Nucleoside Analogs as Anti-HBV Agents

Abstract

Chronic hepatitis B virus (HBV) infection affects about 400 million people worldwide. The development of nucleoside analogs that inhibit HBV polymerase provides an important approach for treating HBV infection. The approval of lamivudine, adefovir and entecavir represents a cornerstone of hepatitis B therapy. However, the challenges from the resistance and the off-therapy viral rebound are still unmet, and there is a need of developing new therapeutic agents. This review will discuss the structure-activity relationship of the most significant anti-HBV nucleoside analogs and the latest development in the field.

Lamivudine for chronic hepatitis B: a brief review

“…Recent preliminary results show that adefovir dipivoxil and entecavir could be potent analogs for the treatment of HBV. Further studies are being made to assess the long-term efficacy and safety of these drugs [12,13].…”

HBeAg and hepatitis B virus DNA as outcome predictors during therapy with peginterferon alfa-2a for HBeAg-positive chronic hepatitis B

“…Reduction in hepatitis B virus deoxyribonucleic acid (HBV DNA) is an excellent measure of antiviral efficacy. However, a decrease in HBV DNA alone may be transient, particularly once antiviral agents are discontinued 2, 3. Seroconversion of hepatitis B e antigen (HBeAg) is another surrogate endpoint that is considered to be a marker for durable therapeutic response and improved clinical outcome in HBeAg‐positive patients with chronic hepatitis B 4, 5.…”

Telbivudine for Chronic Hepatitis B. A Review

“…Thus the treatment should be given in trials in a majority of patients for a long period. In addition, the long-term efficacy of lamivudine is limited by the frequent emergence of drug-resistant HBV mutants [5,6,7]. Adefovir is associated with a low frequency of resistance but its antiviral effect is not optimal [8,9].…”