About the Investigational Medication

Etrasimod (APD334), is an oral, next generation, selective sphingosine 1-phosphate (S1P) 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. Etrasimod exhibits potentially best in class pharmacokinetics and pharmacodynamics with rapid onset of action and rapid recovery of t-lymphocytes. 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.

Etrasimod is an investigational compound not approved for any use in any country.

About Ulcerative Colitis

Ulcerative colitis (UC) is a chronic disease that affects the large intestine. The innermost lining of the large intestine becomes inflamed and ulcers may form on the surface, which can cause symptoms such as frequent bowel movements, diarrhea and bloody stools. The inflammation is usually found in the rectum and can include all or a portion of the colon. Currently available treatment options have limitations in terms of side effects, patient response, efficacy and administration. We believe that an effective, oral, selective S1P receptor modulator that provides clinical benefits without current limitations has the potential to improve treatment for patients with ulcerative colitis.

Phase 3 planning is ongoing.

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