Role of Mrp2 in the hepatic disposition of mycophenolic acid and its glucuronide metabolites: effect of cyclosporin
نویسندگان
چکیده
Department of Clinical Pharmacology, The Queen Elizabeth Hospital, Woodville, South Australia, Australia, 5011 (ISW, RGM, BCS); Department of Clinical and Experimental Pharmacology, University of Adelaide, Adelaide, South Australia, Australia, 5000 (RGM, BCS); School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, South Australia, Australia, 5000 (ISW, LRB, AME). DMD Fast Forward. Published on November 4, 2005 as doi:10.1124/dmd.105.006122
منابع مشابه
Role of Mrp2 in the hepatic disposition of mycophenolic acid and its glucuronide metabolites: effect of cyclosporine.
Mycophenolic acid (MPA) is part of the immunosuppressant therapy for transplant recipients. This study examines the role of the canalicular transporter, Mrp2, and the effect of cyclosporin A (CsA), on the biliary secretion of the ether (MPAGe) and acyl (MPAGa) glucuronides of MPA. Isolated livers from Wistar rats (n = 6), or Wistar TR- rats (n = 6) were perfused with MPA (5 mg/l). A third group...
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The drug pump protein MRP2 is a membrane drug efflux transporter widely distributed in normal and tumor tissues. Its role is thought to be crucial for the disposition of many drugs and their substrates in different tissues. In this study, we aimed to examine the effects of systematic inflammation induced by lipopolysaccharide (LPS) on the expression and function of this transporter in rats. Jug...
متن کاملExpression of Drug Pump Protein MRP2 in Lipopolysaccharide-Treated Rats and Its Impact on the Disposition of Acetaminophen
The drug pump protein MRP2 is a membrane drug efflux transporter widely distributed in normal and tumor tissues. Its role is thought to be crucial for the disposition of many drugs and their substrates in different tissues. In this study, we aimed to examine the effects of systematic inflammation induced by lipopolysaccharide (LPS) on the expression and function of this transporter in rats. Jug...
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The onset of diarrhea after the administration of mycophenolate mofetil (MMF) is possibly associated with the biliary excretion of its metabolite, mycophenolic acid glucuronide (MPAG). This study was undertaken to clarify the mechanism underlying the biliary excretion of MPAG. Intravenously administered mycophenolic acid (MPA, 5 mg/kg) rapidly disappeared from plasma and was efficiently excrete...
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PKI166, a specific inhibitor of the tyrosine kinase activity of two epidermal growth factor receptors, was under development for the treatment of cancer. In preclinical studies PKI166 was mainly cleared by metabolism, and its metabolites were eliminated by biliary excretion, emphasizing the role of liver transport processes for its disposition. Here the transport properties of [14C]PKI166 and i...
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