Etrasimod Explained

Tradename:Velsipity
Dailymedid:Etrasimod
Pregnancy Au:D
Pregnancy Au Comment:[1]
Routes Of Administration:By mouth
Class:Sphingosine-1-phosphate receptor modulator
Atc Prefix:L04
Atc Suffix:AE05
Legal Au:S4
Legal Au Comment:[2] [3]
Legal Ca:Rx-only
Legal Ca Comment:[4] [5]
Legal Us:Rx-only
Legal Us Comment:[6] [7]
Legal Eu:Rx-only
Legal Eu Comment:[8]
Protein Bound:97.9%
Metabolism:Liver (CYP2C8, 2C9, 3A4)
Elimination Half-Life:30 hours
Excretion:Feces (82%), kidneys (5%)
Index2 Label:as arginine
Cas Number:1206123-37-6
Cas Number2:1206123-97-8
Pubchem:44623998
Drugbank:DB14766
Drugbank2:DBSALT003430
Chemspiderid:52084233
Chemspiderid2:57643656
Unii:6WH8495MMH
Unii2:MXE5EMA09L
Kegg:D10930
Kegg2:D10931
Chebi:229230
Chembl:3358920
Synonyms:APD334, APD-334
Iupac Name:2-[(3''R'')-7-{[4-cyclopentyl-3-(trifluoromethyl)phenyl]methoxy}-1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl]acetic acid
C:26
H:26
F:3
N:1
O:3
Smiles:C1CCC(C1)C2=C(C=C(C=C2)COC3=CC4=C(C=C3)NC5=C4CC[C@@H]5CC(=O)O)C(F)(F)F
Stdinchi: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
Stdinchikey:MVGWUTBTXDYMND-QGZVFWFLSA-N

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

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

Etrasimod was discovered by Arena Pharmaceuticals, with subsequent development by Pfizer.[9] Etrasimod was approved for medical use in the United States in October 2023, and in the European Union in February 2024.

Medical uses

Etrasimod is used for the treatment of moderate to severe ulcerative colitis.

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.[10] [11] [12] [13] [14] [15]

Society and culture

Legal status

Velsipity was approved by the US Food and Drug Administration (FDA) in October 2023.[16] [17]

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. The applicant for this medicinal product is Pfizer Europe MA EEIG.[18] Etrasimod was approved for medical use in the European Union in February 2024.

Names

Etrasimod is the international nonproprietary name.[19]

