Elvitegravir-d6 is intended for use as an internal standard for the quantification of elvitegravir by GC- or LC-MS. Elvitegravir is a quinolone antibiotic that inhibits HIV-1 integrase (IC50 = 7.2 nM).1 It has antiviral activity against laboratory strains and clinical isolates of HIV-1 (EC50s = 0.1-1.26 nM) in MAGI cells and HIV-2 (EC50s = 0.3-0.9) in peripheral blood mononuclear cells (PBMCs).1,2 Formulations containing elvitegravir have been used in the treatment of HIV infections.
1.Sato, M., Motomura, T., Aramaki, H., et al.Novel HIV-1 integrase inhibitors derived from quinolone antibioticsJ. Med. Chem.49(5)1506-1508(2006) 2.Roquebert, B., Damond, F., Collin, G., et al.HIV-2 integrase gene polymorphism and phenotypic susceptibility of HIV-2 clinical isolates to the integrase inhibitors raltegravir and elvitegravir in vitroJ. Antimicrob. Chemother.62(5)914-920(2008)