Journal
LIFE SCIENCES
Volume 83, Issue 7-8, Pages 229-235Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.lfs.2008.06.013
Keywords
micafungin; multidrug resistance-associated protein 2 (ABCC2/Mrp2) hepatobiliary excretion; Eisai hyperbilirubinemic rats (EHBR)
Funding
- Ministry of Education, Culture, Sports, Science and Technology of Japan [17590500]
- Promotion and Mutual Aid Corporation for Private Schools of Japan
- Grants-in-Aid for Scientific Research [17590500] Funding Source: KAKEN
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The drug transporter, multidrug resistance-associated protein 2 (ABCC2/Mrp2), is known to play important roles in excretion of various drugs. In the present study, we investigated whether Mrp2 is involved in the transport of micafungin, a newly developed antifungal agent. When Sprague-Dawley rats received an intravenous injection of micafungin (1 mg/kg) in combination with cyclosporine, the cyclosporine significantly delayed the disappearance of micafungin from plasma and decreased the systemic clearance and volume of distribution at steady-state of micafungin to 54% and 65% of the corresponding control values, respectively. When Sprague-Dawley rats received a constant-rate infusion of micafungin, cyclosporine significantly decreased the steady-state biliary clearance of micafungin (similar to 80%). A significant decrease in the biliary clearance of micafungin (similar to 60%) was observed in Eisai hyperbilirubinemic rats, which have a hereditary deficiency in Mrp2. The present findings at least suggest that Mrp2 is involved mainly in the hepatobiliary excretion of micafungin in rats. (C) 2008 Elsevier Inc. All rights reserved.
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