Author(s): Stellbrink HJ
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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.
This article was published in Drug Des Devel Ther
and referenced in Journal of Antivirals & Antiretrovirals