Etrasimod is a sphingosine 1-phosphate (S1P) receptor modulator developed by ViiV Healthcare, which was first approved in the United States in 2023. As a novel oral medication for the treatment of ulcerative colitis, Etrasimod provides patients with a new treatment option through its unique immunomodulatory effect.
Indication of Etrasimod
Primary Therapeutic Use
The primary indication of Etrasimod is the treatment of moderate to severe active ulcerative colitis (UC) in adults.
Characteristics of Applicable Population
Patients who have an inadequate response to or cannot tolerate aminosalicylates, corticosteroids, or thiopurines.
Patients who have an inadequate response to or cannot tolerate biological agents (such as TNF blockers, anti-integrins, anti-IL12/23) or JAK inhibitors.
Patients with moderate to severe active ulcerative colitis who require long-term maintenance treatment.
Specification and Characteristic of Etrasimod
Dosage Form and Specification
Etrasimod is a round, green, film-coated tablet.
Active ingredient: Etrasimod arginine salt, each tablet containing 2mg of Etrasimod (equivalent to 2.76mg of Etrasimod arginine salt).
Tablet marking: Engraved with "ETR" on one side and "2" on the other side.
Packaging specification: 30 tablets per bottle, with a child-resistant cap design.
Composition
Active ingredient: Etrasimod arginine salt.
Core excipients: Magnesium stearate, mannitol, microcrystalline cellulose, and sodium starch glycolate.
Film-coating ingredients: FD&C Blue No. 1/Brilliant Blue FCF Aluminum Lake, FD&C Blue No. 2/Indigo Carmine Aluminum Lake, FD&C Yellow No. 5/Tartrazine Aluminum Lake, polyethylene glycol 3350, partially hydrolyzed polyvinyl alcohol, talc, and titanium dioxide.
From the perspective of chemical structure, the chemical name of Etrasimod arginine salt is L-Arginine, (3R)-7-[[4-cyclopentyl-3-(trifluoroethyl)phenyl]methoxy]-1,2,3,4-tetrahydrocyclopenta[b]indole-3-acetate (1:1), with a molecular formula of C₃₂H₄₀F₃N₅O₅ and a molecular weight of 631.69g/mol.
Storage Method of Etrasimod
Storage Condition Requirements
Temperature requirement: Store at 20°C to 25°C (68°F to 77°F), with short-term exposure to 15°C to 30°C (59°F to 86°F) allowed.
Packaging requirement: Keep in the original packaging; each bottle contains 4 grams of silica gel desiccant.
Safety requirement: Keep out of the reach of children.
Precautions for Use
Administration method: Take 2mg once daily at a fixed time each day, either with food or on an empty stomach.
Swallow whole: The tablet should be swallowed whole; do not chew, crush, or split it.
Management of missed doses: If a dose is missed, take it as soon as possible. However, if it is almost time for the next scheduled dose, skip the missed dose and take the next dose as planned.
Monitoring after discontinuation: After discontinuing the medication, monitor for signs of infection for at least 5 weeks, as the immunomodulatory effect of the drug may persist.
