Raltegravir is the first licensed compound in 2007 of the new
integrase inhibitor drug class. At the dose of 400 mg twice daily,
raltegravir showed a potent
antiviral action in antiretroviral-naïve patients when associated with
tenofovir and
emtricitabine.
Raltegravir was also found to be highly active in antiretroviral-experienced patients with virological failure and displaying multiresistant virus, as shown with the BENCHMRK and ANRS 139 TRIO trials. Finally, the use of
raltegravir was assessed in the context of a switch strategy in antiretroviral-experienced patients with virological success [human immunodeficiency virus type 1 (HIV-1)
RNA below detection limit], highlighting the following mandatory criteria in this strategy: the
nucleoside reverse transcriptase inhibitors associated with
raltegravir have to be fully active. In the different studies,
raltegravir had a favorable safety and tolerability profile. In the clinical situation a switch in virologically suppressed patients receiving a
protease inhibitor, an improvement of the
lipid profile was observed. Overall, when analyzing the Phase II and III trials together, only a few patients on
raltegravir discontinued for adverse events. The development of resistance to
raltegravir mainly involved three resistance mutations in
integrase gene: Q148H/K/R, N155H, and Y143C/H/R. In conclusion,
raltegravir improved the clinical management of HIV-1
infection both in antiretroviral-naïve and in antiretroviral-experienced patients.