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Role of FK506 Binding Protein on Tacrolimus Distribution in Red Blood Cells

Pharmaceutical Research, 2020
Tacrolimus is distributed mainly in red blood cells (RBCs) after transfer into blood. This study aimed to evaluate the effect of FK506-binding proteins (FKBPs) on RBC distribution of tacrolimus in a physiological environment.Human RBCs were isolated from fresh blood samples from healthy volunteers.
Nobuhiro Matsumoto   +2 more
exaly   +3 more sources

Validation of methods to study the distribution and protein binding of tacrolimus in human blood

Journal of Pharmacological and Toxicological Methods, 2001
Tacrolimus is a macrolide immunosuppressant that has a narrow therapeutic index, displays considerable variability in response, and has the potential for serious drug interactions. Therapeutic drug monitoring and dose individualisation for tacrolimus is complicated but essential.
Andrew Mclachlan, K F Brown
exaly   +3 more sources

Equilibrium studies of a fluorescent tacrolimus binding to surfactant protein A

Analytical Biochemistry, 2005
Tacrolimus (FK506) is a hydrophobic immunosuppressive agent used in kidney, liver, and lung transplantation. The objective of this study was to characterize the binding of FK506 to surfactant protein A (SP-A), an abundant lipoprotein found in the alveolar fluid that functions as part of the innate immune system in the lung.
Alejandra Saenz   +2 more
exaly   +3 more sources

Effect of Tacrolimus on Activity and Expression of P-Glycoprotein and ATP-Binding Cassette Transporter A5 (ABCA5) Proteins in Hematoencephalic Barrier Cells

open access: yesBiological and Pharmaceutical Bulletin, 2008
Tacrolimus is an agent used in clinical immunosuppressive drug therapies. A wide spectrum of adverse effects has been reported in association with this immunosuppressor, including neurotoxic effect. The upper limit of therapeutic blood concentrations of tacrolimus has been described as 30 ng/ml in immunosuppressed patients.
Juan Guillermo Carcamo
exaly   +4 more sources

Plasma Protein Binding of Tacrolimus in Humans

Journal of Pharmaceutical Sciences, 1993
An ultracentrifugation method was used for the determination of the tacrolimus (FK 506) free fraction in plasma. Samples of 400 microL were centrifuged for 6 h at 160,000 x g, and concentrations of [3H]tacrolimus were measured in the original plasma and in the second layer of the supernatant.
Wojciech Piekoszewski, William Jusko
exaly   +3 more sources

Sirolimus and tacrolimus binding proteins: double-edged swords for GVHD prophylaxis

Blood, 2003
Postgrafting immunosuppression is the main approach for the prevention of graft-versus-host disease (GVHD) after allogeneic blood or marrow transplantation. Controlled trials have found that the combination of cyclosporine, a calcineurin inhibitor that reduces T-cell cytokine gene activation ...
Hans-Peter Kiem   +2 more
exaly   +2 more sources

Binding of Pimecrolimus and Tacrolimus to Skin and Plasma Proteins: Implications for Systemic Exposure after Topical Application

Drug Metabolism and Disposition, 2008
Pimecrolimus and tacrolimus are calcineurin inhibitors used for the topical treatment of atopic dermatitis. Although structurally similar, they display specific differences including higher lipophilicity and lower skin permeation of pimecrolimus. The aim of the present study was to understand the reason for the differences in skin permeation; in ...
Andreas Billich, Anton Stuetz
exaly   +3 more sources

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