Etrasimod

Etrasimod is an orally bioavailable and potent antagonist of sphingosine-1-phosphate (S1P) receptors with EC₅₀ values of 0.093, 0.44, 0.32, 0.34, and 0.32 nM for human, mouse, rat, dog, and monkey S1P₁ receptors.¹ It is selective for S1P₁, S1P₄, and S1P₅ receptors with EC₅₀ values of 6.1, >10,000, >10,000, 147, and 24.4 nM for S1P_1-5, respectively, in a β-arrestin assay. Etrasimod (1 mg/kg, i.v.) decreases peripheral lymphocytes in mouse, rat, dog, and monkey (IC₅₀s = 101, 51, 58, and 98 nM, respectively). It delays or prevents the onset and severity of murine experimental autoimmune encephalomyelitis (EAE) when administered at 0.3, 1, or 3 mg/kg. It also leads to lower EAE disease scores relative to vehicle when administered after disease onset and is efficacious in a rat model of collagen-induced arthritis.

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1. Buzard, D.J., Kim, S.H., Lopez, L., et al. Discovery of APD334: Design of a clinical stage functional antagonist of the sphingosine-1-phosphate-1 receptor. ACS Med. Chem. Lett. 5(12), 1313-1317 (2014).