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A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya)

Academic Article
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Overview

authors

  • Chun, Jerold
  • Brinkmann, V.

publication date

  • 2011

journal

  • Discovery Medicine  Journal

abstract

  • Multiple sclerosis (MS) is a chronic autoimmune disorder affecting the central nervous system (CNS) through demyelination and neurodegeneration. Until recently, major therapeutic treatments have relied on agents requiring injection delivery. In September 2010, fingolimod/FTY720 (Gilenya, Novartis) was approved by the FDA as the first oral treatment for relapsing forms of MS. Fingolimod is a novel compound produced by chemical modification of a fungal precursor. Its active metabolite, formed by in vivo phosphorylation, modulates sphingosine 1-phosphate (S1P) receptors that are a subset of a larger family of cell-surface, G protein-coupled receptors (GPCRs) mediating the effects of bioactive lipids known as lysophospholipids. Fingolimod's mechanism of action in MS is not completely understood; however, its relevant biology indicates a fundamentally different mechanism compared to all previously approved MS therapies, with evolving research supporting both immunological and nervous system activities. This duality may herald a paradigm shift in the treatment of MS and other neurological disorders.

subject areas

  • Administration, Oral
  • Animals
  • Drug Discovery
  • Fingolimod Hydrochloride
  • Humans
  • Immunologic Factors
  • Multiple Sclerosis
  • Propylene Glycols
  • Receptors, Lysosphingolipid
  • Sphingosine
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Identity

PubMed Central ID

  • PMC3694567

International Standard Serial Number (ISSN)

  • 1539-6509

PubMed ID

  • 21955849
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Additional Document Info

start page

  • 213

end page

  • 228

volume

  • 64

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