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Concomitant Cyclosporine and Micafungin Pharmacokinetics in Healthy Volunteers
Author(s) -
Hebert Mary F.,
Townsend Robert W.,
Austin Stephen,
Balan Guhan,
Blough David K.,
Buell Donald,
Keirns James,
Bekersky Ihor
Publication year - 2005
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 - 10.1177/0091270005278601
Subject(s) - micafungin , pharmacokinetics , concomitant , pharmacology , medicine , ciclosporin , drug interaction , cyp3a , oral administration , metabolism , transplantation , antifungal , amphotericin b , dermatology , cytochrome p450
Cyclosporine is a marketed immunosuppressive agent and a known substrate for CYP3A. Micafungin is an antifungal agent and a mild inhibitor of CYP3A‐mediated metabolism in vitro. The objectives of this study were to evaluate the pharmacokinetics of cyclosporine and micafungin before and with concomitant administration. The pharmacokinetics of single‐dose oral cyclosporine (5 mg/kg) were estimated on days 1, 9, and 15 (n = 27). Subjects received micafungin (100 mg/d over 1 hour) on days 7, 9, and 11 through 15. Micafungin pharmacokinetics were estimated on days 7, 9, and 15. Mean apparent oral cyclosporine clearances were estimated to be 645 ± 236 mL/h/kg, 546 ± 101 mL/h/kg (P = .01), and 540 ± 104 mL/h/kg (P = .02) for days 1, 9, and 15, respectively. Micafungin appears to be a mild inhibitor of cyclosporine metabolism.