DESCRIPTION Ponesimod (ACT-128800) is an orally active sphingosine-1-phosphate (S1P) receptor modulator that was developed as a disease-modifying therapy (DMT) for multiple sclerosis (MS). The compound is reported as a partial S1P₄ and S1P₅ receptor agonist, with maximum activity 18% and 42% of that induced by the endogenous ligand S1P (at 10μM ACT-128800) .
The INN record for ponesimod stipulates the (2R) stereoisomer ((2Z,5Z)-5-{3-chloro-4-[(2R)-2,3-dihydroxypropoxy]phenylmethylidene}-3-(2-methylphenyl)-2-(propylimino)-1,3-thiazolidin-4-one).
Selective SIP₁ receptor agonists are being developed and investigated for immunomodulatory/immunosuppressant potential in autoimmune diseases. (GtoPdb)

DESCRIPTION Ponesimod is an orally active and selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator that acts as a functional antagonist. It has potential immunomodulating activity. It may be used as a new therapeutic approach in lymphocyte-mediated autoimmune diseases. It is also an experimental drug for the treatment of multiple sclerosis (MS) and psoriasis. It protects against lymphocyte-mediated tissue inflammation. It activated S1P(1)-mediated signal transduction with high potency (EC(50) of 5.7 nM) and selectivity in vitro. It prevented edema formation, inflammatory cell accumulation and cytokine release in the skin of mice with delayed-type hypersensitivity. It also prevented the increase in paw volume and joint inflammation in rats with adjuvant-induced arthritis. It reduces both the amount of circulating peripheral lymphocytes and the infiltration of lymphocytes into target tissues by preventing egress of lymphocytes. It was developed by Actelion. It is in Clinical stage three. (BOC Sciences Bioactive Compounds)