TY - CHAP M1 - Book, Section TI - Tacrolimus A1 - Bauer, Larry A. Y1 - 2015 N1 - T2 - Applied Clinical Pharmacokinetics, 3e AB - Tacrolimus (also known as FK506) is a macrolide-based calcineurin inhibitor, with immunosuppressant actions, that is used for the prevention of graft rejection in solid organ transplant patients.1 Currently, it is approved for use in heart, liver, and renal transplant patients. It is also used in lung, heart-lung, and other solid organ transplant recipients, as well as the treatment of graft-versus-host disease in hematopoietic stem cell transplant patients.1,2 The immunomodulating effects of tacrolimus are due to its ability to block the production of interleukin-2 and other cytokines produced by T lymphocytes.1,2, and 3 Tacrolimus binds to FK-binding protein-12 (FKPB-12), an intracellular cytoplasmic protein found in T cells. The tacrolimus-FKPB complex interacts with calcineurin, inhibits the catalytic activity of calcineurin, and blocks the production of intermediaries involved with the expression of genes regulating the production of cytokines. SN - PB - McGraw-Hill Medical CY - New York, NY Y2 - 2024/04/19 UR - accesspharmacy.mhmedical.com/content.aspx?aid=1106304380 ER -