Etrasimod

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5. It partially and reversibly blocks the capacity of lymphocytes to egress from lymphoid organs, reducing the number of lymphocytes in peripheral blood.

The mechanism by which etrasimod exerts therapeutic effects in UC is unknown but may involve the reduction of lymphocyte migration into the intestines.

• Ulcerative Colitis: Used for the treatment of moderately to severely active ulcerative colitis in adults.

Ulcerative Colitis

S1P Receptor Modulator

Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1, 4, and 5. Etrasimod has minimal activity on S1P3 and no activity on S1P2.

Etrasimod modulates S1P receptors to inhibit lymphocyte egress and reduce inflammation in the intestine.

Adult Dose (Oral):

• Recommended dosage: 2 mg orally once daily.
• Swallow the tablet whole, with or without food.

Take 2 mg tablet orally once daily at the same time each day. Swallow the tablet whole. Do not chew, crush or break it. May be taken with or without food.

If a dose is missed, take the missed dose at the next scheduled time; do not double the next dose.

Common Side Effects (>=5%):

• Headache
• Elevated liver tests
• Dizziness

Precautions:

• Infections: May increase risk of infections; obtain CBC before initiation; monitor during treatment and for 5 weeks after discontinuation.
• Bradyarrhythmia and AV Conduction Delays: May result in transient decrease in heart rate and AV conduction delays; obtain ECG before starting treatment.
• Liver Injury: Elevations of aminotransferases may occur; obtain transaminase and bilirubin levels before initiation.
• Macular Edema: May increase risk; obtain baseline evaluation of fundus.
• Increased Blood Pressure: Monitor blood pressure during treatment.
• Fetal Risk: May cause fetal harm; use effective contraception.

Contraindications:

• MI, unstable angina, stroke, TIA, decompensated heart failure, or Class III or IV heart failure in the last 6 months
• Mobitz type II second-degree or third-degree AV block, sick sinus syndrome, or sino-atrial block (unless patient has a functioning pacemaker)

Drug Interactions:

• CYP2C8, CYP2C9, and CYP3A4 inhibitors and inducers: May interact.

Food Interactions: May be taken with or without food. Caution with alcohol.

Use in Pregnancy: Limited data on use during pregnancy; fetal risk may exist.

Use in Lactation: No data on presence in human milk; caution required.

Pediatric Use: Safety and efficacy not established.

Geriatric Use: No specific dosage adjustment is necessary for elderly patients.

Renal Impairment: No specific dosage adjustment is necessary.

Hepatic Impairment: Use with caution in patients with liver disease.

Overdose: Limited information on overdose; symptomatic treatment.

Storage: Keep below 30 degree C, away from light and moisture. Keep out of reach of children.

Etrasimod