Etrasimod

VELSIPITY

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Pronunciation: e-TRAS-i-mod (vel-SI-pi-tee)

Etrasimod ballicule: receptor binding, kinetics and half-life diagram — Mechanism of action: Etrasimod ballicule

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.

Etrasimod molecular structure (skeletal formula) — Molecular structure: Etrasimod

FDA label

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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

Etrasimod (VELSIPITY)

Strength		#/mo	generic $/mo	CostPlus
2 mg	tab	30 qd		not offered

NADAC is a voluntary CMS survey of what retail community pharmacies pay for the drugs they stock. Etrasimod is dispensed outside retail pharmacies, so it rarely appears on surveyed invoices.

NO BOXED WARNINGS

Principal riskInfections; bradyarrhythmia and AV conduction delay

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk2 / 4

Legacy pregnancy categoryN/A (post-2015 labeling)

Defining liabilityImmunosuppression and initial bradycardia/AV conduction delay

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