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Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis.
Future Med Chem. 2012 Apr; 4(6):771-81.FM

Abstract

Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor type 1 (S1P(1)), inhibits lymphocyte egress from secondary lymphoid organs and shows immunomodulating effects. Phase III studies in multiple sclerosis demonstrated that oral FTY720 had superior efficacy compared with intramuscular IFN-β1a (AVONEX(®)) with regard to reducing the rate of relapse and the number of inflammatory lesions in the CNS. FTY720 has been approved as a new therapeutic drug for multiple sclerosis in more than 50 countries, including the USA, Japan and some of those in the EU.

Authors+Show Affiliations

Research Division, Mitsubishi Tanabe Pharma Corporation, Yokohama, Kanagawa, 227-0033, Japan. chiba.kenji@ mk.mt-pharma.co.jpNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

22530640

Citation

Chiba, Kenji, and Kunitomo Adachi. "Discovery of Fingolimod, the Sphingosine 1-phosphate Receptor Modulator and Its Application for the Therapy of Multiple Sclerosis." Future Medicinal Chemistry, vol. 4, no. 6, 2012, pp. 771-81.
Chiba K, Adachi K. Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis. Future Med Chem. 2012;4(6):771-81.
Chiba, K., & Adachi, K. (2012). Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis. Future Medicinal Chemistry, 4(6), 771-81. https://doi.org/10.4155/fmc.12.25
Chiba K, Adachi K. Discovery of Fingolimod, the Sphingosine 1-phosphate Receptor Modulator and Its Application for the Therapy of Multiple Sclerosis. Future Med Chem. 2012;4(6):771-81. PubMed PMID: 22530640.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Discovery of fingolimod, the sphingosine 1-phosphate receptor modulator and its application for the therapy of multiple sclerosis. AU - Chiba,Kenji, AU - Adachi,Kunitomo, PY - 2012/4/26/entrez PY - 2012/4/26/pubmed PY - 2012/8/15/medline SP - 771 EP - 81 JF - Future medicinal chemistry JO - Future Med Chem VL - 4 IS - 6 N2 - Fingolimod (FTY720) is a first-in-class, orally active, sphingosine 1-phosphate (S1P)-receptor modulator with a structure closely related to sphingosine. The compound was discovered by chemical modification of a natural product, myriocin. Phosphorylated form of FTY720 acts as a functional antagonist at S1P receptor type 1 (S1P(1)), inhibits lymphocyte egress from secondary lymphoid organs and shows immunomodulating effects. Phase III studies in multiple sclerosis demonstrated that oral FTY720 had superior efficacy compared with intramuscular IFN-β1a (AVONEX(®)) with regard to reducing the rate of relapse and the number of inflammatory lesions in the CNS. FTY720 has been approved as a new therapeutic drug for multiple sclerosis in more than 50 countries, including the USA, Japan and some of those in the EU. SN - 1756-8927 UR - https://www.unboundmedicine.com/medline/citation/22530640/Discovery_of_fingolimod_the_sphingosine_1_phosphate_receptor_modulator_and_its_application_for_the_therapy_of_multiple_sclerosis_ L2 - https://www.future-science.com/doi/full/10.4155/fmc.12.25?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -