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Velsipity (Etrasimod Arginine)
Etrasimod binds S1P receptors 1, 4, and 5, blocking lymphocyte egress from lymphoid organs.
Velsipity (etrasimod) is an S1P receptor modulator indicated for moderately to severely active ulcerative colitis in adults, working by reducing lymphocyte migration into the intestines. The drug demonstrates favorable pharmacokinetics with a 30-hour half-life and dose-proportional exposure, though it requires careful monitoring for cardiac effects including bradycardia and AV conduction delays, particularly in patients on concurrent cardiac medications. Major safety concerns include infections, liver injury, macular edema, hypertension, and potential fetal risk, with the most common adverse reactions being headache, elevated liver tests, and dizziness. Clinical utility is supported by efficacy data from two randomized controlled trials, but requires baseline cardiac assessment and ongoing monitoring for serious adverse events.
At a glance
| Generic name | Etrasimod Arginine |
|---|---|
| Sponsor | Pfizer Inc. |
| Drug class | Sphingosine 1-phosphate receptor modulator |
| Target | Sphingosine 1-phosphate (S1P) receptors 1, 4, and 5 |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
Mechanism of action
Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5. It has minimal activity on S1P3 (25-fold lower than Cmax at the recommended dose) and no activity on S1P2. The drug partially and reversibly blocks the capacity of lymphocytes to egress from lymphoid organs, reducing the number 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 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 remission in adults with moderately to severely active Crohn's disease
Common side effects
- Headache
- Elevated liver tests
- Dizziness
- Arthralgia
- Nausea
- Hypertension
- Urinary tract infection
- Hypercholesterolemia
- Bradycardia
- Herpes viral infection
- Decrease in visual acuity
Serious adverse events
- Infections
- Bradyarrhythmia and Atrioventricular Conduction Delays
- Liver Injury
- Macular Edema
- Increased Blood Pressure
- Fetal Risk
- Cutaneous Malignancies
- Posterior Reversible Encephalopathy Syndrome
Drug interactions
- Class Ia anti-arrhythmic drugs (e.g., quinidine, procainamide)
- Class III anti-arrhythmic drugs (e.g., amiodarone, sotalol)
- QT prolonging drugs
- Beta-blockers or Calcium channel blockers
- Fluconazole (moderate CYP2C9 and CYP3A4 inhibitor)
- Rifampin (strong CYP3A4, moderate CYP2C8 and CYP2C9 inducer)
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 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:
- Velsipity CI brief — competitive landscape report
- Velsipity updates RSS · CI watch RSS
- Pfizer Inc. portfolio CI