Overview
Etrasimod is a synthetic next-generation selective Sphingosine 1-phosphate (S1P) receptor modulator that targets the S1P with no detectable activity on S1P and S1P receptors. S1P receptors are membrane-derived lysophospholipid signaling molecules that are involved in the sequestration of circulating peripheral lymphocytes in lymph nodes. Therefore, S1P receptor modulators like etrasimod were investigated in treating immune-mediated diseases like ulcerative colitis where a high level of inflammatory T cells is present in the gastrointestinal tract, thus causing diffuse mucosal inflammation. In fact, it has been observed that antigen-activated T cells within peripheral lymphoid organs can transiently downregulate S1P receptor levels to facilitate immune cells trafficking into the intestinal mucosa. Etrasimod was approved on October 13, 2023, by the FDA under the brand name VELSIPITY for the treatment of adults with moderately to severely active ulcerative colitis. This approval was based on favorable results obtained from Pfizer’s Elevate UC Phase III registrational program, consisting of the Elevate UC 52 and Elevate UC 12 clinical trials, that investigates the efficacy of a 2-mg daily dose regimen of etrasimod, with a 32% and 26% remission rate observed in UC 52 and UC 12 trials respectively.
Background
Etrasimod is a synthetic next-generation selective Sphingosine 1-phosphate (S1P) receptor modulator that targets the S1P with no detectable activity on S1P and S1P receptors. S1P receptors are membrane-derived lysophospholipid signaling molecules that are involved in the sequestration of circulating peripheral lymphocytes in lymph nodes. Therefore, S1P receptor modulators like etrasimod were investigated in treating immune-mediated diseases like ulcerative colitis where a high level of inflammatory T cells is present in the gastrointestinal tract, thus causing diffuse mucosal inflammation. In fact, it has been observed that antigen-activated T cells within peripheral lymphoid organs can transiently downregulate S1P receptor levels to facilitate immune cells trafficking into the intestinal mucosa. Etrasimod was approved on October 13, 2023, by the FDA under the brand name VELSIPITY for the treatment of adults with moderately to severely active ulcerative colitis. This approval was based on favorable results obtained from Pfizer’s Elevate UC Phase III registrational program, consisting of the Elevate UC 52 and Elevate UC 12 clinical trials, that investigates the efficacy of a 2-mg daily dose regimen of etrasimod, with a 32% and 26% remission rate observed in UC 52 and UC 12 trials respectively.
Indication
Etrasimod is indicated for the treatment of moderately to severely active ulcerative colitis (UC) in adults.
Associated Conditions
- Moderately to Severely Active Ulcerative Colitis
Research Report
Etrasimod (VELSIPITY™): A Comprehensive Pharmacological and Clinical Review for Ulcerative Colitis
1. Introduction to Etrasimod (VELSIPITY™)
1.1. Overview and Therapeutic Class
Etrasimod, marketed under the brand name VELSIPITY™, is an orally administered small molecule medication.[1] It is identified by DrugBank ID DB14766 and CAS Number 1206123-37-6.[1] Etrasimod is classified as a synthetic, next-generation selective sphingosine-1-phosphate (S1P) receptor modulator.[4] This agent was initially discovered by Arena Pharmaceuticals, with subsequent development undertaken by Pfizer.[1]
1.2. Approved Indication (Ulcerative Colitis)
Etrasimod is primarily indicated for the treatment of moderately to severely active ulcerative colitis (UC) in adult populations.[1] In certain jurisdictions, such as the European Union and Canada, this indication is extended to include patients 16 years of age and older who have demonstrated an inadequate response, experienced a loss of response, or were intolerant to either conventional therapy or an advanced treatment modality, such as a biologic agent or a Janus kinase (JAK) inhibitor.[3]
Ulcerative colitis is a chronic, immune-mediated inflammatory bowel disease (IBD) characterized by diffuse mucosal inflammation predominantly affecting the colon and rectum. The clinical manifestations of UC are burdensome and include persistent diarrhea, often with blood and mucus, abdominal pain, rectal urgency, and systemic symptoms such as fatigue and weight loss.[8]
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2024/07/26 | Phase 2 | Recruiting | |||
2024/05/03 | N/A | Recruiting | |||
2024/03/06 | N/A | Recruiting | |||
2023/11/18 | Phase 1 | Completed | |||
2023/09/06 | N/A | AVAILABLE | |||
2023/07/21 | Phase 1 | Completed | |||
2023/02/17 | Phase 2 | Terminated | |||
2022/03/18 | Phase 2 | Recruiting | |||
2021/09/29 | Phase 2 | Completed | |||
2021/01/13 | Phase 3 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| No FDA approvals found for this drug. | |||||
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| VELSIPITY FILM-COATED TABLET 2 MG | SIN17015P | TABLET, FILM COATED | 2 mg | 5/30/2024 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| No TGA approvals found for this drug. | |||||