Etrasimod is a sphingosine-1-phosphate (S1P) receptor modulator, used for the treatment of moderately to severely active ulcerative colitis (UC) in adults.

How to Use Etrasimod

Routine Dosage and Administration

Recommended dosage: 2mg orally once daily, which can be taken with food or on an empty stomach.

Dosage form and specification: 2mg tablets, round green film-coated tablets, engraved with "ETR" on one side and "2" on the other side.

Administration requirements: Swallow the tablet whole; do not break or chew it.

Pre-Treatment Evaluation

Blood tests: Complete blood count (CBC), including lymphocyte count.

Cardiac evaluation: Electrocardiogram (ECG) to detect the presence of conduction abnormalities.

Liver function tests: Measurement of transaminase and bilirubin levels.

Ophthalmic examination: Baseline assessment of the fundus and macular region.

Vaccination: If the varicella vaccine has not been administered or varicella antibody is negative, vaccination should be completed 4 weeks before treatment initiation.

Precautions for Medication Use

Infection risk: Monitor for infection symptoms (such as fever, fatigue) during treatment and within 5 weeks after discontinuing the medication.

Cardiac monitoring: A transient decrease in heart rate may occur after the first dose; be alert to symptoms such as dizziness and weakness.

Dosage Adjustment and Contraindications for Etrasimod

Situations Not Requiring Dosage Adjustment

Patients with mild to moderate hepatic insufficiency (Child-Pugh Class A/B) or mild to moderate renal insufficiency.

Contraindications

Cardiovascular events: Myocardial infarction, unstable angina pectoris, stroke, or New York Heart Association (NYHA) Class III/IV heart failure occurring within the past 6 months.

Conduction abnormalities: Mobitz type II second-degree or third-degree atrioventricular block, or sick sinus syndrome in patients without a pacemaker implanted.

Situations Requiring Treatment Suspension or Discontinuation

Severe infection: If active infection is confirmed, suspend treatment until the infection is under control.

Liver injury: If transaminase levels increase to ≥ 3 times the upper limit of normal (ULN) accompanied by elevated bilirubin, permanently discontinue the medication.

Medication Use in Special Populations for Etrasimod

Pregnant Women

Animal studies have shown embryotoxicity, which may cause fetal malformations.

It is contraindicated during pregnancy; women must use highly effective contraceptive measures during medication use and within 1 week after discontinuing the medication.

Lactating Women

Etrasimod may be excreted in breast milk; for lactating women, the risks and benefits should be weighed, or breastfeeding should be suspended.

Patients with Hepatic Insufficiency

Severe hepatic insufficiency (Child-Pugh Class C): Use is not recommended.

Patients with mild to moderate hepatic insufficiency do not require dosage adjustment, but close monitoring of liver function is necessary.

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Administration Instructions