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Safety and Efficacy Study of LB80380 in the Patients With Lamivudine-Refractory Chronic Hepatitis B

Phase 1
Completed
Conditions
Chronic Hepatitis B
Interventions
Registration Number
NCT00895596
Lead Sponsor
LG Life Sciences
Brief Summary

The purpose of the study is to investigate the safety and the antiviral activity of ascending multiple oral doses of LB80380 for 12 weeks in adults with lamivudine-refractory chronic hepatitis B infection.

Detailed Description

LB80380, an oral prodrug, is a promising candidate nucleoside analogue with antiviral activity against wild-type HBV. LB80380 is undergoing clinical development by LG Life Sciences for use in the treatment of chronic HBV infection and for treatment of lamivudine-resistant disease.

In this study, the treatment period was divided into two parts: a 4-week treatment period with dose escalation assessment (Part 1), followed by an 8-week extension period (Part 2).

During Part 1, patients received LB80380 and LVD 100 mg once daily for 4 weeks. Each patient was then given only LB80380 for an additional 8 weeks (Part 2) unless dose-limiting toxicity (DLT) was observed during Part 1. At each dose level, all patients were to complete at least Part 1 of the treatment period before enrolment into the next Dose Group could commence. Dose escalation to the next group was not to be initiated if more than two patients experienced DLT during Part 1 in the previous Dose Group. Additionally, patients enrolled in LB80380 150mg and 240mg groups who agreed to participate in the pharmacokinetic (PK) analyses visited the study site the day before Week 12 for blood sampling. Follow-up period was 24 weeks, and patients were treated with adefovir dipivoxil during the follow-up period. During the study, patients were evaluated for changes from baseline in serum HBV DNA. Safety was evaluated on the basis of occurrence of AEs and changes from baseline in clinical laboratory parameters, physical examination findings, and vital signs.

Recruitment & Eligibility

Status
COMPLETED
Sex
All
Target Recruitment
65
Inclusion Criteria
  • Compensated chronic hepatitis B patient
  • Presence of serum HBsAg for more than 6 months.
  • Presence of HBeAg for more than 1 month with compensated liver disease
  • Confirmation of YMDD mutants (M552V, M552I and its related double mutant at L528M) by genotyping of the YMDD motif using line probe assay (INNO-LiPA HBV DR assay)
  • Screening HBV DNA value higher than or equal to 1,000,000 copies/mL (measured by the COBAS Amplicor HBV Monitor™ assay)
  • Screening ALT value between 1.5 and 10 x ULN
Exclusion Criteria
  • Co-infection with hepatitis C or D virus (HCV or HDV) or HIV
  • Pregnancy or breast-feeding
  • Previous treatment with nucleoside analogue or any other treatment for HBV except for lamivudine within 6 months prior to study entry
  • Treatment with immunomodulatory agent or corticosteroids within 6 months prior to study entry.
  • De-compensated liver disease
  • Screening alpha-fetoprotein (AFP) value > 20 ng/mL, and a follow-up ultrasonography performed prior to baseline shows findings indicative of HCC.
  • Presence of anti-HBs at screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
Not specified
Arm && Interventions
GroupInterventionDescription
LB80380 30mgLB80380LB80380 30mg
LB80380 60mgLB80380LB80380 60mg
LB80380 90mg,LB80380LB80380 90mg
LB80380 150mgLB80380LB80380 150mg
LB80380 240mgLB80380LB80380 240mg
Primary Outcome Measures
NameTimeMethod
Mean serum HBV DNA level (log10) reduction from the baseline at Week 12Week 12
Secondary Outcome Measures
NameTimeMethod
Proportion of patients with HBeAg seroconversion at 12 weeks Proportion of patients with HBsAg seroconversion at 12 weeks Proportion of patients with ALT normalization at 12 weeks Safety assessment during the whole study periodWeek 12

Trial Locations

Locations (4)

Korea University Medical Center

🇰🇷

Seoul, Korea, Republic of

Queen Mary Hospital

🇨🇳

Hong Kong, China

Severance Hospital of Yonsei University

🇰🇷

Seoul, Korea, Republic of

The Catholic University of Korea, Kangnam St. Mary's Hospital

🇰🇷

Seoul, Korea, Republic of

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