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. 2021 Oct 26;12:733285. doi: 10.3389/fphar.2021.733285

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Copyright © 2021 Sallustio.

This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.

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Schematic representation of tacrolimus (Tac) distribution within whole blood showing binding to FKBP12 (FKBP), high density lipoproteins (HDL) and alpha-1 acid glycoprotein (α1-AGP). The large rectangle is divided into sections whose area approximates relative distribution between erythrocytes, plasma proteins and plasma water (unbound tacrolimus). The PBMC compartment is not shown and represents < 1% of tacrolimus in whole blood. Blue arrows indicate distribution into: lymphocytes, where biding with FKBP12 results in inhibition of calcineurin and prevention of rejection; liver, the primary site of clearance; and kidneys, where binding with FKBP12 and inhibition of calcineurin may be associated with nephrotoxicity.