353)
57. Republique Francaise Ministere de la Sante, et des Sports. Rapport 2010 sous la direction du Pr. Patrick Yeni: Prise en charge medicale des personnes infectees par le VIH. 2010. Available from: http://www.sante.gouv.fr/rapport- 2010-sur-la- prise-en-charge-medicale-des-personnes- infectees-par-le-vih-sous- la-direction-du- pr-patrick-yeni.html [Last accessed 1 September 2011]
58. Seaberg EC, Belle SH, Beringer KC, et al. Liver transplantation in the United States from 1987 - 1998: updated results from the Pitt-UNOS Liver Transplant Registry. Clin Transpl 1998;17-37
59. Akyildiz M, Karasu Z, Zeytunlu M, et al. Adefovir dipivoxil therapy in liver transplant recipients for recurrence of hepatitis B virus infection despite lamivudine plus hepatitis B immunoglobulin prophylaxis. J Gastroenterol Hepatol 2007;22:2130-4 (Pubitemid 350145596)
60. Lok ASF, McMahon BJ. Chronic hepatitis B. Hepatology 2007;45:507-39 (Pubitemid 46374607)
61. Schiff E, Lai C-L, Hadziyannis S, et al. Adefovir dipivoxil for wait-listed and post-liver transplantation patients with lamivudine-resistant hepatitis B: final long-term results. Liver Transpl 2007;13:349-60 (Pubitemid 46444463)
62. Lo CM, Liu CL, Lau GK, et al. Liver transplantation for chronic hepatitis B with lamivudine-resistant YMDD mutant using add-on adefovir dipivoxil plus lamivudine. Liver Transpl 2005;11:807-13 (Pubitemid 40975583)
63. Osborn MK, Han SH, Regev A, et al. Outcomes of patients with hepatitis B who developed antiviral resistance while on the liver transplant waiting list. Clin Gastroenterol Hepatol 2007;5:1454-61 (Pubitemid 350181591)
64. Marzano A, Lampertico P, Mazzaferro V, et al. Prophylaxis of hepatitis B virus recurrence after liver transplantation in carriers of lamivudine-resistant mutants. Liver Transpl 2005;11:532-8 (Pubitemid 40704065)
65. Freshwater DA, Dudley T, Cane P, et al. Viral persistence after liver transplantation for hepatitis B virus: a cross-sectional study. Transplantation 2008;85:1105-11 (Pubitemid 351590187)
66. Angus PW, Patterson SJ, Strasser SI, et al. A randomized study of adefovir dipivoxil in place of HBIG in combination with lamivudine as post-liver transplantation hepatitis B prophylaxis. Hepatology 2008;48:1460-6
67. Neff GW, Kemmer N, Kaiser TE, et al. Combination therapy in liver transplant recipients with hepatitis B virus without hepatitis B immune globulin. Dig Dis Sci 2007;52:2497-500 (Pubitemid 47373893)
68. Nath DS, Kalis A, Nelson S, et al. Hepatitis B prophylaxis post-liver transplant without maintenance hepatitis B immunoglobulin therapy. Clin Transplant 2006;20:206-10
69. Katz LH, Tur-Kaspa R, Guy DG, Paul M. Lamivudine or adefovir dipivoxil alone or combined with immunoglobulin for preventing hepatitis B recurrence after liver transplantation. Cochrane Database Syst Rev 2010;7:CD006005
70. Gane E, Strasser S, Patterson S, et al. A prospective study on the safety and efficacy of lamivudine and adefovir dipivoxil prophylaxis in HBsAg positive liver transplantation candidates. Hepatology 2007;46(Suppl 1):479A
71. Yang Y, Zhang Q, Cai C-jie, et al. Prophylaxis of hepatitis B recurrence in post-liver transplantation patients with lamivudine-resistant YMDD mutant. Chin Med J 2007;120:1400-3 (Pubitemid 47364969)
72. Wai C-T, Prabhakaran K, Wee A, et al. Adefovir dipivoxil as the rescue therapy for lamivudine-resistant hepatitis B post liver transplant. Transplant Proc 2004;36:2313-14 (Pubitemid 39550829)
