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, and atopic dermatitis.

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.

Status

Ulcerative Colitis

We have received positive Phase 2 results for etrasimod and have initiated a Phase 3 global program – ELEVATE UC.  In March 2018, we completed a dose finding randomized, double-blind, placebo-controlled multinational Phase 2 clinical trial of etrasimod in moderate to severe UC. The aim of the trial includes investigating a clear dose response and establishing a clinically meaningful signal for the active arm(s) from placebo. The trial is expected to evaluate the effects of etrasimod, 1 mg and 2 mg, versus placebo on multiple efficacy measures including a 3-component Mayo Score, total Mayo Score (TMS), clinical remission and clinical response in up to 160 patients. Subjects from this study have the possibility to continue after 12 weeks in an open label extension study for up to 46 weeks with the focus on safety and maintenance of therapeutic effect.

Crohn’s Disease

In light of the overwhelmingly positive Phase 2 data in UC, we have initiated a program in Crohn’s disease. Phase 2/3 planning is ongoing.

Atopic Dermatitis

The Phase 2 ADVISE trial is ongoing.

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

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

Last updated as of 8/7/19