Name Mechanism Disease References
FTY720 (Fingolimod,Gilenya) -Prodrug; phosphorylated by SphK2. -S1PR1, S1PR3-5 agonist - Downregulates S1P1 -FDA approved for multiple sclerosis* -Dermatitis, Arthritis, Allergy [13,80]
SK1-1 (BML-258) -SphK1 inhibitor -Glioblastoma -Leukemia [114,115]
Safingol L-threo-dihydrosphingosine -pan SphK inhibitor -Solid tumors(Phase 1)* [116]
SK1-2 SphK1 inhibitor Induces proteasomal and lysosomal degradation of SphK1 -Pancreatic cancer -Leukemia [117,118]
ABC294640 SphK2 inhibitor Estrogen receptor agonist -Cancer -Inflammatory bowel disease [119,120]
ABC294735 pan SphK inhibitor -Cancer [121]
SKI-II (SKI-2, SPHK I2) SphK1 inhibitor -Asthma [122]
THI 2-acetyl-4(5)-[1(R) S1P Lyase inhibitor -Ischemia/reperfusion injury [123]
LX2931 S1P Lyase inhibitor -Rheumatoid arthritis(Phase II) * [124]
SKI 5C SphK1 inhibitor -Sepsis [125]
SEW2871 S1PR1 agonist -Diabetic nephropathy -Renal protection [126,127]
JTE013 S1PR2 antagonist -Anaphylaxis -Cancer [128] [71]
AAL® Prodrug; phosphorylated by SphK2 S1PR1/S1PR3 agonist -Influenza [129]
AUY954 S1PR1 agonist -Experimental autoimmune neuritis [130]
Table 2: Small molecules targeting S1P and applications in health. *Effects in humans. All other compounds have only been tested in animal models.