TY - CHAP M1 - Book, Section TI - Sirolimus A1 - Bauer, Larry A. Y1 - 2015 N1 - T2 - Applied Clinical Pharmacokinetics, 3e AB - Sirolimus (also known as rapamycin) is a macrocyclic lactone-based mTOR (mammalian target of rapamycin) inhibitor that is used for the prevention of graft rejection in solid organ transplant patients.1 It is currently approved for use in renal transplant patients. It is also used to prevent rejection in 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 properties of sirolimus are due to its ability to block the effects of interleukin-2 on T-lymphocyte activation and proliferation.1,3 Sirolimus binds to FK-binding protein-12 (FKPB-12), an intracellular cytoplasmic protein found in T cells. The sirolimus-FKPB complex then binds to mTOR, which inhibits the reaction of the T cell to interleukin-2 binding to its outer cell wall. This action prevents T-cell proliferation and progression of the cell cycle. SN - PB - McGraw-Hill Medical CY - New York, NY Y2 - 2024/04/23 UR - accesspharmacy.mhmedical.com/content.aspx?aid=1106304470 ER -