Abstract:
:Faldaprevir (FDV) is a potent, orally administered inhibitor of hepatitis C virus. In this single-centre, open-label, fixed-sequence, crossover study of 32 healthy adult male and female volunteers, subjects received either a single dose of cyclosporine (CsA) 50 mg (N = 16) or tacrolimus (TAC) 0.5 mg (N = 16), followed by a washout of at least 14 days. Each subject then received a loading dose of FDV 240 mg followed by 120 mg FDV once daily for 6 days. FDV 120 mg was then co-administered with an additional single dose of CsA (50 mg) or TAC (0.5 mg), followed by an additional 6 days of FDV 120 mg once daily. Intensive blood sampling was performed to assess the PK interaction potential. Assessment of relative BA indicated that exposure to CsA co-administered with FDV was similar to CsA alone. However, the AUCτ,ss and Cmax,ss of FDV were increased by 23% and 41%, respectively, when FDV was co-administered with CsA. Exposure to TAC was slightly increased (AUC0-∞ increased by 27%, no change in Cmax ) when TAC was co-administered with FDV. In contrast, exposure to FDV co-administered with TAC was similar to FDV alone. No unexpected safety findings arose from the trial. The limitations of the study (use of single, low dose of TAC and CsA, and only healthy volunteers in the trial) are discussed.
journal_name
Basic Clin Pharmacol Toxicoljournal_title
Basic & clinical pharmacology & toxicologyauthors
Huang F,Voelk C,Trampisch M,Rowland L,Schultz A,Sabo JPdoi
10.1111/bcpt.12980subject
Has Abstractpub_date
2018-07-01 00:00:00pages
84-93issue
1eissn
1742-7835issn
1742-7843journal_volume
123pub_type
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