Raltegravir-d4 is intended for use as an internal standard for the quantification of raltegravir by GC- or LC-MS. Raltegravir is an orally bioavailable inhibitor of HIV-1 integrase (IC50 = 15 nM in a strand transfer assay).1 It inhibits the spread of HIV-1IIIb infection in MT-4 cell culture with 95% cell culture inhibitory concentration (CIC95) values of 19 and 31 nM in medium containing 10% heat-inactivated fetal bovine serum (FBS) or 50% normal human serum, respectively. Formulations containing raltegravir have been used in combination therapy in the treatment of HIV-1 infection.
1.Summa, V., Petrocchi, A., Bonelli, F., et al.Discovery of raltegravir, a potent, selective orally bioavailable HIV-integrase inhibitor for the treatment of HIV-AIDS infectionJ. Med Chem.1(18)5843-5855(2008)