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Phase 3 Completed N=280 Randomized Double-blind Treatment

Tenofovir Disoproxil Fumarate (Tenofovir DF) Versus Emtricitabine/Tenofovir DF in Subjects Resistant to Lamivudine

Source: ClinicalTrials.gov NCT00737568 ↗
Enrolled (actual)
280
Serious AEs
15.7%
Results posted
Apr 2013
Primary outcomePrimary: Percentage of Participants With HBV DNA < 400 Copies/mL at Week 96 — 89.4; 86.3 percentage of participants — p=0.43

Summary

The aim of therapy for the treatment of chronic hepatitis B virus (HBV) is to maintain suppression of viral replication to prevent the emergence of complications, which requires long-term therapy. Durable suppression of viral replication is achieved in the treatment of chronic viral diseases by preventing of the emergence of drug-resistant mutations. The clinical guidelines for the management of lamivudine resistant patients are variable. Some recommend switching to another agent without cross-resistance, while others recommend adding on another agent without cross-resistance. Limited clinical data exists to demonstrate whether tenofovir disoproxil fumarate (tenofovir DF; TDF) is an effective monotherapy for lamivudine resistant patients or if it should be used as part of a combination therapy regimen. This study is designed to evaluate the effectiveness, safety, and tolerability of tenofovir DF monotherapy versus emtricitabine (FTC)/tenofovir DF combination therapy in participants with chronic HBV with lamivudine resistance (presence of the rtM204I/V mutation with or without the rtL180M mutation) over a 240-week period. Participants in this study must be receiving lamivudine treatment at the time of enrollment.

Outcome Measures

OutcomeResultp-value
PRIMARY
Percentage of Participants With HBV DNA < 400 Copies/mL at Week 96
89.4; 86.3 0.43
SECONDARY
Percentage of Participants With HBV DNA < 400 Copies/mL at Weeks 48, 144, 192, and 240
81.6; 84.2; 87.2; 84.9; 86.5; 85.6
SECONDARY
Percentage of Participants With HBV DNA < 169 Copies/mL at Weeks 48, 96, 144, 192, and 240
76.6; 77.7; 85.8; 83.5; 86.5; 84.9
SECONDARY
HBV DNA Level at Weeks 48, 96, 144, 192, and 240
2.42; 2.48; 2.29; 2.28; 2.26; 2.29
SECONDARY
Percentage of Participants With Normal ALT at Weeks 48, 96, 144, 192, and 240
67.4; 69.8; 70.2; 69.8; 70.2; 75.5
SECONDARY
Percentage of Participants With HBeAg Loss at Weeks 48, 96, 144, 192, and 240
9.2; 5.9; 15.4; 13.2; 23.1; 17.6
SECONDARY
Percentage of Participants With Seroconversion to Antibody Against HBeAg (Anti-HBe) at Weeks 48, 96, 144, 192, and 240
6.2; 4.4; 10.8; 10.3; 12.3; 11.8
SECONDARY
Percentage of Participants With HBV Surface Antigen (HBsAg) Loss at Weeks 48, 96, 144, 192, and 240
0.0; 0.7; 0.0; 0.7; 0.7; 1.4
SECONDARY
Percentage of Participants With Seroconversion to Antibody Against HBV Surface Antigen (Anti-HBs) at Weeks 48, 96, 144, 192, and 240
0.0; 0.0; 0.0; 0.0; 0.0; 0.7
SECONDARY
Percentage of Participants With Virologic Breakthrough at Weeks 48, 96, 144, 192, and 240
0.0; 0.8; 0.0; 0.0; 0.8; 0.8
SECONDARY
Percent Change From Baseline in Bone Mineral Density (BMD) of the Spine at Weeks 24, 48, 72, 96, 144, 192, and 240
-1.74; -1.83; -1.68; -1.73; -1.35; -1.95
SECONDARY
Percent Change From Baseline in BMD of the Hip at Weeks 24, 48, 72, 96, 144, 192, and 240
-0.71; -0.59; -1.15; -1.00; -1.59; -1.61
SECONDARY
Development of Drug-resistant Mutations (DRMs)
0; 0; 0; 0; 0; 0

Eligibility Criteria

Inclusion Criteria

  • Chronic HBV infection, defined as positive serum HBsAg for at least 6 months
  • 18 through 75 years of age, inclusive
  • HBV DNA ≥ 10^3 IU/mL
  • Receiving treatment with lamivudine with confirmation of HBV reverse transcriptase mutation(s) known to confer resistance to lamivudine (rtM204I/V with or without rtL180M) by central laboratory assessment prior to randomization; adefovir dipivoxil treatment of ≤ 48 weeks at the time of screening (inclusive of combination adefovir dipivoxil + lamivudine at entry) was allowed
  • Willing and able to provide written informed consent
  • Negative serum pregnancy test (for females of childbearing potential only)
  • Calculated creatinine clearance ≥ 50 mL/min
  • Hemoglobin ≥ 10 g/dL
  • Neutrophils ≥ 1000 /mm^3
  • No prior oral HBV therapy with approved nucleotide and/or nucleoside therapy or other investigational agents for HBV infection other than lamivudine or adefovir dipivoxil

Exclusion Criteria

  • Pregnant women, women who are breast feeding or who believe they may wish to become pregnant during the course of the study
  • Males and females of reproductive potential who are not willing to use an effective method of contraception during the study
  • Alanine aminotransferase (ALT) ≥ 10 × the upper limit of the normal range (ULN)
  • Decompensated liver disease
  • Interferon or pegylated interferon therapy within 6 months of the screening visit
  • Alpha fetoprotein > 50 ng/mL
  • Evidence of hepatocellular carcinoma
  • Coinfection with hepatitis C virus, HIV, or hepatitis D virus
  • Significant renal, cardiovascular, pulmonary, or neurological disease
  • Received solid organ or bone marrow transplantation
  • Receiving therapy with immunomodulators (eg, corticosteroids, etc.), investigational agents, nephrotoxic agents, or agents susceptible of modifying renal excretion
  • Proximal tubulopathy
  • Known hypersensitivity to the study drugs, the metabolites or formulation excipients
View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT00737568). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.

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