Raltegravir in the management of HIV-infected patients

Hans-Jürgen Stellbrink

ICH and IPM Study Center Hamburg, Hamburg, Germany

Abstract: Raltegravir has recently been licensed for the treatment of HIV-1 infection. Currently its use is limited to treatment-experienced patients and subjects with resistant virus. In addition to its activity in the setting of resistance and treatment failure, it appears to have great potential for first-line therapy and as a switch option for subjects with intolerance to other agents, as well. Overall tolerability in clinical trials was excellent, and the toxicity profile is non-overlapping with other agents, with no clear neuropsychiatric, gastrointestinal, or metabolic toxicity. Its metabolization occurs mainly via UGT1A1 rather than by the CYP450 system, resulting in a relatively unproblematic drug interaction profile. The independence of the compound from “boosting” of drug levels with ritonavir is an attractive feature for many patients suffering from ritonavir-associated side effects. However, it has to be dosed twice daily. The unique effect of raltegravir on the establishment of viral latency makes it a logical component of treatment attempts aiming at reducing and controlling this viral sanctuary. This review summarizes the clinical view on the role of this novel compound in HIV therapy.

Keywords: raltegravir, MK-0518, integrase inhibitor, HIV infection, HAART