Drug Metabolism and Pharmacokinetics
Online ISSN : 1880-0920
Print ISSN : 1347-4367
ISSN-L : 1347-4367
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Larger Dosage Required for Everolimus than Sirolimus to Maintain Same Blood Concentration in Two Pancreatic Islet Transplant Patients with Tacrolimus
Eriko SATOIkuko YANOMasahiro SHIMOMURASatohiro MASUDAToshiya KATSURAShin-ichi MATSUMOTOTeru OKITSUYasuhiro IWANAGAShinji UEMOTOKen-ichi INUI
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2009 Volume 24 Issue 2 Pages 175-179

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Abstract

  We attempted a switch of mammalian target of rapamycin (mTOR) inhibitors from sirolimus to everolimus, a derivative of sirolimus and now on the market in Japan, in two pancreatic islet transplant patients. Both patients were administered tacrolimus with sirolimus or everolimus. They had been administered 5 or 9 mg sirolimus once a day and had maintained a trough concentration of about 15 ng/mL as measured by high performance liquid chromatography with ultraviolet detection. After the switch from sirolimus to everolimus, they were given 10 or 12 mg/day of everolimus twice a day to maintain a trough concentration of 12-15 ng/mL as measured by a fluorescence polarization immunoassay (FPIA) method. Afterward, the blood concentrations of everolimus and sirolimus after the conversion were measured by high performance liquid chromatography with mass spectrometry and everolimus concentrations were found to be 5-10 ng/mL. These data show that a larger dosage is needed for everolimus than sirolimus to maintain the same trough blood concentration. Data obtained by the FPIA for everolimus should be carefully evaluated after switching from sirolimus to everolimus because of the cross-reactivity of the antibody with sirolimus.

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© 2009 by The Japanese Society for the Study of Xenobiotics
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