Cyclosporine is a marketed immunosuppressive agent and a known substrate for CYP3A. Micofungin 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 micofungin (160 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.