Rapamune (RAPA, rapamycin, sirolimus): mechanism of action immunosuppressive effect results from blockade of signal transduction and inhibition of cell cycle progression

Clin Biochem. 1998 Jul;31(5):335-40. doi: 10.1016/s0009-9120(98)00045-9.


Rapamune is a novel immunosuppressive agent in Phase III clinical trial in renal transplantation. Its unique mechanism of action has created great interest in its use as a biochemical probe of signal transduction pathways that has provided insight into its molecular mechanism of action. This article reviews the current state of our understanding of the mechanism of action of rapamune.

Publication types

  • Review

MeSH terms

  • Animals
  • Cell Cycle / drug effects
  • Humans
  • Immunosuppressive Agents / pharmacology*
  • Immunosuppressive Agents / therapeutic use*
  • Kidney Transplantation / immunology*
  • Lymphocyte Activation
  • Models, Biological
  • Ribosomal Protein S6 Kinases / metabolism
  • Signal Transduction / drug effects
  • Sirolimus / pharmacology*
  • Sirolimus / therapeutic use*
  • T-Lymphocytes / drug effects
  • T-Lymphocytes / immunology


  • Immunosuppressive Agents
  • Ribosomal Protein S6 Kinases
  • Sirolimus