Abstract
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▴ Atazanavir is a novel azapeptide protease inhibitor with high specificity for, and activity against, HIV-1 protease.
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▴ The resistance profile of atazanavir is distinct, with an I50L protease substitution appearing to be the signature mutation.
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▴ Atazanavir was not associated with increases in total cholesterol, low density lipoprotein-cholesterol or triglyceride levels after 108 weeks.
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▴ Atazanavir has a pharmacokinetic profile that allows for once-daily oral administration. It is a moderate inhibitor of hepatic cytochrome P450 enzymes and interacts with several drugs.
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▴ In combination with stavudine plus didanosine, atazanavir 200, 400 or 500mg once daily produced a rapid and sustained reduction from baseline in viral load of 2.57, 2.42 and 2.53 log10 copies/mL, respectively, in treatment-naive patients after 48 weeks, compared with a decrease of 2.33 log10 copies/mL with nelfinavir 750mg three times daily.
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▴ Nausea was the most clinically relevant adverse event reported in patients receiving atazanavir-based regimens.
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Goldsmith, D.R., Perry, C.M. Atazanavir. Drugs 63, 1679–1693 (2003). https://doi.org/10.2165/00003495-200363160-00003
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DOI: https://doi.org/10.2165/00003495-200363160-00003