Etrasimod

Etrasimod is a pivotal pharmaceutical active ingredient and research compound in immunology and inflammatory bowel disease, functioning as a highly selective S1P receptor modulator . As the first high-selectivity oral S1P receptor-targeted therapy for ulcerative colitis, Etrasimod offers a novel mechanism of action by partially and reversibly blocking lymphocyte egress from lymphoid tissues, thereby reducing the migration of inflammatory lymphocytes to the gut . This targeted approach means that Etrasimod can provide effective immunomodulation while minimizing the risk of bradycardia and pulmonary function impairment associated with S1P₂ and S1P₃ receptor engagement . In preclinical studies, Etrasimod (1 mg/kg, i.v.) decreases peripheral lymphocytes in mouse, rat, dog, and monkey models with IC50 values of 101, 51, 58, and 98 nM, respectively . Etrasimod has also demonstrated efficacy in delaying or preventing the onset and severity of murine experimental autoimmune encephalomyelitis (EAE) at doses of 0.3, 1, or 3 mg/kg, and has shown activity in rat models of collagen-induced arthritis . The compound's favorable pharmacokinetic profile and oral bioavailability make Etrasimod an invaluable tool for both mechanistic studies of S1P signaling and as a reference standard for analytical method development .

Product Parameters

S1P receptor modulators

Etrasimod (formerly known by the code name APD-334) is an oral selective sphingosine-1-phosphate (S1P) receptor modulator discovered by Arena Pharmaceuticals and developed by Pfizer; in October 2023, it received FDA approval in the United States for the treatment of moderate-to-severe active ulcerative colitis in adults.

Pharmacological Action

Etrasimod is a novel oral, selective 1-phosphorylated sphingosine (S1P) receptor modulator that partially reversibly blocks lymphocyte egress, reduces the number of lymphocytes in peripheral blood, thereby decreasing lymphocyte migration to the intestine and exerting its therapeutic effects. Compared with other S1P modulators (such as cinemizumab), etrasimod avoids binding to S1P₂/S1P₃ receptors, thereby reducing the risk of adverse effects such as bradycardia and pulmonary function impairment. As the first highly selective S1P receptor-targeted drug for ulcerative colitis, its oral administration route significantly improves patient adherence, representing a major advancement in the treatment of immune-mediated inflammatory diseases.

Synthetic Route

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Understanding the complexities of S1P receptor pharmacology requires tools you can trust—and Cosperpharm is here to provide them. Get in touch to learn how we can support your research with Etrasimod that meets the highest standards of purity and traceability.