Raltegravir: an integrase inhibitor for HIV-1.

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Evering TH, Markowitz M

Raltegravir: an integrase inhibitor for HIV-1.

Expert Opin Investig Drugs. 2008 Mar;17(3):413-22. doi: 10.1517/13543784.17.3.413 .

PubMed ID

18321239 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Raltegravir	Integrase	Protein	Human immunodeficiency virus 1	Yes	Inhibitor	Details