Tenofovir disoproxil fumarate in the treatment of chronic hepatitis B

Expert Review of Anti-Infective Therapy

Volumn 8, Issue 10, 2010, Pages 1079-1092

  Jenh, Alice M ^a   Pham, Paul A ^b  

^a JOHNS HOPKINS HOSPITAL   (United States)

^b JOHNS HOPKINS UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

chronic hepatitis B; nucleotide analog reverse transcriptase inhibitor; tenofovir disoproxil fumarate

Indexed keywords

ACICLOVIR; ADEFOVIR; ADEFOVIR DIPIVOXIL; ALANINE AMINOTRANSFERASE; ALPHA2A INTERFERON; ALPHA2B INTERFERON; CIDOFOVIR; EMTRICITABINE; EMTRICITABINE PLUS TENOFOVIR DISOPROXIL; ENTECAVIR; GANCICLOVIR; HEPATITIS B SURFACE ANTIGEN; HEPATITIS B(E) ANTIGEN; INTERFERON; LAMIVUDINE; NUCLEOSIDE ANALOG; NUCLEOTIDE DERIVATIVE; PEGINTERFERON ALPHA2A; PROBENECID; RECOMBINANT ALPHA2B INTERFERON; TELBIVUDINE; TENOFOVIR; TENOFOVIR DISOPROXIL; TRIMETHOPRIM; VALACICLOVIR; VALGANCICLOVIR; VIRUS DNA;

ABDOMINAL PAIN; ABNORMAL LABORATORY RESULT; AREA UNDER THE CURVE; BACKACHE; CLINICAL TRIAL; CONCENTRATION RESPONSE; CROSS RESISTANCE; DECOMPENSATED LIVER CIRRHOSIS; DIARRHEA; DIZZINESS; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG ELIMINATION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG TOLERABILITY; DRUG TREATMENT FAILURE; FATIGUE; HEPATITIS B; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1 INFECTION; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; NAUSEA; NEPHROTOXICITY; NONHUMAN; PRACTICE GUIDELINE; RECOMMENDED DRUG DOSE; REVIEW; RHINOPHARYNGITIS; SIDE EFFECT; THROMBOCYTOPENIA; VIRUS RESISTANCE;

ADENINE; ANTIVIRAL AGENTS; CLINICAL TRIALS, PHASE III AS TOPIC; DOUBLE-BLIND METHOD; HEPATITIS B VIRUS; HEPATITIS B, CHRONIC; HUMANS; MULTICENTER STUDIES AS TOPIC; PHOSPHONIC ACIDS; PRACTICE GUIDELINES AS TOPIC; RANDOMIZED CONTROLLED TRIALS AS TOPIC; REVERSE TRANSCRIPTASE INHIBITORS; TREATMENT OUTCOME;

EID: 77958156082     PISSN: 14787210     EISSN: 17448336     Source Type: Journal    
DOI: 10.1586/eri.10.91     Document Type: Review

References (59)

