Etrasimod

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5 (S1P 1,4,5 ). Etrasimod has minimal activity on S1P 3 (25-fold lower than C max at the recommended dose) and no activity on S1P 2 .

• VELSIPITY is indicated for the treatment of moderately to severely active ulcerative colitis (UC) in adults. VELSIPITY is a sphingosine 1-phosphate receptor modulator indicated for the treatment of moderately to severely active ulcerative colitis in adults.ICD-10: K51.90

• VELSIPITY is contraindicated in patients who: • In the last 6 months, have experienced a myocardial infarction, unstable angina pectoris, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure [see Warnings and Precautions (5.2) ] . • Have a history or presence of Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker [see Warnings and Precautions (5.2) ] .contraindicated

• Assessments are required prior to initiating VELSIPITY. ( 2.1 ) • The recommended dosage is 2 mg orally once daily. ( 2.2 ) 2.1 Assessments, Medications, and Vaccinations Prior to First Dose of VELSIPITY Before initiation of treatment with VELSIPITY, assess the following: Complete Blood Count Obtain a recent (i.e., within the last 6 months or after discontinuation of prior UC therapy) complete blood count (CBC), including lymphocyte count [see Warnings and Precautions (5.1) ]. Cardiac Evaluation Obtain an electrocardiogram (ECG) to determine whether preexisting conduction abnormalities are present. In patients with certain preexisting conditions, advice from a cardiologist should be sought [see Warnings and Precautions (5.2) ] . Liver Function Tests Obtain recent (i.e., within the last 6 months) transaminase and bilirubin levels [see Warnings and Precautions (5.3) ]. Ophthalmic Assessment Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with VELSIPITY [see Warnings and Precautions (5.4) ]. Skin Examination Obtain a skin examination prior to or shortly after initiation of VELSIPITY. If a suspicious skin lesion is observed, it should be promptly evaluated [see Warnings and Precautions (5.7) ] . Current or Prior Medications • Determine if patients are taking drugs that could slow heart rate or atrioventricular (AV) conduction [see Warnings and Precautions (5.2) and Drug Interactions (7) ].

• Infections : May increase the risk of infections. Obtain a complete blood count (CBC) before initiation of treatment. Monitor for infection during treatment and for 5 weeks after discontinuation. Consider interruption of treatment if a serious infection develops. Avoid use of live attenuated vaccines during and for up to 5 weeks after treatment. ( 5.1 ) • Bradyarrhythmia and Atrioventricular Conduction Delays : May result in a transient decrease in heart rate and AV conduction delays. Obtain an electrocardiogram (ECG) to assess for preexisting cardiac conduction abnormalities before starting treatment. Consider cardiology consultation for conduction abnormalities or concomitant use with other drugs that decrease heart rate. ( 2.1 , 5.2 , 7 ) • Liver Injury : Elevations of aminotransferases may occur. Obtain transaminase and bilirubin levels before initiating VELSIPITY. Discontinue if significant liver injury is confirmed. ( 2.1 , 5.3 ) • Macular Edema : May increase the risk of macular edema. Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with VELSIPITY. Periodically conduct an evaluation of the fundus, including the macula, while on therapy and any time there is a change in vision. Consider discontinuing VELSIPITY if macular edema develops. ( 2.1 , 5.4 ) • Increased Blood Pressure : Monitor blood pressure during treatment. ( 5.5 ) • Fetal Risk : May cause fetal harm.

The following serious adverse reactions are described elsewhere in the labeling: • Infections [see Warnings and Precautions (5.1) ] • Bradyarrhythmia and Atrioventricular Conduction Delays [see Warnings and Precautions (5.2) ] • Liver Injury [see Warnings and Precautions (5.3) ] • Macular Edema [see Warnings and Precautions (5.4) ] • Increased Blood Pressure [see Warnings and Precautions (5.5) ] • Fetal Risk [see Warnings and Precautions (5.6) ] • Cutaneous Malignancies [see Warnings and Precautions (5.7) ] • Posterior Reversible Encephalopathy Syndrome [see Warnings and Precautions (5.8) ] • Respiratory Effects [see Warnings and Precautions (5.9) ] • Unintended Additive Immune System Effects from Prior Treatment with Immunosuppressive or Immune-Modulating Drugs [see Warnings and Precautions (5.10) ] • Immune System Effects After Stopping VELSIPITY [see Warnings and Precautions (5.11) ] Most common adverse reactions (incidence ≥5%) are: headache, elevated liver tests, and dizziness. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Pfizer Inc. at 1-800-438-1985 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.

