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Coadministration With Lopinavir and Ritonavir Decreases Exposure to BILR 355, a Nonnucleoside Reverse Transcriptase Inhibitor, in Healthy Volunteers
Author(s) -
Huang Fenglei,
Scholl Paul,
Huang David B.,
MacGregor Thomas R.,
Vinisko Richard,
Castles Mark A.,
Berger Frank,
Robinson Patrick
Publication year - 2011
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270010376971
Subject(s) - lopinavir , ritonavir , lopinavir/ritonavir , pharmacokinetics , pharmacology , dosing , medicine , drug interaction , reverse transcriptase inhibitor , viral load , human immunodeficiency virus (hiv) , immunology , antiretroviral therapy
The objective of this investigation was to evaluate the pharmacokinetic interaction of lopinavir/ritonavir (LPV/r) with BILR 355. In group A, 26 healthy participants were administered LPV/r (400mg/100mg) twice daily for 14 days, followed by coadministration of BILR 355, 150 mg twice daily for an additional 7 days. Pharmacokinetic assessments were performed on days 14 and 21. In group B, 8 healthy participants were given BILR 355/ritonavir (BILR 355/r, 150mg/100mg) twice daily for 7 days. The pharmacokinetic data from group B (BILR 355/r‐alone group) were also pooled with group B subjects from 3 similar phase I drug‐drug interaction trials performed in parallel to this study. Coadministration with LPV/r resulted in a 51% decrease in steady‐state area under plasma concentration‐time curve from 0 to 12 hours (AUC 0–12, ss ) and steady‐state maximum measured plasma concentration over a dosing interval (C max, ss ) and a 50% decrease in steady‐state plasma concentration 12 hours post last dosing (C 12, ss ) for BILR 355. Exposure to LPV was not changed after coadministration. BILR 355/r was well tolerated in this study. There was no evidence of increased risk of lopinavir or ritonavir toxicity upon coadministration with BILR 355.