1. Ayoub WS, Keeffe EB. Review article: current antiviral therapy of chronic hepatitis B. Aliment Pharmacol. Ther. 28(2), 167-177 (2008).
2. Chen CJ, Yang HI, Su J et al. Risk of hepatocellular carcinoma across a biological gradient of serum hepatitis B virus DNA level. JAMA 295(1), 65-73 (2006).
3. Fattovich G. Natural history and prognosis of hepatitis B. Semin. Liver Dis. 23(1), 47-58 (2003).
4. Reijnders JG, Perquin MJ, Zhang N, Hansen BE, Janssen HL. Nucleos (t) ide analogues only induce temporary hepatitis b e antigen seroconversion in most patients with chronic hepatitis B. Gastroenterology 139(2), 491-498 (2010).
5. ®, package insert. Gilead Sciences, Inc., Foster City, CA, USA (2010).
6. Marcellin P, Heathcote EJ, Buti M et al. Tenofovir disoproxil fumarate versus adefovir dipivoxil for chronic hepatitis B. N. Engl. J. Med. 359(23), 2442-2455 (2008). •• Two Phase III double-blind randomized controlled trials (Study 102 in hepatitis B e antigen [HBeAg]-negative patients, Study 103 in HBeAg-positive patients) that showed superiority of tenofovir compared to adefovir at 48 weeks for the treatment of chronic hepatitis B (CHB).
7. Leung N. Recent data on treatment of chronic hepatitis B with nucleos (t) ide analogues. Hepatol. Int. 2(2), 163-178 (2008).
8. Lok AS, Lai CL, Leung N et al. Long-term safety of lamivudine treatment in patients with chronic hepatitis B. Gastroenterology 125(6), 1714-1722 (2003).
9. Chang TT, Lai CL, Chien RN et al. Four years of lamivudine treatment in Chinese patients with chronic hepatitis B. J. Gastroenterol. Hepatol. 19(11), 1276-1282 (2004).
10. Yuen MF, Seto WK, Chow DH et al. Long-term lamivudine therapy reduces the risk of long-term complications of chronic hepatitis B infection even in patients without advanced disease. Antivir. Ther. 12(8), 1295-1303 (2007).
11. Liaw YF, Gane E, Leung N et al. 2-year GLOBE trial results: telbivudine is superior to lamivudine in patients with chronic hepatitis B. Gastroenterology 136(2), 486-495 (2009).
12. Hsu CW, Chen YC, Liaw YF et al. Prolonged effcacy and safety of 3 years of continuous telbivudine treatment in pooled data from Globe and 015 studies in chronic hepatitis B patients. Presented at: European Association for the Study of the Liver 2009 (EASL 2009). Copenhagen, Denmark, 22-26 April 2009.
13. Marcellin P, Chang TT, Lim SG et al. Long-term effcacy and safety of adefovir dipivoxil for the treatment of hepatitis B e antigen-positive chronic hepatitis B. Hepatology 48(3), 750-758 (2008).
14. 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 131(6), 1743-1751 (2006).
15. Tenney DJ, Rose RE, Baldick CJ et al. Long-term monitoring shows hepatitis B virus resistance to entecavir in nucleosidenaive patients is rare through 5 years of therapy. Hepato logy 49(5), 1503-1514 (2009).
16. Tenney DJ, Pokorowski KA, Rose RE et al. Entecavir maintains a high genetic barrier to HBV resistance through 6 years in naive patients. J. Hepatol. 50 (Suppl. 1), S10 (2009).
17. Nguyen MH, Keeffe EB. Chronic hepatitis B: early viral suppression and long-term outcomes of therapy with oral nucleos (t) ides. J. Viral Hepat. 16(3), 149-155 (2009).
18. Carey I, Harrison PM. Monotherapy versus combination therapy for the treatment of chronic hepatitis B. Expert Opin. Investig Drugs 18(11), 1655-1666 (2009). • Recent comprehensive review of monotherapy versus combination antiviral therapy for CHB in monoinfected patients.
19. Terrault NA. Benefits and risks of combination therapy for hepatitis B. Hepatology 49 (5 Suppl.), S122-S128 (2009). • Recent review of the benefits and risks of combination antiviral therapy in the treatment of CHB.
20. Yatsuji H, Suzuki F, Sezaki H et al. Low risk of adefovir resistance in lamivudine-resistant chronic hepatitis B patients treated with adefovir plus lamivudine combination therapy: two-year follow-up. J. Hepatol 48(6), 923-931 (2008).
21. Sung JJ, Lai JY, Zeuzem S et al. Lamivudine compared with lamivudine and adefovir dipivoxil for the treatment of HBeAgpositive chronic hepatitis B. J. Hepatol 48(5), 728-735 (2008).
22. Poordad F, Chee GM. Viral resistance in hepatitis B: prevalence and management. Curr. Gastroenterol. Rep. 12(1), 62-69 (2010). • Recent comprehensive review of genotypic and phenotypic resistance to hepatitis B virus nucleos (t) ide analogs.