Notes and References

  1. Web site: Velsipity (Etrasimod) . Therapeutic Goods Administration (TGA) . 24 June 2024 . 7 July 2024 . 7 July 2024 . https://web.archive.org/web/20240707063502/https://www.tga.gov.au/resources/auspmd/velsipity-etrasimod . live .
  2. Web site: Velsipity (Pfizer Australia Pty Ltd) . Therapeutic Goods Administration (TGA) . 1 July 2024 . 7 July 2024 . 7 July 2024 . https://web.archive.org/web/20240707063503/https://www.tga.gov.au/resources/prescription-medicines-registrations/velsipity-pfizer-australia-pty-ltd . live .
  3. Web site: Therapeutic Goods (Poisons Standard—June 2024) Instrument 2024 . Federal Register of Legislation . 30 May 2024 . 10 June 2024 . 10 June 2024 . https://web.archive.org/web/20240610054546/https://www.legislation.gov.au/F2024L00589/asmade/text . live .
  4. Web site: Regulatory Decision Summary for Velsipity . Drug and Health Products Portal . 31 January 2024 . 1 April 2024 . 1 April 2024 . https://web.archive.org/web/20240401070514/https://dhpp.hpfb-dgpsa.ca/review-documents/resource/RDS1710775270976 . live .
  5. Web site: Notice: Multiple Additions to the Prescription Drug List (PDL) [2024-04-30] ]. Health Canada . 30 April 2024 . 3 May 2024 . 3 May 2024 . https://web.archive.org/web/20240503030205/https://www.canada.ca/en/health-canada/services/drugs-health-products/drug-products/prescription-drug-list/notices-changes/multiple-additions-2024-04-30.html . live .
  6. Web site: Velsipity- etrasimod tablet, film coated . DailyMed . 16 November 2023 . 23 February 2024 . 23 February 2024 . https://web.archive.org/web/20240223225214/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=65171e4a-d136-4abc-b08c-c40c1b486ff6 . live .
  7. Web site: Velsipity- etrasimod tablet, film coated . DailyMed . 17 November 2023 . 23 February 2024 . 23 February 2024 . https://web.archive.org/web/20240223225215/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=d5b2a717-1b5c-4aed-a69c-64a0c4561c40 . live .
  8. Web site: Velsipity Product information . Union Register of medicinal products . 19 February 2024 . 23 February 2024 . 23 February 2024 . https://web.archive.org/web/20240223132606/https://ec.europa.eu/health/documents/community-register/html/h1790.htm . live .
  9. Web site: Pfizer tosses newly acquired meds out of the Arena . Fierce Biotech . 13 October 2023 . 2 May 2023 . Bayer M . 21 October 2023 . https://web.archive.org/web/20231021022938/https://www.fiercebiotech.com/biotech/pfizer-tosses-newly-acquired-meds-out-arena-part-midstage-cleaning . live .
  10. Atreya R, Neurath MF . The sphingosine-1-phosphate receptor agonist etrasimod in ulcerative colitis . Lancet . 401 . 10383 . 1132–1133 . April 2023 . 36871570 . 10.1016/S0140-6736(23)00228-3 . 257286238 .
  11. Sandborn WJ, Vermeire S, Peyrin-Biroulet L, Dubinsky MC, Panes J, Yarur A, Ritter T, Baert F, Schreiber S, Sloan S, Cataldi F, Shan K, Rabbat CJ, Chiorean M, Wolf DC, Sands BE, D'Haens G, Danese S, Goetsch M, Feagan BG . Etrasimod as induction and maintenance therapy for ulcerative colitis (ELEVATE): two randomised, double-blind, placebo-controlled, phase 3 studies . Lancet . 401 . 10383 . 1159–1171 . April 2023 . 36871574 . 10.1016/S0140-6736(23)00061-2 . 257286271 . free .
  12. Dal Buono A, Gabbiadini R, Alfarone L, Solitano V, Repici A, Vetrano S, Spinelli A, Armuzzi A . Sphingosine 1-Phosphate Modulation in Inflammatory Bowel Diseases: Keeping Lymphocytes Out of the Intestine . Biomedicines . 10 . 7 . 1735 . July 2022 . 35885040 . 9313037 . 10.3390/biomedicines10071735 . free .
  13. Argollo M, Furfaro F, Gilardi D, Roda G, Allocca M, Peyrin-Biroulet L, Danese S . Modulation of sphingosine-1-phosphate in ulcerative colitis . Expert Opinion on Biological Therapy . 20 . 4 . 413–420 . April 2020 . 32093531 . 10.1080/14712598.2020.1732919 . 211475181 .
  14. Al-Shamma H, Lehmann-Bruinsma K, Carroll C, Solomon M, Komori HK, Peyrin-Biroulet L, Adams J . The Selective Sphingosine 1-Phosphate Receptor Modulator Etrasimod Regulates Lymphocyte Trafficking and Alleviates Experimental Colitis . The Journal of Pharmacology and Experimental Therapeutics . 369 . 3 . 311–317 . June 2019 . 30872391 . 10.1124/jpet.118.254268 . 78093401 . free .
  15. Peyrin-Biroulet L, Christopher R, Behan D, Lassen C . Modulation of sphingosine-1-phosphate in inflammatory bowel disease . Autoimmunity Reviews . 16 . 5 . 495–503 . May 2017 . 28279838 . 10.1016/j.autrev.2017.03.007 .
  16. Web site: FDA Approves New Drug for Ulcerative Colitis . Medscape . 13 October 2023 . 13 October 2023 . Brooks M . 21 October 2023 . https://web.archive.org/web/20231021022937/https://www.medscape.com/viewarticle/997350 . live .
  17. Web site: Velsipity (etrasimod) tablets for the treatment of moderately to severely active ulcerative colitis in adults . Approval Letter . U.S. Food and Drug Administration . 19 October 2023 . 7 July 2024 . https://web.archive.org/web/20240707063451/https://www.accessdata.fda.gov/drugsatfda_docs/appletter/2023/216956Orig1s000ltr.pdf . live .
  18. Web site: Velsipity EPAR . European Medicines Agency (EMA) . 14 December 2023 . 17 December 2023 . 15 December 2023 . https://web.archive.org/web/20231215150024/https://www.ema.europa.eu/en/medicines/human/EPAR/velsipity . live . Text was copied from this source which is copyright European Medicines Agency. Reproduction is authorized provided the source is acknowledged.
  19. ((World Health Organization)) . 2017 . International nonproprietary names for pharmaceutical substances (INN): recommended INN: list 78 . WHO Drug Information . 31 . 3 . 10665/330961 . free . World Health Organization .

This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Etrasimod".

Except where otherwise indicated, Everything.Explained.Today is © Copyright 2009-2024, A B Cryer, All Rights Reserved. Cookie policy.