RT Book, Section
A1 Bauer, Larry A.
SR Print(0)
ID 1106304470
T1 Sirolimus
T2 Applied Clinical Pharmacokinetics, 3e
YR 2015
FD 2015
PB McGraw-Hill Medical
PP New York, NY
SN 9780071794589
LK accesspharmacy.mhmedical.com/content.aspx?aid=1106304470
RD 2024/04/16
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.