23. Sheldon J, Camino N, Rodes B et al. Selection of hepatitis B virus polymerase mutations in HIV-coinfected patients treated with tenofovir. Antivir. Ther. 10(6), 727-734 (2005).
24. 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 49(4), 1158-1165 (2009).
25. Delaney WE 4th, Ray AS, Yang H et al. Intracellular metabolism and in vitro activity of tenofovir against hepatitis B virus. Antimicrob. Agents Chemother. 50(7), 2471-2477 (2006).
26. Fung S, Mazzulli T, Sherman M. Presence of rtA194T at baseline does not reduce effcacy to tenofovir (TDF) in patients with lamivudine (LAM)-resistant chronic hepatitis B [poster no. 880]. Presented at: 59th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2008). CA, USA, 31 October-4 November 2008.
27. Snow-Lampart A, Chappell B, Sorbel J et al. Evaluation of potential virologic resistance in HBV polymerase among subjects with persistent viremia following up to 144 weeks of therapy with tenofovir DF. Presented at: 45th Annual Meeting of the European Association for the Study of the Liver (EASL 2010). Vienna, Austria, 14-18 April 2010.
28. - hepatitis B patients treated with tenofovir DF showed no relationship between virologic breakthrough and emergence of genotypic changes in HBV polymerase. Hepatology 50 (Suppl. 4), A480 (2009).
29. Brunelle MN, Jacquard AC, Pichoud C et al. Susceptibility to antivirals of a human HBV strain with mutations conferring resistance to both lamivudine and adefovir. Hepatology 41(6), 1391-1398 (2005).
30. Qi X, Xiong S, Yang H, Miller M, Delaney WE. In vitro susceptibility of adefovirassociated hepatitis B virus polymerase mutations to other antiviral agents. Antivir. Ther. 12(3), 355-362 (2007).
31. Kitrinos K, Myrick F, Curtis M et al. In vitro tenofovir sensitivity of HBV populations from clinical specimens containing rtA181T/V and/or rtN236T. Hepatology 50 (Suppl. 4), A434 (2009).
32. Pham PA, Gallant JE. Tenofovir disoproxil fumarate for the treatment of HIV infection (review). Expert Opin. Drug Metab. Toxicol. 2(3), 459-469 (2006).
33. th International Symposium on Viral Hepatitis and Liver Disease. Washington DC, USA, 20-24 March 2009.
34. th International Symposium on Viral Hepatitis and Liver Disease. Washington DC, USA, 20-24 March 2009.
35. Marcellin P, Buti M, Krastev Z et al. Three years of tenofovir disoproxil fumarate (TDF) treatment in HBeAgnegative patients with chronic hepatitis B (Study 102); preliminary analysis. Presented at: 60 th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009. • 3-year data on Study 102 that was presented at the 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD), which demonstrate that tenofovir effcacy and safety is sustained at 3 years in HBeAg-negative CHB.
36. +) with chronic hepatitis B (Study 103), preliminary analysis. Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009. • 3-year data on Study 103 that was presented at the 60th Annual Meeting of the AASLD, which demonstrate that tenofovir effcacy and safety is sustained at 3 years in HBeAg-positive CHB.
37. Manns M, Jeffers L, Dalekos G et al. Safety and effcacy of 96 weeks of tenofovir disoproxil fumarate therapy in lamivudine experienced patients. Presented at: 44th Annual Meeting of the European Association for the Study of the Liver (EASL 2009). Copenhagen, Denmark, 22-26 April 2009.
38. Hann HW, Chae HB, Dunn SR. Tenofovir (TDF) has stronger antiviral effect than adefovir (ADV) against lamivudine (LAM)-resistant hepatitis B virus (HBV). Hepatol. Int. 2(2), 244-249 (2008).
39. Kuo A, Dienstag JL, Chung RT. Tenofovir disoproxil fumarate for the treatment of lamivudine-resistant hepatitis B. Clin. Gastroenterol. Hepatol. 2(3), 266-272 (2004).
40. Manns M, Heathcote J, Marcellin P et al. Effcacy of tenofovir DF treatment in patients with a suboptimal response to adefovir dipivoxil. Presented at: 45th Annual Meeting of the European Association for the Study of the Liver (EASL 2010). Vienna, Austria, 14-18 April 2010.
41. Levrero M, Cimino L, Lampertico P et al. Tenofovir DF (TDF) for chronic hepatitis B patients with suboptimal response to adefovir (ADV) or ADV/LAM treatment: interim analysis of the multicenter prospective open label study OptiB. Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009.
