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 effects.
Indications for Etrasimod
Primary Therapeutic Use
The primary indication of etrasimod is the treatment of moderately to severely active ulcerative colitis (UC) in adults.
Characteristics of Eligible Populations
Patients who have had an inadequate response to or are intolerant of aminosalicylates, corticosteroids, or thiopurines.
Patients who have had an inadequate response to or are intolerant of biological agents (e.g., TNF blockers, anti-integrins, anti-IL12/23 agents) or JAK inhibitors.
Patients with moderately to severely active ulcerative colitis who require long-term maintenance treatment.
Dosage Form, Strength, and Properties of Etrasimod
Dosage Form and Strength
Etrasimod is available as round, green film-coated tablets.
Active ingredient: Etrasimod arginine salt. Each tablet contains 2 mg of etrasimod (equivalent to 2.76 mg of etrasimod arginine salt).
Tablet marking: One side is engraved with "ETR" and the other side with "2".
Packaging 规格: 30 tablets per bottle, with a child-resistant cap design.
Ingredient Composition
Active ingredient: Etrasimod arginine salt.
Tablet 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 a chemical structure perspective, 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). Its molecular formula is C₃₂H₄₀F₃N₅O₅, and its molecular weight is 631.69 g/mol.
Storage Methods for Etrasimod
Storage Condition Requirements
Temperature requirement: Store at 20°C to 25°C (68°F to 77°F); short-term exposure to 15°C to 30°C (59°F to 86°F) is 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.
Administration Precautions
Administration method: Take 2 mg 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.
Missed dose handling: 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.
Post-discontinuation monitoring: After discontinuing etrasimod, monitor for signs of infection for at least 5 weeks, as the immunomodulatory effects of the drug may persist.
