Clinical pharmacology, efficacy and safety of atazanavir: a review.
BACKGROUND
Atazanavir (ATV) is a potent and safe protease inhibitor (PI) initially approved in adult HIV-1 infected patients in combination with other antiretroviral drugs with once daily administration. In combination with nucleoside reverse transcriptase inhibitors (NRTIs) and boosted with ritonavir, it has been established as the preferred initial regimen in published guidelines.


OBJECTIVE
This article reviews relevant pharmacodynamic, pharmacokinetic, efficacy and safety data of ATV, administered boosted with ritonavir or unboosted, in comparison with other PIs and/or non-NRTIs, with special focus on recent studies.


METHODS
Review articles, recent primary literature and scientific meeting reports were analyzed.


RESULTS
Compared to most PIs with similar efficacy, the advantages of ATV are a once daily administration with only 100 mg ritonavir when boosted, a good gastrointestinal tolerance with limited diarrhea, a neutral effect on cholesterol and triglycerides, and a favorable resistance profile. However, highly frequent hyperbilirubinemia is observed resulting in some cases in clinical jaundice. Unboosted ATV must be cautiously used because increased resistances have been described.


CONCLUSIONS
The combination of a similar efficacy, a better tolerance and a low pill burden, as compared to other PIs, makes boosted ATV one of the best options, in combination with NRTIs, in PI-naive HIV-1 infected patients.
Bentué-Ferrer
Danièle
D
Centre Hospitalier Universitaire de Rennes, Hôpital de Pontchaillou, France.
Arvieux
Cédric
C
Tribut
Olivier
O
Ruffault
Annick
A
Bellissant
Eric
E
D000328:Adult; D000818:Animals; D000069446:Atazanavir Sulfate; D017322:Clinical Trials, Phase II as Topic; D017326:Clinical Trials, Phase III as Topic; D004347:Drug Interactions; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy*; D017320:HIV Protease Inhibitors / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D009842:Oligopeptides / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use*; D011725:Pyridines / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use*
D017320:HIV Protease Inhibitors; D009842:Oligopeptides; D011725:Pyridines; D000069446:Atazanavir Sulfate