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

Objective: 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.