Etrasimod is an investigational-stage, oral, next-generation, sphingosine-1-phosphate receptor modulator with improved pharmacology and pharmacokinetics intended for the treatment of autoimmune diseases.
The study is a 12-week, randomized, double-blind, placebo-controlled, parallel-group, dose-ranging trial evaluating safety and tolerability. Efficacy endpoints include improvement in the Mayo clinical score (3-component, total), response, remission and mucosal healing versus placebo, and dose response.
The study enrolled 157 patients globally with moderate to severe UC (3-component Mayo score of 4-9 that includes endoscopic sub score >2, rectal bleeding score >1).
Etrasimod (APD334), is an oral, next generation, selective sphingosine 1-phosphate receptor modulator, discovered by Arena, designed to provide systemic and local cell modulation by selectively targeting S1P receptor subtypes 1, 4 and 5, while avoiding subtypes 2, 3.
Selective binding with S1PR1 is believed to inhibit a specific subset of activated lymphocytes from migrating to sites of inflammation. The result is a reduction of circulating T and B lymphocytes that leads to anti-inflammatory activity. Importantly, immune surveillance is maintained.
The receptor subtypes 4, 5 exhibit similar activity on additional proliferating immune cell types. Optimized pharmacology and pharmacokinetics may allow superior clinical utility across a broad range of autoimmune conditions.
Arena Pharmaceuticals is focused on developing small molecule drugs with optimized receptor pharmacology designed to deliver broad clinical utility across multiple therapeutic areas.
Its proprietary pipeline includes potentially first- or best-in-class programs for which it owns global commercial rights.
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