Raltegravir: the first HIV type 1 integrase inhibitor.
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.
Hicks
Charles
C
Duke University Medical Center, Weill Medical College of Cornell University, Durham, North Carolina 27710, USA. charles.hicks@duke.edu
Gulick
Roy M
RM
D019380:Anti-HIV Agents / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D019429:Integrase Inhibitors / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D011760:Pyrrolidinones / Q000378:metabolism / Q000494:pharmacology* / Q000627:therapeutic use*; D000068898:Raltegravir Potassium
D019380:Anti-HIV Agents; D019429:Integrase Inhibitors; D011760:Pyrrolidinones; D000068898:Raltegravir Potassium