Raltegravir: an integrase inhibitor for HIV-1

Background: The need to develop antiretroviral agents with novel mechanisms of action persists for the treatment of both antiretroviral-experienced and antiretroviral-naive patients with HIV/AIDS. This is mandated, in part, by the perpetual advent of antiretroviral-resistant HIV-1 strains. Raltegravir has been shown to specifically inhibit the essential, HIV-1-encoded, integrase enzyme. As a result, this agent represents a promising chemotherapeutic agent for the treatment of HIV/AIDS. Objective: To form an evidence-based determination of the clinical efficacy, pharmacokinetics and safety profile of raltegravir. Method: We discuss available peer-reviewed publications, preliminary data presented in abstract from relevant scientific meetings and data available from the US Food and Drug Administration (FDA). Results/conclusion: Current evidence strongly supports raltegravir use in highly active antiretroviral therapy (HAART) regimens constructed to treat patients failing current therapies with multidrug-resistant HIV-1. Additional data are needed to determine its role in the treatment of less advanced patients. Issue surrounding long-term adverse effects and genetic barriers to raltegravir resistance will be critical in determining the potential of this agent.