. 2020 Oct 13;21(20):7537. doi: 10.3390/ijms21207537

Table 2.

Sphingosine-1-phosphate receptor (S1PR) modulators approved for multiple sclerosis (MS) treatment. Features: receptor affinity, half-life (t1/2), time to reach the highest plasma concentration (Tmax), required phosphorylation (pro-drug), and indication for MS treatment (relapsing-remitting MS (RRMS); secondary progressive MS (SPMS) and clinically isolated syndrome (CIS)).

Compound	Receptor Affinity		T_1/2 (Hours)	T_max (Hours)	Pro-Drug (Phosphorylation)	Indication	References
Compound	High	Low	T_1/2 (Hours)	T_max (Hours)	Pro-Drug (Phosphorylation)	Indication	References
Fingolimod (FTY720 Gilenya) Novartis^©	S1PR1 (EC₅₀ = 0.3 nM) S1PR3 (EC₅₀ = 0.9 nM) S1PR5 (EC₅₀ = 0.50 nM)	S1PR2 (EC₅₀ > 10,000 nM) S1PR4 (EC₅₀ = 345 nM)	144–216	12–16	+	RRMS	[99,100,101]
Siponimod (BAF312 Mayzent) Novartis^©	S1PR1 (EC₅₀ = 0.39 nM) S1PR5 (EC₅₀ = 0.38 nM)	S1PR2 (EC₅₀ > 10,000 nM) S1PR3 (EC₅₀ > 1000 nM) S1PR4 (EC₅₀ > 750 nM)	26–33	6–8	-	RRMS SPMS CIS	[102,103,104,105]
Ozanimod (RPC1063 Zeposia) Celgene^©	S1PR1 (EC₅₀ = 0.41 nM) S1PR5 (EC₅₀ = 11 nM)	S1PR2 (EC₅₀ > 10,000 nM) S1PR3 (EC₅₀ > 10,000 nM) S1PR4 (EC₅₀ > 7 nM)	15–17	8–12	-	RRMS SPMS CIS	[101,106]