Journal Article

Raltegravir: The First HIV Type 1 Integrase Inhibitor

Charles Hicks and Roy M. Gulick

in Clinical Infectious Diseases

Published on behalf of Infectious Diseases Society of America

Volume 48, issue 7, pages 931-939
Published in print April 2009 | ISSN: 1058-4838
Published online April 2009 | e-ISSN: 1537-6591 | DOI: http://dx.doi.org/10.1086/597290
Raltegravir: The First HIV Type 1 Integrase Inhibitor

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Raltegravir is the first approved human immunodeficiency virus type 1 (HIV-1) integrase inhibitor; it targets the strand transfer step of HIV-1 integration. Clinical trials have demonstrated that raltegravir-containing regimens have potent antiretroviral activity and are well tolerated in HIV-1–infected individuals. In antiretroviral treatment–experienced persons with drug-resistant HIV infection, raltegravir-containing treatment with an optimized background regimen was superior to an optimized background regimen alone. In treatment-naive persons, raltegravir was not inferior to efavirenz when the drugs were administered with tenofovir and lamivudine or emtricitabine. Raltegravir is metabolized by glucuronidation, not hepatically; thus, the potential for drug-drug interactions is decreased. Drug resistance, conferred by substitutions in the gene coding for the HIV-1 integrase enzyme, develops relatively frequently after virologic failure. As an antiretroviral drug with a novel mechanism of action, raltegravir is an important advancement in HIV-1 treatment options.

Journal Article.  4941 words.  Illustrated.

Subjects: Infectious Diseases ; Immunology ; Public Health and Epidemiology ; Microbiology

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