Description
InformationOzanimod (RPC1063) Ozanimod (RPC1063) is a selective oral S1P Receptor 1 modulator. Phase 3.TargetsS1P1R (Cell-free assay); S1P5R (Cell-free assay) 0.41 nM(EC50); 11 nM(EC50)In vitroIn S1P1R-HEK293T cells, Ozanimod induces sustained S1P1R internalization and degradation.In vivoOzanimod shows high oral bioavailability and volume of distribution. In a MOG-induced EAE mouse model, Ozanimod (3 mg/kg, p.o.) suppresses clinical symptoms. In a rat TNBS model of inflammatory bowel disease, Ozanimod (1.2 mg/kg, p.o.) inhibits clinical and histological disease scores. In a Naïve CD4+CD45Rbhi T cell adoptive transfer model, Ozanimod (1.2 mg/kg, p.o.) also significantly reduced disease severity as assessed by measuring the degree of inflammation, gland loss, hyperplasia, neutrophil infiltrate and mucosal thickness