Sphingosine-1-phosphate receptor modulator

Sphingosine-1-phosphate receptor modulator
Drug class
Sphingosine-1-phosphate
Class identifiers
UseMultiple Sclerosis (MS), psoriasis, Host vs. graft disease, organ transplant
ATC codeL04AA
Biological targetSphingosine-1-phosphate receptor
Legal status
In Wikidata

Sphingosine-1-phosphate receptor modulators are a class of drugs that interact with S1P receptors, a family of G protein-coupled receptors involved in various physiological processes, particularly in the immune and nervous systems. These modulators have gained significant attention due to their ability to alter lymphocyte trafficking and potentially provide therapeutic benefits in autoimmune diseases, particularly multiple sclerosis (MS).[1] The most well-known compound in this class is fingolimod (FTY720), which was the first oral disease-modifying therapy approved for the treatment of relapsing-remitting MS.

These drugs have the ability to modulate the G-protein coupled S1P receptors. Drugs that modulate S1P1 receptors bind to those receptors in lymph nodes and prevent certain lymphoid immune cells from being excreted into the blood and reaching the central nervous system (CNS), leading to lymphopenia.[2][3][4][5]

  1. ^ "Department of Error". Lancet. 398 (10306): 1132. September 2021. doi:10.1016/S0140-6736(21)02050-X. PMID 34563294.
  2. ^ Dyckman AJ (July 2017). "Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P1) Agonists and Future Perspectives". Journal of Medicinal Chemistry. 60 (13): 5267–5289. doi:10.1021/acs.jmedchem.6b01575. PMID 28291340.
  3. ^ Park SJ, Im DS (January 2017). "Sphingosine 1-Phosphate Receptor Modulators and Drug Discovery". Biomolecules & Therapeutics. 25 (1): 80–90. doi:10.4062/biomolther.2016.160. PMC 5207465. PMID 28035084.
  4. ^ Adachi K, Chiba K (September 2007). "FTY720 story. Its discovery and the following accelerated development of sphingosine 1-phosphate receptor agonists as immunomodulators based on reverse pharmacology". Perspectives in Medicinal Chemistry. 1: 11–23. doi:10.1177/1177391X0700100002. PMC 2754916. PMID 19812733.
  5. ^ Pelletier D, Hafler DA (January 2012). "Fingolimod for multiple sclerosis". The New England Journal of Medicine. 366 (4): 339–347. doi:10.1056/NEJMct1101691. PMID 22276823.