73. Herreros de Tejada Echanojauregui A, Moreno Planas JM, Rubio Gonzalez E, et al. Adefovir dipivoxil therapy in liver transplant recipients with lamivudine-resistant hepatitis B virus. Transplant Proc 2005;37:1507-8 (Pubitemid 40712101)
74. Limquiaco JL, Wong J, Wong VWS, et al. Lamivudine monoprophylaxis and adefovir salvage for liver transplantation in chronic hepatitis B: a seven-year follow-up study. J Med Virol 2009;81:224-9
75. Chan HL-Y, Chui AK-K, Lau W-Y, et al. Outcome of lamivudine resistant hepatitis B virus mutant post-liver transplantation on lamivudine monoprophylaxis. Clin Transplant 2004;18:295-300 (Pubitemid 38744854)
76. Hwang S, Ahn C-S, Song G-W, et al. Posttransplantation prophylaxis with primary high-dose hepatitis B immunoglobulin monotherapy and complementary preemptive antiviral add-on. Liver Transpl 2011;17:456-65
77. Fontana RJ. Side effects of long-term oral antiviral therapy for hepatitis B. Hepatology 2009;49(5 Suppl):S185-95
78. Spiegel PB. The effects of antiretroviral therapy on HIV prevalence in conflict situations: not yet there. AIDS 2009;23:541-2
79. Fisher EJ, Chaloner K, Cohn DL, et al. The safety and efficacy of adefovir dipivoxil in patients with advanced HIV disease: a randomized, placebo-controlled trial. AIDS 2001;15:1695-700 (Pubitemid 32918124)
80. Fontaine H, Vallet-Pichard A, Chaix M-L, et al. Efficacy and safety of adefovir dipivoxil in kidney recipients, hemodialysis patients, and patients with renal insufficiency. Transplantation 2005;80:1086-92 (Pubitemid 41611932)
81. Kamar N, Huart A, Tack I, et al. Renal side effects of adefovir in hepatitis B virus-(HBV) positive kidney allograft recipients. Clin Nephrol 2009;71:36-42
82. Ha NB, Ha NB, Garcia RT, et al. Renal dysfunction in chronic hepatitis B patients treated with adefovir dipivoxil. Hepatology 2009;50:727-34
83. Izzedine H, Hulot JS, Launay-Vacher V, et al. Renal safety of adefovir dipivoxil in patients with chronic hepatitis B: two double-blind, randomized, placebo-controlled studies. Kidney Int 2004;66:1153-8 (Pubitemid 39121022)
84. Cohen SM, Levy RM, Jovanovich JF, et al. Fatal lactic acidosis associated with the use of combination oral medications to treat reactivation of hepatitis B. J Clin Gastroenterol 2009;43:1008-10
85. Wong T, Girgis CM, Ngu MC, et al. Hypophosphatemic osteomalacia after low-dose adefovir dipivoxil therapy for hepatitis B. J Clin Endocrinol Metab 2010;95:479-80
86. Tamori A, Enomoto M, Kobayashi S, et al. Add-on combination therapy with adefovir dipivoxil induces renal impairment in patients with lamivudine-refractory hepatitis B virus. J Viral Hepat 2010;17:123-9
87. Stornaiuolo G, Amato A, Gaeta GB. Adefovir dipivoxil-associated thrombocytopenia in a patient with chronic hepatitis B. Dig Liver Dis 2006;38:211-12 (Pubitemid 44356171)
88. Weber A, Carbonnel F, Simon N, et al. Severe acute pancreatitis related to the use of adefovir in a liver transplant recipient. Gastroenterol Clin Biol 2008;32:247-9
89. Yuen M-F, Lai C-L. Adefovir dipivoxil in chronic hepatitis B infection. Expert Opin Pharmacother 2004;5:2361-7 (Pubitemid 39489988)
90. ClinicalTrials.gov. Study to evaluate the efficacy and safety of tenofovir disoproxil fumarate (TDF) in combination with peginterferon alfa-2a vs standard of care tenofovir disoproxil fumarate monotherapy or peginterferon alfa-2a monotherapy for 48 weeks in chronic hepatitis B (CHB). Available from: http://clinicaltrials.gov/ct2/show/NCT01277601 [Last accessed 19 September 2011]