Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium

Raltegravir is the first integrase strand transfer inhibitor approved for the treatment of HIV‐1 infection. As the first agent in this new class of antiretroviral therapies, raltegravir has demonstrated safety and efficacy in treatment‐naive as well as heavily pretreated HIV‐infected patients failing therapy with multidrug‐resistant virus. Raltegravir has a favorable drug interaction profile that permits both administration to a wide, demographically diverse patient population and coadministration with many other therapeutic agents, including antiretroviral agents and supportive medications, without restrictions or dose adjustment. Data through 96 weeks of follow‐up in three phase III studies, protocol 021 (STARTMRK) in treatment‐naive patients, and protocols 018 (BENCHMRK‐1) and 019 (BENCHMRK‐2) in treatment‐experienced patients, demonstrated the potent and durable antiretroviral and immunologic effects and the favorable long‐term safety profile of raltegravir in both treatment‐naive and treatment‐experienced patients. Raltegravir represents an important addition to the current armamentarium for the treatment of HIV infection.