fingolimod hydrochloride


Summary: A sphingosine-derivative and IMMUNOSUPPRESSIVE AGENT that blocks the migration and homing of LYMPHOCYTES to the CENTRAL NERVOUS SYSTEM through its action on SPHINGOSINE 1-PHOSPHATE RECEPTORS. It is used in the treatment of MULTIPLE SCLEROSIS.

Top Publications

  1. Proia R, Hla T. Emerging biology of sphingosine-1-phosphate: its role in pathogenesis and therapy. J Clin Invest. 2015;125:1379-87 pubmed publisher
    ..The unique mode of signaling of this lysophospholipid mediator is providing novel opportunities for therapeutic intervention, with possibilities to target not only GPCRs but also transporters, metabolic enzymes, and chaperones. ..
  2. Blanc C, Rosen H, Lane T. FTY720 (fingolimod) modulates the severity of viral-induced encephalomyelitis and demyelination. J Neuroinflammation. 2014;11:138 pubmed publisher
    ..FTY720 treatment reduces the severity of neuroinflammatory-mediated demyelination by restricting the access of disease-causing lymphocytes into the CNS but is not associated with viral recrudescence in this model. ..
  3. Cantalupo A, Gargiulo A, Dautaj E, Liu C, Zhang Y, Hla T, et al. S1PR1 (Sphingosine-1-Phosphate Receptor 1) Signaling Regulates Blood Flow and Pressure. Hypertension. 2017;70:426-434 pubmed publisher
    ..Our study identifies S1P-S1PR1-nitric oxide signaling as a new regulatory pathway in vivo of vascular relaxation to flow and BP homeostasis, providing a novel therapeutic target for the treatment of hypertension. ..
  4. Rudick R. MS clinical trials: what can subgroup analyses teach us?. Lancet Neurol. 2012;11:386-8 pubmed publisher
  5. Ma S, Santhosh D, Kumar T P, Huang Z. A Brain-Region-Specific Neural Pathway Regulating Germinal Matrix Angiogenesis. Dev Cell. 2017;41:366-381.e4 pubmed publisher
    ..They also identify tissue-specific molecular targets for GM hemorrhage intervention. ..
  6. Wilk M, Misiak A, McManus R, Allen A, Lynch M, Mills K. Lung CD4 Tissue-Resident Memory T Cells Mediate Adaptive Immunity Induced by Previous Infection of Mice with Bordetella pertussis. J Immunol. 2017;199:233-243 pubmed publisher
    ..Our findings reveal that Ag-specific CD4 TRM cells play a critical role in adaptive immunity against reinfection and memory induced by natural infection with B. pertussis. ..
  7. La Mantia L, Prone V, Marazzi M, Erminio C, Protti A. Multiple sclerosis rebound after fingolimod discontinuation for lymphopenia. Neurol Sci. 2014;35:1485-6 pubmed publisher
  8. Merkel B, Butzkueven H, Traboulsee A, Havrdova E, Kalincik T. Timing of high-efficacy therapy in relapsing-remitting multiple sclerosis: A systematic review. Autoimmun Rev. 2017;16:658-665 pubmed publisher
    ..with a delay after the MS diagnosis. The evidence reported for disability and MRI outcomes is inconclusive. ..
  9. Sucksdorff M, Rissanen E, Tuisku J, Nuutinen S, Paavilainen T, Rokka J, et al. Evaluation of the Effect of Fingolimod Treatment on Microglial Activation Using Serial PET Imaging in Multiple Sclerosis. J Nucl Med. 2017;58:1646-1651 pubmed publisher
    ..The study opens new vistas for designing future therapeutic studies in MS that use the evaluation of microglial activation as an imaging outcome measure. ..

