Second generation S1P pathway modulators: Research strategies and clinical developments

Multiple Sclerosis is a chronic autoimmune disorder affecting the central nervous system through demyelination and neurodegeneration

Marc Bigaud; Danilo Guerini; Andreas Billich; Frederic Bassilana; Volker Brinkmann

2013

Scholarcy highlights

  • Multiple Sclerosis is a chronic autoimmune disorder affecting the central nervous system through demyelination and neurodegeneration
  • Major therapeutic treatments have relied on agents requiring injection delivery
  • Fingolimod causes down-modulation of S1P1 receptors on lymphocytes which prevents the invasion of autoaggressive T cells into the CNS
  • Animal data further suggest that the drug directly supports the recovery of nerve conduction and remyelination
  • In human MS, such mechanisms may explain the significant decrease in the number of inflammatory markers on brain magnetic resonance imaging in recent clinical trials, and the reduction of brain atrophy by the drug
  • Fingolimod binds to 4 of the 5 known S1P receptor subtypes, and significant efforts were made over the past 5 years to develop generation S1P receptor modulators and determine the minimal receptor selectivity needed for maximal therapeutic efficacy in MS patients
  • This article is part of a Special Issue entitled New Frontiers in Sphingolipid Biology

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