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Concomitant Administration of BILR 355/r with Emtricitabine/Tenofovir Disoproxil Fumarate Increases Exposure to Emtricitabine and Tenofovir: A Randomized, Open‐Label, Prospective Study
Author(s) -
Huang Fenglei,
Scholl Paul,
Huang David B.,
MacGregor Thomas R.,
Taub Mitchell E.,
Vinisko Richard,
Castles Mark A.,
Robinson Patrick
Publication year - 2011
Publication title -
basic and clinical pharmacology and toxicology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.805
H-Index - 90
eISSN - 1742-7843
pISSN - 1742-7835
DOI - 10.1111/j.1742-7843.2010.00636.x
Subject(s) - emtricitabine , pharmacokinetics , medicine , concomitant , tenofovir , confidence interval , pharmacology , urology , human immunodeficiency virus (hiv) , antiretroviral therapy , viral load , family medicine
The objective of this study was to evaluate the pharmacokinetic interaction of ritonavir‐boosted BILR 355 (BILR 355/r) with emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF). This was an open‐label, prospective study. For Group A, 26 healthy subjects were given FTC/TDF (200/300 mg) once daily (QD) for 7 days and then co‐administered with BILR 355/r (150/100 mg) twice daily (bid) for an additional 7 days. Pharmacokinetics assessments were performed at days 7 and 14. For Group B, eight subjects were given BILR 355/r (150/100 mg) bid for 7 days. The pharmacokinetic data from Group B were also pooled with Group B subjects from other similar studies performed in parallel to this study. After co‐administration with BILR 355/r, the geometric mean ratio (GMR, %) and 90% confidence interval (CI, %) of combined versus alone treatment for FTC AUC 0–24,ss , C max,ss and C 0–12,ss were 160 (154–166), 128 (121–136) and 223 (206–241), respectively; and for tenofovir AUC 0–24,ss , C max,ss and C 24,ss were 126 (121–132), 131 (117–146) and 132 (124–140), respectively. Co‐administration with FTC/TDF resulted in an 18% increase in AUC 0–12,ss , 14% increase in C max,ss and 19% increase in C 12,ss for BILR 355. BILR 355 was well tolerated in this study. There was no evidence of increased risk of TFV or FTC toxicity upon co‐administration of FTC/TDF with BILR 355/r.