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Emtricitabine

  • Chapter
Book cover Reverse Transcriptase Inhibitors in HIV/AIDS Therapy

Part of the book series: Infectious Disease ((ID))

Abstract

Emtricitabine (FTC, Coviracil®) is a synthetic nucleoside analog of cytosine with activity against HIV-1. It is chemically similar to lamivudine, differing only in having a fluoride at the 5-position of the cytosine ring. Emtricitabine is the (& minus) enantiomer, which is more active than the (+) enantiomer. Emtricitabine has a long plasma half-life (10 h), and even longer intracellular half-life of the active triphosphate (39 h), supporting once-daily dosing. Short-term monotherapy studies have demonstrated that emtricitabine 200 mg QD reduces HIV RNA levels by 1.7 to 1.92 log10 copies/mL. Large, multicenter clinical trials have demonstrated emtricitabine’ efficacy, in combination with efavirenz and either didanosine or tenofovir. Similar to lamivudine, emtricitabine is generally well tolerated. one notable side effect attributable to emtricitabine is skin discoloration of the palms and soles, particularly in African American and Hispanic patients. Preliminary data on emtricitabine in the pediatric population have also demonstrated safety and efficacy. Emtricitabine has not been studied in pregnant women. Resistance to emtricitabine is correlated with the emergence of the same Met184Val mutation in reverse transcriptase that mediates resistance to lamivudine. The emergence of M184V appears to be less frequent in patients failing a regimen containing emtricitabine than in patients failing a lamivudine-containing regimen. Current US DHHS and IAS-USA guidelines support emtricitabine as a recommended component of an initial antiretroviral regimen (1, 2).

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Author information

Authors and Affiliations

  1. Boston University School of Medicine, Providence, RI

    Gail Skowron (Associate Professor of Medicine, Chief)

  2. Division of Infectious Diseases, Roger Williams Medical Center, Providence, RI

    Gail Skowron (Associate Professor of Medicine, Chief)

  3. Department of Pharmacy Practice, University of Rhode Island, Kingston, RI

    Jeffrey Bratberg (Clinical Assistant Professor)

  4. Saint-Legier, Switzerland

    Rudi Pauwels

Authors
  1. Gail Skowron
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  2. Jeffrey Bratberg
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  3. Rudi Pauwels
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Editor information

Editors and Affiliations

  1. National Institute of Allergy and Infectious Diseases National Institutes of Health, USA

    Vassil St.Georgiev

  2. Division of Infectious Diseases, Roger Williams Medical Center, Providence, RI

    Gail Skowron MD (Chief) (Chief)

  3. Boston University School of Medicine, Boston, MA

    Gail Skowron MD (Chief) (Chief)

  4. Pfizer Inc., San Diego, CA

    Richard Ogden PhD

  5. Center for Poverty-Related Communicable Diseases Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands

    Joep M. A. Lange MD, PhD (Professor of Medicine) (Professor of Medicine)

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© 2006 Humana Press Inc., Totowa, NJ

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Skowron, G., Bratberg, J., Pauwels, R. (2006). Emtricitabine. In: St.Georgiev, V., Skowron, G., Ogden, R., Lange, J.M.A. (eds) Reverse Transcriptase Inhibitors in HIV/AIDS Therapy. Infectious Disease. Humana Press. https://doi.org/10.1007/978-1-59745-085-0_4

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  • DOI: https://doi.org/10.1007/978-1-59745-085-0_4

  • Publisher Name: Humana Press

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