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- Title
Raltegravir: The First HIV Type 1 Integrase Inhibitor.
- Authors
Hicks, Charles; Gulick, Roy M.
- Abstract
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.
- Subjects
HIV; HIV infections; THERAPEUTICS; ANTIRETROVIRAL agents; HIV-positive persons; DRUG resistance; GENE expression
- Publication
Clinical Infectious Diseases, 2009, Vol 48, Issue 7, p931
- ISSN
1058-4838
- Publication type
Article
- DOI
10.1086/597290