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FTY720 on the way from the base camp to the summit of the mountain: relevance for remyelination.
Mult Scler. 2012 Mar; 18(3):258-63.MS

Abstract

FTY720 (fingolimod; Gilenya®), a sphingosine 1-phosphate (S1P) receptor modulator, is the first oral disease-modifying therapy to be approved for the treatment of relapsing-remitting multiple sclerosis. FTY720 is rapidly converted in vivo to the active S-fingolimod-phosphate, which binds to S1P receptors. This action inhibits egress of lymphocytes from the lymph nodes, preventing entry into the blood and thus infiltration into the central nervous system. More recent studies, however, convincingly show that FTY720 crosses the blood-brain barrier, where it is thought to act on S1P receptors on cells within the central nervous system, such as astrocytes, oligodendrocytes or microglia. Here we discuss the evidence showing that FTY720 also plays a role in remyelination and repair within the brain. While the mechanisms of action still require firm elucidation, it is clear that FTY720 could also be reparative, extending its therapeutic potential for multiple sclerosis.

Authors+Show Affiliations

Institute of Neuroanatomy, Faculty of Medicine, RWTH Aachen University, Germany. mkipp@ukaachen.deNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

22383435

Citation

Kipp, M, and S Amor. "FTY720 On the Way From the Base Camp to the Summit of the Mountain: Relevance for Remyelination." Multiple Sclerosis (Houndmills, Basingstoke, England), vol. 18, no. 3, 2012, pp. 258-63.
Kipp M, Amor S. FTY720 on the way from the base camp to the summit of the mountain: relevance for remyelination. Mult Scler. 2012;18(3):258-63.
Kipp, M., & Amor, S. (2012). FTY720 on the way from the base camp to the summit of the mountain: relevance for remyelination. Multiple Sclerosis (Houndmills, Basingstoke, England), 18(3), 258-63. https://doi.org/10.1177/1352458512438723
Kipp M, Amor S. FTY720 On the Way From the Base Camp to the Summit of the Mountain: Relevance for Remyelination. Mult Scler. 2012;18(3):258-63. PubMed PMID: 22383435.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - FTY720 on the way from the base camp to the summit of the mountain: relevance for remyelination. AU - Kipp,M, AU - Amor,S, PY - 2012/3/3/entrez PY - 2012/3/3/pubmed PY - 2012/6/20/medline SP - 258 EP - 63 JF - Multiple sclerosis (Houndmills, Basingstoke, England) JO - Mult. Scler. VL - 18 IS - 3 N2 - FTY720 (fingolimod; Gilenya®), a sphingosine 1-phosphate (S1P) receptor modulator, is the first oral disease-modifying therapy to be approved for the treatment of relapsing-remitting multiple sclerosis. FTY720 is rapidly converted in vivo to the active S-fingolimod-phosphate, which binds to S1P receptors. This action inhibits egress of lymphocytes from the lymph nodes, preventing entry into the blood and thus infiltration into the central nervous system. More recent studies, however, convincingly show that FTY720 crosses the blood-brain barrier, where it is thought to act on S1P receptors on cells within the central nervous system, such as astrocytes, oligodendrocytes or microglia. Here we discuss the evidence showing that FTY720 also plays a role in remyelination and repair within the brain. While the mechanisms of action still require firm elucidation, it is clear that FTY720 could also be reparative, extending its therapeutic potential for multiple sclerosis. SN - 1477-0970 UR - https://www.unboundmedicine.com/medline/citation/22383435/FTY720_on_the_way_from_the_base_camp_to_the_summit_of_the_mountain:_relevance_for_remyelination_ L2 - http://journals.sagepub.com/doi/full/10.1177/1352458512438723?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -