2008PubMedRequires access

[New treatment options in chronic hepatitis B].

Mario Umberto Mondelli

Open publisher page 2 citations

Abstract

To date, four different nucleoside/nucleotide analogues are available in the treatment of chronic hepatitis B (CHB): lamivudine, adefovir dipivoxil and entecavir; telbivudine, a deoxythymidine analogue that specifically inhibits polymerase-DNA of HBV, approved by the European Medicines Agency (EMEA), has recently become obtainable in Italy. Lamivudine, the first antiviral drug to be used in the treatment of chronic hepatitis B, shows an excellent bioavailability, a virtual absence of significant adverse drug reactions, and a high efficacy in reducing the viral load. Such good pharmacological features are not paralleled by a high genetic barrier. Adefovir dipivoxil, a nucleotide analogue, is considered an effective alternative option to lamivudine, due to the better genetic barrier (almost 30 percent of resistant mutants after 5 years of treatment). However, at the therapeutic approved doses (10 mg/die), adefovir demonstrates sub-optimal efficacy in suppressing viral replication. By contrast, it has proved highly effective against viral strains resistant to lamivudine. Entecavir, the nucleoside analogue most recently introduced in Italy, exhibits a substantial inhibition of viral replication and a high genetic barrier both in naive patients (< 1% of resistant mutants after three years), and in patients resistant to lamivudine treatment. Telbivudine appears a new, promising antiviral agent, characterised by a rapid and sustained virologic response, together with a good genetic barrier. Its excellent tolerability and safety profile (FDA Pregnancy Category B), specific mechanism of activity (no activity against HIV) and efficacy characteristics make telbivudine a first choice therapeutic option for treatment of patients affected by CHB.

About this research paper

What this paper is about

To date, four different nucleoside/nucleotide analogues are available in the treatment of chronic hepatitis B (CHB): lamivudine, adefovir dipivoxil and entecavir; telbivudine, a deoxythymidine analogue that specifically inhibits polymerase-DNA of HBV, approved by the European Medicines Agency (EMEA), has recently become obtainable in Italy. Lamivudine, the first antiviral drug to be used in the treatment of chronic hepatitis B, shows an excellent bioavailability, a virtual absence of significant adverse drug reactions, and a high efficacy in reducing the viral load. Such good pharmacological features are not paralleled by a high genetic barrier. Adefovir dipivoxil, a nucleotide analogue, is considered an effective alternative option to lamivudine, due to the better genetic barrier (almost 30 percent of resistant mutants after 5 years of treatment). However, at the therapeutic approved doses (10 mg/die), adefovir demonstrates sub-optimal efficacy in suppressing viral replication. By contrast, it has proved highly effective against viral strains resistant to lamivudine. Entecavir, the nucleoside analogue most recently introduced in Italy, exhibits a substantial inhibition of viral replication and a high genetic barrier both in naive patients (< 1% of resistant mutants after three years), and in patients resistant to lamivudine treatment. Telbivudine appears a new, promising antiviral agent, characterised by a rapid and sustained virologic response, together with a good genetic barrier. Its excellent tolerability and safety profile (FDA Pregnancy Category B), specific mechanism of activity (no activity against HIV) and efficacy characteristics make telbivudine a first choice therapeutic option for treatment of patients affected by CHB.

Why it matters

OpenAlex reports 2 citations for this work. Citation counts describe recorded attention and do not establish research quality.

Key contribution

A contribution statement is not available in the OpenAlex record.

Method / approach

Method details are not available in the OpenAlex metadata.

Main findings

Findings are not separately available in the OpenAlex metadata.

Limitations

Limitations are not available in the OpenAlex metadata.

Applications

Application details are not available in the OpenAlex metadata.

Available abstract

To date, four different nucleoside/nucleotide analogues are available in the treatment of chronic hepatitis B (CHB): lamivudine, adefovir dipivoxil and entecavir; telbivudine, a deoxythymidine analogue that specifically inhibits polymerase-DNA of HBV, approved by the European Medicines Agency (EMEA), has recently become obtainable in Italy. Lamivudine, the first antiviral drug to be used in the treatment of chronic hepatitis B, shows an excellent bioavailability, a virtual absence of significant adverse drug reactions, and a high efficacy in reducing the viral load. Such good pharmacological features are not paralleled by a high genetic barrier. Adefovir dipivoxil, a nucleotide analogue, is considered an effective alternative option to lamivudine, due to the better genetic barrier (almost 30 percent of resistant mutants after 5 years of treatment). However, at the therapeutic approved doses (10 mg/die), adefovir demonstrates sub-optimal efficacy in suppressing viral replication. By contrast, it has proved highly effective against viral strains resistant to lamivudine. Entecavir, the nucleoside analogue most recently introduced in Italy, exhibits a substantial inhibition of viral replication and a high genetic barrier both in naive patients (< 1% of resistant mutants after three years), and in patients resistant to lamivudine treatment. Telbivudine appears a new, promising antiviral agent, characterised by a rapid and sustained virologic response, together with a good genetic barrier. Its excellent tolerability and safety profile (FDA Pregnancy Category B), specific mechanism of activity (no activity against HIV) and efficacy characteristics make telbivudine a first choice therapeutic option for treatment of patients affected by CHB.

Key concepts: Telbivudine, Adefovir, Entecavir, Lamivudine, Nucleoside analogue, Virology, Hepatitis B, Pharmacology

Related papers

Back to paper searchBrowse research topicsOriginal source