Etrasimod

Etrasimod
Skeletal formula of etrasimod
Clinical data
Trade namesVelsipity
Other namesAPD334, APD-334
AHFS/Drugs.comMonograph
MedlinePlusa623050
License data
Pregnancy
category
Routes of
administration		By mouth
Drug classSphingosine-1-phosphate receptor modulator
ATC code
Legal status
Legal status
Pharmacokinetic data
Protein binding97.9%
MetabolismLiver (CYP2C8, 2C9, 3A4)
Elimination half-life30 hours
ExcretionFeces (82%), kidneys (5%)
Identifiers
  • 2-[(3R)-7-{[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy}-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC26H26F3NO3
Molar mass457.493 g·mol−1
3D model (JSmol)
  • C1CCC(C1)C2=C(C=C(C=C2)COC3=CC4=C(C=C3)NC5=C4CC[C@@H]5CC(=O)O)C(F)(F)F
  • InChI=1S/C26H26F3NO3/c27-26(28,29)22-11-15(5-8-19(22)16-3-1-2-4-16)14-33-18-7-10-23-21(13-18)20-9-6-17(12-24(31)32)25(20)30-23/h5,7-8,10-11,13,16-17,30H,1-4,6,9,12,14H2,(H,31,32)/t17-/m1/s1
  • Key:MVGWUTBTXDYMND-QGZVFWFLSA-N

Etrasimod, sold under the brand name Velsipity, is a medication that is used for the treatment of ulcerative colitis.[6] It is a selective sphingosine-1-phosphate (S1P) receptor modulator that modifies the activity of the immune system.[6] It is taken by mouth.[6]

The most common side effects include lymphopenia (low levels of lymphocytes) and headache.[8]

Etrasimod was discovered by Arena Pharmaceuticals, with subsequent development by Pfizer.[10] Etrasimod was approved for medical use in the United States in October 2023,[6] and in the European Union in February 2024.[8]

  1. ^ a b "Velsipity (Etrasimod)". Therapeutic Goods Administration (TGA). 24 June 2024. Archived from the original on 7 July 2024. Retrieved 7 July 2024.
  2. ^ "Velsipity (Pfizer Australia Pty Ltd)". Therapeutic Goods Administration (TGA). 1 July 2024. Archived from the original on 7 July 2024. Retrieved 7 July 2024.
  3. ^ "Therapeutic Goods (Poisons Standard—June 2024) Instrument 2024". Federal Register of Legislation. 30 May 2024. Archived from the original on 10 June 2024. Retrieved 10 June 2024.
  4. ^ "Regulatory Decision Summary for Velsipity". Health Canada. 31 January 2024. Archived from the original on 1 April 2024. Retrieved 1 April 2024.
  5. ^ "Summary Basis of Decision for Velsipity". Health Canada. 21 August 2024. Retrieved 12 October 2024.
  6. ^ a b c d e "Velsipity- etrasimod tablet, film coated". DailyMed. 16 November 2023. Archived from the original on 23 February 2024. Retrieved 23 February 2024.
  7. ^ "Velsipity- etrasimod tablet, film coated". DailyMed. 17 November 2023. Archived from the original on 23 February 2024. Retrieved 23 February 2024.
  8. ^ a b c Cite error: The named reference Velsipity EPAR was invoked but never defined (see the help page).
  9. ^ "Velsipity Product information". Union Register of medicinal products. 19 February 2024. Archived from the original on 23 February 2024. Retrieved 23 February 2024.
  10. ^ Bayer M (2 May 2023). "Pfizer tosses newly acquired meds out of the Arena". Fierce Biotech. Archived from the original on 21 October 2023. Retrieved 13 October 2023.