Severe Hepatic Impairment : Use is not recommended. ( 8.6 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in females exposed to VELSIPITY during pregnancy. Pregnant females exposed to VELSIPITY and healthcare providers are encouraged to contact the pregnancy registry by calling 1-800-616-3791. Risk Summary Based on findings from animal studies, VELSIPITY may cause fetal harm when administered to a pregnant woman. Available data from reports of pregnancies from the clinical development program with VELSIPITY are insufficient to identify a drug-associated risk of major birth defects, miscarriage or other adverse maternal or fetal outcomes. There are risks to the mother and the fetus associated with increased disease activity in women with inflammatory bowel disease during pregnancy (see Clinical Considerations ). In animal reproduction studies, administration of etrasimod during organogenesis produced adverse effects on development, including embryolethality and fetal malformations, in both rats and rabbits at maternal exposures 5 and 6 times, respectively, the exposure at the maximum recommended human dose (MRHD).

Metabolism

Etrasimod mean (SD) steady-state maximum plasma concentration (C max ) was 113 (27.5) ng/mL and area under the time concentration curve at the dosing interval (AUC tau ) was 2162 (488) ng*h/mL at the recommended dosage. Etrasimod C max and AUC are approximately dose proportional from 0.7 mg to 2 mg (0.35 times up to the recommended dosage).

• Oct 12, 2023NDANDA216956Pfizer

1. 1Drug Ineffective30119%
2. 2Condition Aggravated17311%
3. 3Headache936.0%
4. 4Dizziness925.9%
5. 5Colitis Ulcerative825.3%
6. 6Diarrhoea724.6%
7. 7Fatigue724.6%
8. 8Type 2 Diabetes Mellitus664.3%
9. 9Nausea583.7%
10. 10Malaise563.6%
11. 11Diabetic Eye Disease523.4%
12. 12Haematochezia513.3%
13. 13Colitis473.0%
14. 14Abdominal Pain442.8%
15. 15Rectal Haemorrhage392.5%

The 10 most recently updated of 31 ClinicalTrials.gov registrations naming Etrasimod as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Etrasimod as Prevention of Pouchitis
  Recruiting · Phase 2 · Interventional · 40 enrolled · Maia Kayal
  NCT07486921updated 2026-06-10
• A Study to Evaluate Etrasimod Treatment in Adolescents With Ulcerative Colitis
  Recruiting · Phase 2 · Interventional · 36 enrolled · Pfizer
  NCT05287126updated 2026-06-08
• An Observational Study to Learn About Velsipity After Long Term Use in Patients With Ulcerative Colitis
  Recruiting · Observational · 553 enrolled · Pfizer
  NCT07459686updated 2026-05-18
• Describing Treatment Patterns and Creating an Updated Treatment Flow in an Ulcerative Colitis Population
  Active not recruiting · Observational · 4,000 enrolled · Pfizer
  NCT07177209updated 2026-05-14
• An Extension Study for Treatment of Moderately to Severely Active Ulcerative Colitis
  Active not recruiting · Phase 3 · Interventional · 896 enrolled · Pfizer
  NCT03950232updated 2026-05-11
• A Study of How the Medicine Called "Etrasimod" Works in Children With the Gut Disease Called Ulcerative Colitis
  Recruiting · Phase 2 · Interventional · 24 enrolled · Pfizer
  NCT07470879updated 2026-05-06
• An Observational Study of Etrasimod in Adult Patients With Moderate to Severe Ulcerative Colitis
  Recruiting · Observational · 300 enrolled · Pfizer
  NCT06398626updated 2026-04-28
• A Study to Learn How the Study Medicine Called Etrasimod is Taken up Into Blood and Breastmilk of Healthy Breastfeeding Women
  Recruiting · Phase 1 · Interventional · 8 enrolled · Pfizer
  NCT07153159updated 2026-04-07
• A Study to Learn About the Effectiveness of Etrasimod in People With Ulcerative Colitis
  Recruiting · Observational · 360 enrolled · Pfizer
  NCT06294925updated 2026-03-30
• Etrasimod for Immune Checkpoint Inhibitor Diarrhea and Colitis
  Withdrawn · Phase 2 · Interventional · 0 enrolled · Yale University
  NCT06521762updated 2026-01-14

Frequently asked questions

How does Etrasimod work?

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5 (S1P 1,4,5 ). Etrasimod has minimal activity on S1P 3 (25-fold lower than C max at the recommended dose) and no activity on S1P 2 .

What is Etrasimod used for?

According to FDA labeling, Etrasimod carries indications including: VELSIPITY is indicated for the treatment of moderately to severely active ulcerative colitis (UC) in adults. VELSIPITY is a sphingosine 1-phosphate receptor modulator indicated for the treatment of moderately to severely active ulcerative colitis in adults.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Etrasimod?

Etrasimod is classified as Sphingosine-1-phosphate (S1P) receptor modulators, Hormone Receptor Modulators, Decreased Cellular Migration.

What are the brand names for Etrasimod?

Etrasimod is marketed under brand names including Velsipity.

What are the contraindications for Etrasimod?

Etrasimod labeling lists contraindications including: VELSIPITY is contraindicated in patients who: • In the last 6 months, have experienced a myocardial infarction, unstable angina pectoris, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure [see Warnings and Precautions (5.2) ] . • Have a history or presence of Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker [see Warnings and Precautions (5.2) ] .. Always consult the full prescribing information and a clinician.