Etrasimod

Drug Candidate for Treatment of Immune-Mediated and Inflammatory Diseases

Etrasimod is a next-generation, once-daily, oral, highly selective sphingosine 1-phosphate (S1P) receptor modulator discovered by Arena, and designed for optimized pharmacology and engagement of S1P receptor 1, 4 and 5 which may lead to an improved efficacy and safety profile.

Etrasimod provides systemic and local effects on specific immune cell types and has the potential to treat multiple immune-mediated inflammatory diseases, including ulcerative colitis, Crohn’s disease, atopic dermatitis and alopecia areata.

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

About Autoimmune Diseases

Autoimmune diseases are characterized by an inappropriate immune response against substances and tissues that are normally present in the body. In an autoimmune reaction, a person’s antibodies and immune cells target healthy tissues, triggering an inflammatory response. Reducing the immune and/or inflammatory response is an important goal in the treatment of autoimmune disease.

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.

About Crohn’s Disease

Crohn’s disease (CD) is a chronic inflammatory condition of the gastrointestinal tract. Crohn’s most commonly affects the end of the small bowel (the ileum) and the beginning of the colon, but it may affect any part of the gastrointestinal (GI) tract. Crohn’s disease can also affect the entire thickness of the bowel wall. Symptoms vary from patient to patient, but typically include persistent diarrhea, rectal bleeding, urgent need to move bowels, abdominal cramps and pain, constipation (can lead to bowel obstruction), fever, loss of appetite, weight loss, fatigue and night sweats. In more severe cases, Crohn’s can lead to tears (fissures) in the lining of the anus, which may cause severe pain and bleeding. Inflammation may also cause a fistula to develop which can be very serious and require immediate medical attention. A large number of patients suffering from Crohn’s disease are given opioids to help manage their pain. Opioids can cause further irritation to the GI tract and are becoming strictly regulated due to high rates of addiction.

About Atopic Dermatitis

Atopic dermatitis (AD) is a serious, chronic immune-mediated disease in which symptoms vary, but often include severe dry skin, itching, patches, swollen skin and raised bumps which may leak fluid.

About Alopecia Areata

Alopecia areata (AA) is a T-cell-mediated autoimmune skin disorder with unmet medical need that causes non-scarring patchy hair loss, most often on the scalp. Mild disease typically presents as one or more round or oval bald patches on the scalp. In moderate-to-severe disease, extensive and chronic hair loss occurs, with the most severe forms involving hair loss on the entire scalp (alopecia totalis) or body (alopecia universalis). Patients with persistent moderate-to-severe AA also often suffer emotional and psychosocial distress and reduced quality of life as a result of their hair loss.

Status

Drug Candidate Disease Area Target Status
Etrasimod (APD334) Ulcerative Colitis ELEVATE UC 52 S1P Receptor Phase 3
Ulcerative Colitis ELEVATE UC 12 S1P Receptor Phase 3
Crohn’s Disease (CD) S1P Receptor Phase 2/3
Eosinophilic Esophagitis (EoE) S1P Receptor Phase 2b Planning
Atopic Dermatitis (AD) ADVISE S1P Receptor Phase 2b
Alopecia Areata (AA) S1P Receptor Phase 2
Retained Rights
Worldwide, excluding rights granted to Everest Medicines for Greater China & certain other Asian territories

Etrasimod has not been approved by the US Food and Drug Administration or any other regulatory agency.

Drug Candidate Disease Area Status
Etrasimod (APD334) Ulcerative Colitis  – ELEVATE UC 52 Ph 3
Ulcerative Colitis – ELEVATE UC 12 Ph 3
Crohn’s Disease (CD) Ph 2/3
Eosinophilic Esophagitis (EoE) Ph 2b Planning
Atopic Dermatitis (AD) ADVISE Ph 2b
Alopecia Areata (AA) Ph 2
Retained Rights
Worldwide, excluding rights granted to Everest Medicines for Greater China & certain other Asian territories

Visit https://clinicaltrials.gov/ for more information.

Last updated as of 10/7/20