3rd International AIDS Society Conference on HIV Pathogenesis and Treatment Rio de Janeiro - July 24 - 27, 2005

PHARMACOKINETICS OF SCH 417690 ADMINISTERED ALONE OR IN COMBINATION WITH TENOFOVIR

IAS Conf HIV Pathog Treat 2005 Jul 24-27;3rd: Abstract No. TuPe3.1B09

Guillaume M.¹, Kraan M.², Soni P.², Keung A.², Sansone A.^2
1Aster Cephac, Paris, France, ²Schering Plough Research Institute, Kenilworth, New Jersey, United States of America

INTRODUCTION: Understanding potential interactions of SCH 417690, a CCR5 antagonist metabolized by CYP 3A4, with different antiretroviral therapies is essential. In this study, the potential interaction between tenofovir (Viread®), a recently introduced nucleotide analog, and SCH 417690 was assessed.

METHODS: In this randomized, open-label, parallel-group study, healthy adults were given SCH 417690 10 mg BID alone or coadministered with tenofovir 300 mg QD for 7 days. Tenofovir was given with the morning dose of SCH 417690 with a meal to maximize the exposure of tenofovir. Blood samples for pharmacokinetic analysis were obtained on Days 1, 7, and 8 through 12. The primary pharmacokinetic end points were SCH 417690 C_max and AUC_0-12, analyzed using a 1-way ANOVA. C_min values on Days 5 and 6 were used to assess steady-state concentrations. Safety was evaluated using adverse events (AEs), vital sign measurements, electrocardiograms (ECGs), and laboratory values.

RESULTS: Twenty-four subjects were enrolled (median age, 28 yrs; 54% men; 79% Caucasian), 12 per treatment group; 23 subjects completed the study. SCH 417690 steady-state was reached by Day 7 in both groups. There were no significant differences in SCH 417690 C_max, AUC_0-12, total body clearance, or terminal-phase half-life on Day 7 with and without tenofovir coadministration. Overall, 54% of subjects reported ≥1 AE (50% SCH 417690 alone and 54% combination). The most commonly reported AEs considered possibly related to study medication(s) included mild to moderate headache, abdominal pain, and flatulence. No clinically significant changes in ECGs, laboratory values, or vital signs were associated with either SCH 417690 alone or the combination treatment.

CONCLUSIONS: Coadministration of tenofovir with SCH 417690 did not affect SCH 417690 exposure significantly. SCH 417690 was well tolerated in healthy volunteers, with and without administration of tenofovir, supporting combined administration of SCH 417690 and tenofovir for the treatment of HIV.

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Basic | TuPe3.1B09 | Angela Sansone
PK and pharmacodynamics

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