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Etrasimod (etrasimod)
Etrasimod is an S1P receptor modulator that blocks lymphocyte egress from lymphoid organs, reducing peripheral blood lymphocytes.
VELSIPITY (etrasimod) is an S1P receptor modulator indicated for moderately to severely active ulcerative colitis in adults. The drug demonstrates moderate efficacy through lymphocyte sequestration with a favorable pharmacokinetic profile (30-hour half-life, once-daily dosing). Significant risks include cardiac conduction abnormalities and QT prolongation, requiring careful patient selection and cardiologist consultation in high-risk populations. The drug represents an important oral alternative for UC management with manageable drug interactions primarily through CYP450 pathways.
At a glance
| Generic name | etrasimod |
|---|---|
| Sponsor | Pfizer |
| Drug class | Sphingosine 1-phosphate receptor modulator |
| Target | Sphingosine 1-phosphate (S1P) receptors 1, 4, and 5 |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 2023 |
Mechanism of action
Etrasimod binds with high affinity to S1P receptors 1, 4, and 5, with minimal activity on S1P3 (25-fold lower than Cmax at recommended dose) and no activity on S1P2. The drug partially and reversibly blocks the capacity of lymphocytes to egress from lymphoid organs, resulting in reduced numbers of lymphocytes in peripheral blood. The mechanism by which etrasimod exerts therapeutic effects in ulcerative colitis is unknown but may involve the reduction of lymphocyte migration into the intestines.
Approved indications
- Moderate to severe ulcerative colitis
- Induction of remission in adults with moderately to severely active ulcerative colitis
- Maintenance of clinical response and endoscopic remission in adults with moderately to severely active ulcerative colitis
- Moderate to severe Crohn's disease
- Induction of clinical remission in adults with moderately to severely active Crohn's disease
- Maintenance of clinical response and endoscopic remission in adults with moderately to severely active Crohn's disease
Common side effects
- Headache
- Elevated liver tests
- Dizziness
- Arthralgia
- Hypertension
- Urinary tract infection
- Nausea
- Hypercholesterolemia
- Herpes viral infection
- Headache
Drug interactions
- Fluconazole (moderate CYP2C9 and CYP3A4 inhibitor)
- Rifampin (strong CYP3A4, moderate CYP2C8 and CYP2C9 inducer)
- Class Ia and Class III anti-arrhythmic drugs and QT prolonging drugs
- Beta-blockers or Calcium channel blockers
Key clinical trials
- Etrasimod as Prevention of Pouchitis (PHASE2)
- A Study of How the Medicine Called "Etrasimod" Works in Children With the Gut Disease Called Ulcerative Colitis (PHASE2)
- An Observational Study to Learn About Velsipity After Long Term Use in Patients With Ulcerative Colitis
- Describing Treatment Patterns and Creating an Updated Treatment Flow in an Ulcerative Colitis Population
- A Study to Evaluate Etrasimod Treatment in Adolescents With Ulcerative Colitis (PHASE2)
- Etrasimod for Immune Checkpoint Inhibitor Diarrhea and Colitis (PHASE2)
- An Extension Study for Treatment of Moderately to Severely Active Ulcerative Colitis (PHASE3)
- Efficacy and Safety of Etrasimod in Elderly Patients With Ulcerative Colitis (NA)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Etrasimod CI brief — competitive landscape report
- Etrasimod updates RSS · CI watch RSS
- Pfizer portfolio CI