More Information


  1. Laroni A, Brogi D, Milesi V, Abate L, Uccelli A, Mancardi G. Early switch to fingolimod may decrease the risk of disease recurrence after natalizumab interruption. Mult Scler. 2013;19:1236-7 pubmed publisher
  2. Izquierdo G, Damas F, Páramo M, Ruiz Peña J, Navarro G. The real-world effectiveness and safety of fingolimod in relapsing-remitting multiple sclerosis patients: An observational study. PLoS ONE. 2017;12:e0176174 pubmed publisher
    ..The real-world fingolimod benefits observed in this study seem to be similar than those observed in previous clinical trials. ..
  3. González Suárez I, Rodriguez de Antonio L, Orviz A, Moreno García S, Valle Arcos M, Matias Guiu J, et al. Catastrophic outcome of patients with a rebound after Natalizumab treatment discontinuation. Brain Behav. 2017;7:e00671 pubmed publisher
    ..A very careful evaluation of benefit-risk should be considered before NTZ withdrawal, and a close monitoring and a short washout period is recommended after drug withdrawal. ..
  4. Gusman D, Shoemake C. Evaluation and Optimization of in silico designed Sphingosine-1-Phosphate (S1P) Receptor Subtype 1 Modulators for the Management of Multiple Sclerosis. Yale J Biol Med. 2017;90:15-23 pubmed
    ..A rigorous selection process identified two molecules, Molecules 003 and 019, deriving from fingolimod and amiselimod, respectively, which were deemed most suitable for further optimization. ..
  5. Paroni M, Maltese V, De Simone M, Ranzani V, Larghi P, Fenoglio C, et al. Recognition of viral and self-antigens by TH1 and TH1/TH17 central memory cells in patients with multiple sclerosis reveals distinct roles in immune surveillance and relapses. J Allergy Clin Immunol. 2017;140:797-808 pubmed publisher
    ..Thus the selective targeting of TH1/TH17 cells could inhibit relapses without causing John Cunningham virus-dependent progressive multifocal encephalomyelitis. ..
  6. Pelletier D, Hafler D. Fingolimod for multiple sclerosis. N Engl J Med. 2012;366:339-47 pubmed publisher
  7. Mohammad M, Tsai V, Ruitenberg M, Hassanpour M, Li H, Hart P, et al. Immune cell trafficking from the brain maintains CNS immune tolerance. J Clin Invest. 2014;124:1228-41 pubmed publisher
  8. Piscolla E, Hakiki B, Pasto L, Razzolini L, Portaccio E, Amato M. Rebound after Fingolimod suspension in a pediatric-onset multiple sclerosis patient. J Neurol. 2013;260:1675-7 pubmed publisher
  9. Lindsey J, Haden Pinneri K, Memon N, Buja L. Sudden unexpected death on fingolimod. Mult Scler. 2012;18:1507-8 pubmed
  10. Ordoñez Boschetti L, Rey R, Cruz A, Sinha A, Reynolds T, Frider N, et al. Safety and Tolerability of Fingolimod in Latin American Patients with Relapsing-Remitting Multiple Sclerosis: The Open-Label FIRST LATAM Study. Adv Ther. 2015;32:626-35 pubmed publisher
    ..5 mg was well tolerated in RRMS patients from Latin America. The overall safety profile was clinically manageable and consistent with previous fingolimod studies. Novartis. #NCT01497262. ..
  11. Rumah K, Vartanian T, Fischetti V. Oral Multiple Sclerosis Drugs Inhibit the In vitro Growth of Epsilon Toxin Producing Gut Bacterium, Clostridium perfringens. Front Cell Infect Microbiol. 2017;7:11 pubmed publisher
    ..Moreover, inhibition of C. perfringens growth and resulting blockade of epsilon toxin production may contribute to the clinical efficacy of these disease-modifying drugs. ..
  12. Brito V, Gines S. p75NTR in Huntington's disease: beyond the basal ganglia. Oncotarget. 2016;7:1-2 pubmed publisher
  13. van Pesch V, Marchandise S, El Sankari S, Sindic C. Ventricular arrhythmia in a male MS patient on fingolimod. Acta Neurol Belg. 2015;115:77-9 pubmed publisher
  14. Centonze D, Rossi S, Rinaldi F, Gallo P. Severe relapses under fingolimod treatment prescribed after natalizumab. Neurology. 2012;79:2004-5 pubmed publisher
  15. . Fingolimod for multiple sclerosis. Drug Ther Bull. 2012;50:18-20 pubmed publisher
    ..It is the first oral disease-modifying drug for the treatment of patients with multiple sclerosis. Here we assess the place of this drug. ..
  16. Teo T, Chan Y, Lee W, Lum F, Amrun S, Her Z, et al. Fingolimod treatment abrogates chikungunya virus-induced arthralgia. Sci Transl Med. 2017;9: pubmed publisher
    ..These results set the stage for further clinical evaluation of fingolimod in the treatment of CHIKV-induced joint pathologies. ..
  17. Sheth K, Rosand J. Targeting the immune system in intracerebral hemorrhage. JAMA Neurol. 2014;71:1083-4 pubmed publisher
  18. Alsop J, Medin J, Cornelissen C, Vormfelde S, Ziemssen T. Two studies in one: A propensity-score-matched comparison of fingolimod versus interferons and glatiramer acetate using real-world data from the independent German studies, PANGAEA and PEARL. PLoS ONE. 2017;12:e0173353 pubmed publisher
    ..2% vs 15.2%; worsening: 16.4% vs 30.4%; p < 0.0001). Fingolimod appears to be more effective than BRACE in improving clinical and physician-/patient-reported outcomes in individuals with active MS. ..
  19. Velmurugan B, Lee C, Chiang S, Hua C, Chen M, Lin S, et al. PP2A deactivation is a common event in oral cancer and reactivation by FTY720 shows promising therapeutic potential. J Cell Physiol. 2018;233:1300-1311 pubmed publisher
    ..All our results suggest that PP2A is frequently deactivated in oral cancer and determines poor outcome, restoring its expression by FTY720 can be an alternative therapeutic approach in OSCC. ..
  20. Fox R. In the coming year we should abandon interferons and glatiramer acetate as first-line therapy for MS: yes. Mult Scler. 2013;19:24-5 pubmed publisher
  21. Tian T, Zhang J, Zhu X, Wen S, Shi D, Zhou H. FTY720 ameliorates renal fibrosis by simultaneously affecting leucocyte recruitment and TGF-? signalling in fibroblasts. Clin Exp Immunol. 2017;190:68-78 pubmed publisher
  22. Tyler K. Fingolimod and risk of varicella-zoster virus infection: back to the future with an old infection and a new drug. JAMA Neurol. 2015;72:10-3 pubmed publisher
  23. King A, Houlihan D, Kavanagh D, Haldar D, Luu N, Owen A, et al. Sphingosine-1-Phosphate Prevents Egress of Hematopoietic Stem Cells From Liver to Reduce Fibrosis. Gastroenterology. 2017;153:233-248.e16 pubmed publisher
    ..Strategies to reduce SIP signaling and increase retention of HSCs in the liver could increase their antifibrotic activities and be developed for treatment of patients with liver fibrosis. ..
  24. Janes K, Little J, Li C, Bryant L, Chen C, Chen Z, et al. The development and maintenance of paclitaxel-induced neuropathic pain require activation of the sphingosine 1-phosphate receptor subtype 1. J Biol Chem. 2014;289:21082-97 pubmed