Etrasimod

Routes of
administrationBy mouthDrug classSphingosine-1-phosphate receptor modulatorATC codeLegal statusLegal status Pharmacokinetic dataProtein binding97.9%MetabolismLiver (CYP2C8, 2C9, 3A4)Elimination half-life30 hoursExcretionFeces (82%), kidneys (5%)IdentifiersCAS NumberPubChem CIDDrugBankChemSpiderUNIIKEGGChEBIChEMBLChemical and physical dataFormulaC₂₆H₂₆F₃NO₃Molar mass457.493 g·mol⁻¹3D model (JSmol)

Etrasimod, sold under the brand name Velsipity, is a medication that is used for the treatment of ulcerative colitis.^[2] It is a selective sphingosine-1-phosphate (S1P) receptor modulator that modifies the activity of the immune system.^[2] It is taken by mouth.^[2]

The most common side effects include lymphopenia (low levels of lymphocytes) and headache.^[4]

Etrasimod was discovered by Arena Pharmaceuticals, with subsequent development by Pfizer.^[6] Etrasimod was approved for medical use in the United States in October 2023,^[2] and in the European Union in February 2024.^[4]

Medical uses

Etrasimod is used for the treatment of moderate to severe ulcerative colitis.^[2][4]

Mechanism of action

It works by causing T cells to become trapped in the lymph nodes, preventing them from entering the bloodstream, from where they would travel to other tissues in the body and mediate inflammation.^{[7][8][9][10][11][12]}

Society and culture

Legal status

Velsipity was approved by the US Food and Drug Administration (FDA) in October 2023.^[2][13][14]

In December 2023, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency (EMA) adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Velsipity, intended for the treatment of ulcerative colitis.^[4] The applicant for this medicinal product is Pfizer Europe MA EEIG.^[4] Etrasimod was approved for medical use in the European Union in February 2024.^[4]

Names

Etrasimod is the international nonproprietary name.^[15]

References