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Effect of Adherence as Measured by MEMS, Ritonavir Boosting, and CYP3A5 Genotype on Atazanavir Pharmacokinetics in Treatment-Naive HIV-Infected Patients.
MedLine Citation:
PMID:  23033116     Owner:  NLM     Status:  Publisher    
Abstract/OtherAbstract:
We investigated population pharmacokinetics and pharmacogenetics of ritonavir-boosted atazanavir (ATV), using drug intake times exactly recorded by the Medication Event Monitoring System. The ANRS 134-COPHAR 3 trial was conducted in 35 HIV-infected treatment-naive patients. ATV (300 mg), ritonavir (100 mg), and tenofovir (300 mg) + emtricitabine (200 mg), in bottles with MEMS caps, were taken once daily for 6 months. Six blood samples were collected at week 4 to measure drug concentrations, and trough levels were measured bimonthly. A model integrating ATV and ritonavir pharmacokinetics and pharmacogenetics used nonlinear mixed effects. Use of exact dosing data halved unexplained variability in ATV clearance. The ritonavir-ATV interaction model suggested that optimal boosting effect is achievable at lower ritonavir exposures. Patients with at least one copy of the CYP3A5*1 allele exhibited 28% higher oral clearance. We provide evidence that variability in ATV pharmacokinetics is defined by adherence, CYP3A5 genotype, and ritonavir exposure.Clinical Pharmacology & Therapeutics (2012); advance online publication 3 October 2012. doi:10.1038/clpt.2012.137.
Authors:
R M Savic; A Barrail-Tran; X Duval; G Nembot; X Panhard; D Descamps; C Verstuyft; B Vrijens; A-M Taburet; C Goujard; F Mentré
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Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2012-10-03
Journal Detail:
Title:  Clinical pharmacology and therapeutics     Volume:  -     ISSN:  1532-6535     ISO Abbreviation:  Clin. Pharmacol. Ther.     Publication Date:  2012 Oct 
Date Detail:
Created Date:  2012-10-3     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  0372741     Medline TA:  Clin Pharmacol Ther     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Affiliation:
1] Université Paris Diderot, Sorbonne Paris Cité, INSERM, UMR 738, Paris, France [2] Department of Bioengineering and Therapeutic Sciences, University of California, San Francisco, San Francisco, California, USA.
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