Teresa H Evering1, Martin Markowitz. 1. The Aaron Diamond AIDS Research Center/Rockefeller University, 455 First Avenue, New York, NY 10016, USA.
Abstract
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 multi-drug-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.
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 multi-drug-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.
Authors: Alonso Heredia; Olga Latinovic; Robert C Gallo; Gregory Melikyan; Marv Reitz; Nhut Le; Robert R Redfield Journal: Proc Natl Acad Sci U S A Date: 2008-12-15 Impact factor: 11.205
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