Abstract
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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adult
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Antifungal Agents / administration & dosage
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Antifungal Agents / pharmacology*
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Area Under Curve
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Cyclosporine / administration & dosage
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Cyclosporine / blood
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Cyclosporine / pharmacokinetics*
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Cytochrome P-450 CYP3A
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Cytochrome P-450 Enzyme Inhibitors*
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Cytochrome P-450 Enzyme System / metabolism
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Drug Interactions
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Echinocandins
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Female
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Half-Life
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Humans
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Immunosuppressive Agents / administration & dosage
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Immunosuppressive Agents / blood
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Immunosuppressive Agents / pharmacokinetics*
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Lipopeptides
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Lipoproteins / administration & dosage
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Lipoproteins / pharmacology*
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Male
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Metabolic Clearance Rate
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Micafungin
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Middle Aged
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Peptides, Cyclic / administration & dosage
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Peptides, Cyclic / pharmacology*
Substances
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Antifungal Agents
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Cytochrome P-450 Enzyme Inhibitors
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Echinocandins
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Immunosuppressive Agents
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Lipopeptides
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Lipoproteins
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Peptides, Cyclic
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Cyclosporine
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Cytochrome P-450 Enzyme System
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CYP3A protein, human
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Cytochrome P-450 CYP3A
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Micafungin