Abstract::FTY720 is an analog of sphingosine-1-phosphate (S1P) derived from the ascomycete
Cordyceps sinensis. As a new immunosuppressant, FTY720 is widely used to treat multiple sclerosis.
FTY720 binds to the S1P receptor after phosphorylation, thereby exerting immunosuppressive
effects. The nonphosphorylated form of FTY720 can induce cell apoptosis, enhance chemotherapy
sensitivity, and inhibit tumor metastasis of multiple tumors by inhibiting SPHK1 (sphingosine
kinase 1) and activating PP2A (protein phosphatase 2A) and various cell death pathways. FTY720
can induce neutrophil extracellular traps to neutralize and kill pathogens in vitro, thus exerting anti-
infective effects. At present, a series of FTY720 derivatives, which have pharmacological effects
such as anti-tumor and alleviating airway hyperresponsiveness, have been developed through
structural modification. This article reviews the pharmacological effects of FTY720 and its derivatives.