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Raltegravir is the first antiretroviral drug in the class of integrase inhibitors approved for the treatment of human immunodeficiency virus type 1 (HIV-1) in combination with other antiretroviral agents in treatment-experienced adults with evidence of ongoing viral replication and resistance to multiple antiretroviral drugs. Since raltegravir has a different mechanism of action to the currently licensed antiretroviral agents, it is a welcome addition in the treatment of HIV-1. Results from clinical studies to date indicate that raltegravir exhibits potent antiviral activity particularly against HIV-1 strains which exhibit resistance to other classes of antiretroviral drugs. It is well tolerated and has a favorable safety profile. Long-term follow-up data on its resistance profile and on potential interactions with other antiretroviral as well as concomitant medications will ultimately define its future role in the treatment of HIV-1 infection. This review briefly describes the mechanism of action of raltegravir and its pharmacokinetic profile, summarizes efficacy and safety data from recent clinical trials and implications for the use in treatment-naïve as well as treatment-experienced patients, depicts raltegravir's emerging resistance profile, and highlights potential drug-drug interactions. [ABSTRACT FROM AUTHOR]