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Tenofovir disoproxil fumarate for the treatment of hepatitis B virus infection: pharmacokinetics and clinical efficacy

David J Quan and Marion G Peters

Tenofovir is an acyclic nucleotide phosphonate diester analogue of adenosine monophosphate with antiviral activity against HIV-1 and hepatitis B virus. After two phosphorylations, tenofovir inhibits HIV-1 reverse transcriptase by competing with the natural substrate, deoxyadenosine 5´-triphosphate. Tenofovir disoproxil fumarate has been approved by the US FDA for the treatment of HIV-1 infection in combination with other antiretroviral agents. Although not approved by the FDA for the treatment of chronic hepatitis B virus infection, tenofovir has anti-hepatitis B virus activity in patients co-infected with HIV and hepatitis B. This paper will review the pharmacology and clinical experience with tenofovir, with a focus on hepatitis B infection.