Abstract：
: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 (approximately 80%). A significant decrease in the biliary clearance of micafungin (~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.
journal_name
Life Scijournal_title
Life sciencesauthors
Abe F,Ueyama J,Kimata A,Kato M,Hayashi T,Nadai M,Saito H,Takeyama N,Noguchi H,Hasegawa Tdoi
10.1016/j.lfs.2008.06.013subject
Has Abstractpub_date
2008-08-15 00:00:00pages
229-35issue
7-8eissn
0024-3205issn
1879-0631pii
S0024-3205(08)00236-1journal_volume
83pub_type
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