42. Sarin N, Yim C, Feld JJ et al. Tenofovir is effective salvage therapy for nucleosideresistant Hepatitis B. Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009.
43. Alazawi W, Cottle R, Ross V et al. Substitution of adefovir for tenofovir in patients with chronic HBV receiving combination therapy who have incomplete control or virological breakthrough-is it worthwhile? Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009.
44. van Bömmel F, Zöllner B, Sarrazin C et al. Tenofovir for patients with lamivudineresistant hepatitis B virus (HBV) infection and high HBV DNA level during adefovir therapy. Hepatology 44(2), 318-325 (2006).
45. Santos SA, Uriel AJ, Park JS et al. Effect of switching to tenofovir with emtricitabine in patients with chronic hepatitis B failing to respond to an adefovir-containing regimen. Eur. J. Gastroenterol. Hepatol. 18(12), 1247-1253 (2006).
46. Schildgen O, Sirma H, Funk A et al. Variant of hepatitis B virus with primary resistance to adefovir. N. Engl. J. Med. 354(17), 1807-1812 (2006).
47. van Bömmel F, de Man RA, Wedemeyer H et al. Long-term effcacy of tenofovir monotherapy for hepatitis B virusmonoinfected patients after failure of nucleoside/nucleotide analogues. Hepatology 51(1), 73-80 (2010).
48. Leemans WF, Niesters HG, van der Eijk AA, Janssen HL, Schalm SW, de Man RA. Selection of an entecavir-resistant mutant despite prolonged hepatitis B virus DNA suppression, in a chronic hepatitis B patient with preexistent lamivudine resistance: successful rescue therapy with tenofovir. Eur. J. Gastroenterol. Hepatol. 20(8), 773-777 (2008).
49. Buti M, Hadziyannis S, Mathurin P et al. Two years safety and effcacy of tenofovir disoproxil fumarate (TDF) in patients with HBV-induced cirrhosis. Presented at: 44th Annual Meeting of the European Association for the Study of the Liver (EASL 2009). Copenhagen, Denmark, 22-26 April 2009.
50. 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. 13(30), 4096-4099 (2007).
51. Choe WH, Kwon SY, Kim BK et al. Tenofovir plus lamivudine as rescue therapy for adefovir-resistant chronic hepatitis B in hepatitis B e antigen-positive patients with liver cirrhosis. Liver Int. 28(6), 814-820 (2008).
52. Liaw Y, Lee C, Akarca US et al. Interim results of a double-blind, randomized Phase 2 study of the safety of tenofovir disoproxil fumarate, emtricitabine plus tenofovir disoproxil fumarate, and entecavir in the treatment of chronic hepatitis B subjects with decompensated liver disease. Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009.
53. Tan J, Degertekin B, Wong SN, Husain M, Oberhelman K, Lok AS. Tenofovir monotherapy is effective in hepatitis B patients with antiviral treatment failure to adefovir in the absence of adefovir-resistant mutations. J. Hepatol. 48(3), 391-398 (2008).
54. Berg T, Moller B, Trinh H et al. Tenofovir disoproxil fumarate (TDF) versus emtricitabine plus TDF (FTC/TDF) for treatment of chronic hepatitis B (CHB) in patients with persistent viral replication receiving adefovir dipivoxil. Presented at: 44th Annual Meeting of the European Association for the Study of the Liver (EASL 2009). Copenhagen, Denmark, 22-26 April 2009.
55. Petersen J, Lutgehetmann M, Zoulim F et al. Entecavir and tenofovir combination therapy in chronic hepatitis B: rescue therapy in patients with advanced fbrosis and multiple previous treatment failures. Results from an international multicenter cohort study. Presented at: 60th Annual Meeting of the American Association for the Study of Liver Diseases (AASLD 2009). Boston, MA, USA, 30 October-1 November 2009.
56. Fontana RJ. Side effects of long-term oral antiviral therapy for hepatitis B. Hepatology 49 (5 Suppl.), S185-S195 (2009).
57. Gitman MD, Hirschwerk D, Baskin CH, Singhal PC. Tenofovir-induced kidney injury. Expert Opin. Drug Saf. 6(2), 155-164 (2007).
58. Buti M, Brosa M, Casado MA, Rueda M, Esteban R. Modeling the cost-effectiveness of different oral antiviral therapies in patients with chronic hepatitis B. J. Hepatol. 51(4), 640-646 (2009).
59. Jenh AM, Thio CL, Pham PA. Tenofovir for the treatment of hepatitis B virus. Pharmacotherapy 29(10), 1212-1227 (2009).