伊曲莫德(Etrasimod)的功效与作用

Etrasimod is an oral sphingosine 1-phosphate receptor modulator. It was approved for marketing by the U.S. Food and Drug Administration (FDA) on October 13, 2023.

Efficacy and role of Etrasimod

It can highly selectively bind to S1P receptors 1, 4, and 5, inhibiting the migration of lymphocytes from lymphoid tissues, thereby reducing the number of lymphocytes in peripheral blood and reducing intestinal inflammatory response.

Indications of Etrasimod

Etrasimod is suitable for the treatment of moderately to severely active ulcerative colitis in adults.

The pictures are from public channels (such as the official website of the FDA, the official website of the original drug manufacturer, etc.) and are for reference only.

Usage and dosage of Etrasimod

1. Recommended dose

Take 2 mg orally once a day.

2. How to take the medicine

It can be taken with food or on an empty stomach.

3. Treatment of missed doses

If a dose is missed, it should be taken at the next regular time without double dose.

4. Pre-medication assessment

Before starting treatment, the following examinations need to be completed: blood routine (including lymphocyte count), electrocardiogram (evaluating cardiac conduction function), liver function (transaminase and bilirubin), fundus examination (including macular area), skin examination (especially for those at risk of skin cancer), chickenpox virus antibody test (if there is no clear history of infection or vaccination).

5. Special groups

(1) It is not recommended for patients with severe liver damage.

(2) No dose adjustment is required for mild to moderate liver injury.

(3) Elderly patients need to be monitored carefully.

Adverse reactions of Etrasimod

1. Common adverse reactions

Including headache (about 9%), elevated liver enzymes (6%), dizziness (5%), nausea, joint pain, high blood pressure, urinary tract infection, etc.

2. Other adverse reactions (incidence 2%-5%)

arthralgia, hypertension (including increased blood pressure), urinary tract infection (including cystitis), nausea, hypercholesterolemia (including increased blood cholesterol), herpes virus infection (including herpes zoster, oral herpes, herpes simplex), bradycardia (including sinus bradycardia, decreased heart rate).

3. Serious adverse reactions

Infection (including severe infection, progressive multifocal leukoencephalopathy, herpes virus infection, cryptococcal infection), bradycardia and atrioventricular conduction delay, liver damage, macular edema, elevated blood pressure, skin malignant tumors, reversible posterior encephalopathy syndrome, decreased respiratory function, etc.

Drug interactions of Etrasimod

1. Antiarrhythmic drugs and QT interval prolonging drugs

Etrasimod may cause a temporary decrease in heart rate and atrioventricular conduction delay, and combined use with Class Ia and Class III antiarrhythmic drugs or QT interval prolonging drugs may increase the risk of QT prolongation and torsade de pointes. Consult a cardiologist before combined use.

2. Beta-blockers or calcium channel blockers

Itramod may cause a decrease in heart rate. No additive effect has been observed when combined with beta-blockers (stable doses), but the risk of starting beta-blocker therapy or combining with other heart-rate slowing drugs is unknown. Itrimod therapy may be initiated in patients who are stable on a beta-blocker; a cardiologist should be consulted when initiating beta-blocker therapy or concomitantly with other heart rate-lowering drugs in a patient who is stable on itramod.

3. Anti-tumor drugs, immunomodulators or non-corticosteroid immunosuppressants

The combined use has not been studied and may increase the additive immunosuppressive effect. Avoid concomitant use; when switching from a drug with long-term immune effects to itridimod, its half-life and mode of action need to be considered to avoid additive effects.

4. Moderate and potent inhibitor of CYP2C9 and CYP3A4

Coadministration with fluconazole (a moderate inhibitor of CYP2C9 and CYP3A4) may increase the exposure of itramod. Not recommended for use together.

5. Rifampicin

Rifampicin (a strong inducer of CYP3A4, a moderate inducer of CYP2C8 and CYP2C9) can reduce the exposure of itrimod, and its combined use is not recommended.