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Emtricitabine/Tenofovir Disoproxil Fumarate

In Combination with a Protease Inhibitor in HIV-1 Infection

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Abstract

  • ▲ Emtricitabine, a nucleoside reverse transcriptase inhibitor (RTI), and tenofovir disoproxil fumarate (tenofovir DF), a nucleotide RTI, as a fixed-dose combination tablet (emtricitabine/tenofovir DF) for once-daily oral administration, are used as the nucleoside/nucleotide RTI backbone in combination with other antiretroviral agents, including ritonavir-boosted protease inhibitors (PIs), in the treatment of adults with HIV-1 infection.

  • ▲ Emtricitabine and tenofovir DF show good activity against laboratory strains and clinical isolates of HIV-1 in vitro, although strains with resistance to emtricitabine or tenofovir have also been reported.

  • ▲ Regimens consisting of once-daily emtricitabine/tenofovir DF 200 mg/300 mg plus lopinavir/ritonavir (in the randomized, double-blind, placebo-matched, multicentre HEAT study) or boosted atazanavir or efavirenz (in the randomized, partially-blind, multicentre ACTG 5202 trial) were effective in the initial treatment of patients with HIV-1 infection (with screening plasma HIV-1 RNA levels of ≥100 000 copies/mL in ACTG 5202).

  • ▲ In other randomized studies, emtricitabine/tenofovir DF 200 mg/300 mg once daily was an effective backbone for boosted PI-based regimens in the initial treatment of HIV-1 infection. Treatment-experienced patients with HIV-1 infection also experienced beneficial virological effects when treated with similar regimens.

  • ▲ Emtricitabine/tenofovir DF in combination with various boosted PIs was generally well tolerated by adults with HIV-1 infection.

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Acknowledgments and Disclosures

This manuscript was reviewed by: A. Hill, Department of Pharmacology, University of Liverpool, Liverpool, England; D. Podzamczer, HIV Unit, Infectious Disease Service, Hospital Universitari de Bellvitge, Barcelona, Spain.

The preparation of this review was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made on the basis of scientific and editorial merit.

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  1. Wolters Kluwer Health ¦ Adis, 41 Centorian Drive, Private Bag 65901, Mairangi Bay, North Shore, Auckland, 0754, New Zealand

    Caroline M. Perry

  2. Wolters Kluwer Health, Conshohocken, Pennsylvania, USA

    Caroline M. Perry

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Correspondence to Caroline M. Perry.

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Perry, C.M. Emtricitabine/Tenofovir Disoproxil Fumarate. Drugs 69, 843–857 (2009). https://doi.org/10.2165/00003495-200969070-00005

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