Mayzent selectively binds to S1P1 and
S1P5 receptors.
Celgene announced additional phase III data analyses evaluating the efficacy and safety of ozanimod, a novel, oral, selective sphingosine 1-phosphate 1, or S1P1, and 5, or
S1P5, receptor modulator, versus interferon beta-1a in patients with relapsing multiple sclerosis, or RMS.
S1P acts through five specific receptors (S1P1, S1P2, S1P3, S1P4, and
S1P5) [55-57].
In general S1P elicits a wide variety of cellular responses including inflammation and can act intracellularly as a second messenger or extracellularly by binding to the G protein-coupled receptors S1P1 to
S1P5 [86, 87].
E-Scape's lead programme, an S1P5 receptor agonist for neuronopathic lysosomal storage disorders, will be in clinical development in 2019.
The company's drug development pipeline includes small molecules targeting known genetic drivers of CNS disorders including an S1P5 agonist for the treatment of CNS lysosomal storage disorders, a Parkinson's disease program targeting LRRK2, and an Alzheimer's disease program targeting ApoE4.
Tang et al., "Extrinsic sphingosine 1-phosphate activates
S1P5 and induces autophagy through generating endoplasmic reticulum stress in human prostate cancer PC-3 cells," Cellular Signalling, vol.
Rivera et al., "T-bet-dependent
S1P5 expression in NK cells promotes egress from lymph nodes and bone marrow," The Journal of Experimental Medicine, vol.