Ceralifimod

Ceralifimod is an agonist of the sphingosine-1-phosphate (S1P) receptors S1P₁ and S1P₅ (K_is = 0.626 and 0.574 nM, respectively).¹ It is selective for S1P₁ and S1P₅ over S1P_2-4 (K_is = >5,450, >5,630, and 28.8 nM, respectively). Ceralifimod induces calcium influx in CHO-K1 cells overexpressing S1P₁ (EC₅₀ = 1 nM) and cAMP accumulation in CHO-K1 cells overexpressing S1P₁ or S1P₅ (EC₅₀s = 0.027 and 0.33 nM, respectively). In vivo, ceralifimod (0.03 and 0.1 mg/kg) reduces paw edema in a rat model of collagen induced arthritis (CIA). It also delays disease onset and inhibits lymphocyte infiltration of the spinal cord in a rat model of experimental autoimmune encephalomyelitis (EAE) and prevents disease relapse in a non-obese diabetic mouse model of relapsing-remitting EAE.²

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1. Kurata, H., Kusumi, K., Otsuki, K., et al. Discovery of a 1-methyl-3,4-dihydronaphthalene-based sphingosine-1-phosphate (S1P) receptor agonist ceralifimod (ONO-4641). A S1P₁ and S1P₅ selective agonist for the treatment of autoimmune disease. J. Med. Chem. 60(23), 9508-9530 (2017).

2. Komiya, T., Sato, K., Shioya, H., et al. Efficacy and immunomodulatory actions of ONO-4641, a novel selective agonist for sphingosine 1-phosphate receptors 1 and 5, in preclinical models of multiple sclerosis. Clin. Exp. Immunol. 171(1), 54-62 (2013).