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Intracellular and plasma pharmacokinetics of 400 mg of etravirine once daily versus 200 mg of etravirine twice daily in HIV-infected patients

AuthorsGutiérrez Valencia, Alicia; Martín-Peña, Reyes; Torres-Cornejo, Almudena; Ruiz-Valderas, Rosa; Castillo, J. R.; López-Cortés, Luis F. CSIC
Issue Date2012
PublisherOxford University Press
CitationJournal of Antimicrobial Chemotherapy 67(3): 681-684 (2012)
AbstractObjectives: To compare intracellular and plasma etravirine concentrations when etravirine was given at 200 mg/12 h versus 400 mg/24 h and to evaluate whether the results would support once-daily dosing.
Methods: This was an open-label sequential study in which eight patients on protease inhibitor (PI)-sparing regimens containing etravirine were included. Full pharmacokinetic profiles were performed while on 200 mg of etravirine/12 h and after switching to 400 mg of etravirine/24 h. Intracellular and plasma levels were determined by liquid chromatography coupled with mass spectrometry. Pharmacokinetic parameters were calculated by non-compartmental analysis and compared by geometric mean ratios (GMRs) using 200 mg of etravirine/12 h as the reference group. Trial registration: NCT01121809.
Results: The geometric mean (GM) for etravirine AUC 0-ο (5602 versus 5076 ng ·h/mL, GMR 0.91), C max (403 versus 495 ng/mL, GMR 1.23) and C min (139 versus 102 ng/mL, GMR 0.74) were similar with both dosing schedules at the intracellular level. In plasma, the GMRs for AUC 0-ο, C max and C min were 1.31, 1.76 and 0.99, respectively. The mean intracellular penetration, evaluated as intracellular and plasma AUC 0-ο ratios, was 81% when etravirine was dosed twice daily and 56% with once-daily dosing.
Conclusions: Our results show that intracellular etravirine levels were similar with both dosing regimens in patients with PI-sparing regimens, while etravirine plasma AUC 0-ο and C max were 30% and 76% higher with the once-daily regimen, respectively. Thus, a once-daily dosing regimen is supported not only by plasma etravirine pharmacokinetic profiles but also by intracellular levels. © The Author 2011. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved.
Identifiersdoi: 10.1093/jac/dkr534
issn: 0305-7453
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