Abstract

Azatanavir is a protease inhibitor (PI) approved for the treatment of HIV-1 infection. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A and an inhibitor and inducer of P-glycoprotein. It has similar virologic efficacy as efavirenz and ritonavir-boosted lopinavir in antiretroviral-naive individuals. Its impact on lipids is less than other PIs and it is suitable for those in whom hyperlipidemia is undesirable. Ritonavir boosting of atazanavir enhances the bioavailability of atazanavir but may result in some elevation of lipids and is recommended for treatment-experienced patients and those receiving efavirenz or tenofovir. Ritonavir-boosted atazanavir has similar antiviral activity as ritonavir-boosted lopinavir in both antiretroviral therapy-naive and -experienced patients. Atazanavir causes unconjugated bilirubinemia in over 40% of patients but results in less than 2% discontinuations. Atazanavir is licensed for once-daily use and atazanavir/ritonavir competes with lopinavir/ritonavir as the most commonly prescribed PI.

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