A review of entecavir in the treatment of chronic hepatitis B infection.

Abstract

BACKGROUND:

Infection with the hepatitis B virus (HBV) affects two billion people worldwide, and an estimated 400 million people are chronically infected. Currently, FDA-approved regimens for the treatment of chronic HBV include interferon-alpha2b, peginterferon-alpha2a, lamivudine, adefovir dipivoxil, and recently, entecavir.

OBJECTIVE:

The purpose of this review is to evaluate the pharmacokinetic and pharmacodynamic properties, and the clinical efficacy and safety of entecavir in the treatment of nucleoside-naĩve and nucleoside-resistant HBeAg-positive and HBeAg-negative chronic hepatitis B (CHB). SEARCH METHODOLOGY: Computerized searches of PubMed and International Pharmaceutical Abstracts from 1985 to July 10, 2005, were performed with the search headings: entecavir, BMS-200475, and chronic hepatitis B.

FINDINGS:

Entecavir, a new deoxyguanosine analog, represents a third agent within the nucleoside/nucleotide HBV polymerase inhibitor class with distinct advantages over lamivudine and adefovir dipivoxil: it has a three-step mechanism of action, is the most potent inhibitor of HBV DNA polymerase, is not associated with any major adverse effects, and has a limited potential for resistance. In phase II and III clinical trials, entecavir was found to be superior to lamivudine for all primary endpoints evaluated in both nucleoside-naïve and lamivudine-resistant patients. Entecavir was effective in both HBeAg-positive and HBeAg-negative nucleoside-naïve patients. At this time, optimal duration of entecavir therapy is unknown.

CONCLUSION:

Entecavir represents a new first- or second-line treatment option for patients chronically infected with HBV. Long-term efficacy and safety studies as well as studies of entecavir in combination with interferon products or other nucleoside/nucleotide analogs are eagerly awaited.

• Authors: Anastasia Rivkin
• Journal: Current medical research and opinion (Curr Med Res Opin) Vol. 21 Issue 11 Pg. 1845-56 (Nov 2005) ISSN: 0300-7995 [Print] England
• PMID: 16307706 (Publication Type: Journal Article, Review)

Chemical References

• Reverse Transcriptase Inhibitors
• Lamivudine
• entecavir
• Guanine

Topics

• Animals
• Clinical Trials as Topic
• Guanine (analogs & derivatives, pharmacokinetics, therapeutic use)
• Hepatitis B virus (metabolism)
• Hepatitis B, Chronic (drug therapy, physiopathology)
• Humans
• Lamivudine (therapeutic use)
• Practice Guidelines as Topic
• Randomized Controlled Trials as Topic
• Reverse Transcriptase Inhibitors (therapeutic use)
• Treatment Outcome