Immunosuppressive agents in solid organ transplantation: Mechanisms of action and therapeutic efficacy

Crit Rev Oncol Hematol. 2005 Oct;56(1):23-46. doi: 10.1016/j.critrevonc.2005.03.012.


Effective immunosuppression is an essential pre-requisite for successful organ transplantation and improvements in outcome after transplantation have to a large extent been dependent on developments in immunosuppressive therapy. Here we provide an overview of the different immunosuppressive agents currently used in solid organ transplantation. A historical perspective on the development of immunosuppression for organ transplantation is followed by a review of the individual agents, with a focus on their mechanism of action and efficacy. Steroids, anti-proliferative agents (azathioprine and mycophenolate), calcineurin inhibitors (cyclosporine and tacrolimus) and TOR inhibitors (sirolimus and everolimus) are discussed along with both polyclonal and monoclonal antibody preparations. Many of the key clinical trials that underpin current clinical usage of these agents are described and side-effects of the different agents are highlighted. Finally, a number of newer agents still in various stages of clinical development are briefly considered.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Drug Design*
  • Drug Monitoring / methods
  • Humans
  • Immunosuppression Therapy* / methods
  • Immunosuppression Therapy* / trends
  • Immunosuppressive Agents / adverse effects
  • Immunosuppressive Agents / pharmacokinetics*
  • Immunosuppressive Agents / therapeutic use*
  • Organ Transplantation* / methods
  • Organ Transplantation* / trends
  • Treatment Outcome


  • Immunosuppressive Agents