Ozanimod (RPC-1063) is a potent, selective agonist of S1P1 and S1P5 receptor with EC50 of 0.41 nM and 11 nM respectively.
Ozanimod (RPC-1063) is less potent for S1P2, S1P3 and S1P4 (EC50> 10 uM).
Ozanimod (RPC-1063) induces S1P1 receptor internalization and induced a reversible reduction in circulating B and CCR7(+) T lymphocytes in vivo.
Ozanimod (RPC-1063) shows high oral bioavailability and volume of distribution, and a circulatory half-life.
