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22 healthy, HIV- and HCV-negative volunteers (12 female) were administered boceprevir 800 mg TID for 10 days with a single dose of raltegravir 400 mg on day 10, as well as another single dose of raltegravir 400 mg, separated by a washout phase. PK sampling occurred on day 10 of boceprevir (compared to historical values) and after each raltegravir dose.
The geometric mean (GM) of raltegravir area under the concentration-time curve (AUC)0-12h and maximum plasma concentration (Cmax) for raltegravir + boceprevir vs raltegravir alone were 4.27 (95% confidence interval [CI], 3.22-5.66) vs 4.04 (95% CI, 3.09-5.28) mg _ hour/L and 1.06 (95% CI, .76-1.49) vs 0.93 (95% CI, .70-1.23) mg/L, respectively.GM ratio estimates of raltegravir AUC0-12h and Cmax for raltegravir + boceprevir vs raltegravir alone were 1.04 (90% CI, .88-1.22) and 1.11 (90% CI, .91-1.36), respectively. The GM of boceprevir AUC0-8h, Cmax, and C8h were 5.45 (95% CI, 5.11-5.81) mg _ hour/L, 1.88 (95% CI, 1.72-2.06) mg/L, and 0.09 (95% CI, .07-.11) mg/L, respectively.The authors reported that boceprevir concentrations in this study did not differ from historical controls.
Clara de_Kanter, Maren Blonk, Angela Colbers, Quirine Fillekes, Bas Schouwenberg, David Burger. Influence of the hcv protease inhibitor boceprevir on the pharmacokinetics of the hiv integrase inhibitor raltegravir. 19th International Conference On Retroviruses And Opportunistic Infections. Seattle, WA, USA. ; 2011.