Atazanavir-d6 is intended for use as an internal standard for the quantification of atazanavir by GC- or LC-MS. Atazanavir is an azapeptide inhibitor of HIV-1 protease (Ki = 2.66 nM).1 It has antiviral activity against a variety of HIV-1 strains in several cell types with EC50 values ranging from 2.62 to 5.28 nM. Atazanavir exhibits a minor synergistic effect when used in combination with the reverse transcriptase inhibitor zidovudine in HIV-1-infected human peripheral blood mononuclear cells (PBMCs) and an additive effect when used in combination with several additional reverse transcriptase or HIV-1 protease inhibitors. Atazanavir also inhibits UDP-glucuronyltransferase 1A1 (UGT1A1), which is involved in bilirubin clearance.2 Formulations containing atazanavir have been used in combination therapy for the treatment of HIV-1 infection.
1.Robinson, B.S., Riccardi, K.A., Gong, Y.F., et al.BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agentsAntimicrobial Agents and Chemotherapy44(8)2093-2099(2000) 2.Michaud, V., Bar-Magen, T., Turgeon, J., et al.The dual role of pharmacogenetics in HIV treatment: Mutations and polymorphisms regulating antiretroviral drug resistance and dispositionPharmacological Reviews64(3)803-833(2012)