Etrasimod
VELSIPITY
Pronunciation: e-TRAS-i-mod (vel-SI-pi-tee)
What it isSelective sphingosine-1-phosphate receptor agonist that sequesters lymphocytes; ulcerative colitis.
Why this oneUnlike ozanimod, it needs no dose titration and has no active metabolites, simplifying initiation and washout.
What limits itBradycardia, infection, liver injury and macular edema matter; check ECG, counts, liver tests and eye risk before starting.
Principal riskInfections; bradyarrhythmia and AV conduction delay
Classes and tags
Clinical profile
Legacy pregnancy categoryN/A (post-2015 labeling)
Defining liabilityImmunosuppression and initial bradycardia/AV conduction delay
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Moderately to severely active ulcerative colitis | Adults | 2 mg QD | 2 mg QD | 2 mg QD |
Renal Undefined
Hepatic Severe (Child-Pugh C): use not recommended; mild-moderate (Child-Pugh A/B): no adjustment needed
CYP2C9 poor metabolizers: concomitant moderate-strong CYP2C8 or CYP3A4 inhibitors not recommended
Instructions
- Swallow tablet whole, with or without food
- Missed dose: take at next scheduled time; do not double
- Before first dose: recent CBC with lymphocytes, ECG (cardiology input for conduction abnormalities), transaminases/bilirubin, baseline fundus exam incl. macula, skin exam
- Test VZV antibodies if no confirmed varicella history/vaccination; vaccinate antibody-negative patients before starting; give live attenuated vaccines >=4 weeks before starting and avoid during and for 5 weeks after treatment
- Review drugs slowing heart rate/AV conduction and prior immunosuppressive therapy before starting
Available strengths
- tab 2 mg
Contraindications
- MI, unstable angina, stroke, TIA, decompensated heart failure requiring hospitalization, or Class III/IV heart failure in the last 6 months
- History or presence of Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sino-atrial block, unless functioning pacemaker
Cautions
- Infections (lymphocyte count falls to ~45% of baseline): monitor during and for 5 weeks after stopping; delay start in active infection; PML reported with S1P modulators
- Bradyarrhythmia and AV conduction delays: baseline ECG; cardiology consult if conduction abnormality or HR-lowering drugs
- Liver injury: baseline transaminases/bilirubin; discontinue if significant liver injury confirmed
- Macular edema: baseline and periodic fundus exams; consider discontinuing if it develops
- Increased blood pressure: monitor
- Cutaneous malignancies: baseline and periodic skin exams
- Posterior reversible encephalopathy syndrome (PRES)
- Respiratory effects: decline in pulmonary function possible; spirometry if indicated
- Additive immune effects with prior/concomitant immunosuppressants; immune effects persist up to 5 weeks after stopping
Adverse reactions
- Headache
- Elevated liver tests
- Dizziness
- Infections (UTI, herpes viral)
- Lymphopenia
Pregnancy May cause fetal harm (animal data); pregnancy exposure registry 1-800-616-3791; use effective contraception during and 1 week after stopping
Lactation No human data; drug in rat milk; weigh benefits of breastfeeding against risk to infant
Cost
| Strength | #/mo | generic $/mo | CostPlus | |
|---|---|---|---|---|
| 2 mg | tab | 30 qd | not offered |
Open Etrasimod in the interactive console ↗
Self-check
- Does etrasimod require dose titration?
No. - Does etrasimod have active metabolites like ozanimod?
No.