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Fingolimod for relapsing multiple sclerosis: an update.
Expert Opin Pharmacother. 2010 May; 11(7):1183-96.EO

Abstract

IMPORTANCE OF THE FIELD

Multiple sclerosis (MS) is the most common inflammatory demyelinating disease of the CNS. There is a large unmet need for new disease-modifying therapies with improved convenience, safety and efficacy. Fingolimod is an oral sphingosine-1-phosphase (S1P) receptor modulator under clinical investigation for the treatment of relapsing-remitting and primary progressive MS.

AREAS COVERED IN THIS REVIEW

This review provides an update on the mechanism of action, pharmacological properties and efficacy and safety of fingolimod in patients with relapsing MS, with a particular emphasis on clinical trials.

WHAT THE READER WILL GAIN

The reader will gain a comprehensive overview of the mechanism of action of fingolimod, particularly how the drug inhibits lymphocyte egress from secondary lymphoid organs by modulation of S1P receptors, and its pharmacokinetic and pharmacodynamic properties. Results from Phase II studies and pivotal Phase III trials of fingolimod for relapsing MS are discussed in depth.

TAKE HOME MESSAGE

Randomized clinical trials have demonstrated the superior efficacy of fingolimod in reducing relapse rates and MRI measures of disease activity, as compared with placebo and intramuscular IFN-beta-1a. Fingolimod also lowered the risk of disability progression compared with placebo. Adverse events included bradycardia and atrioventricular block, respiratory and herpesvirus infections, increased liver enzyme levels, hypertension and macular edema. Fingolimod 0.5 mg seems to provide the best risk-benefit ratio.

Authors+Show Affiliations

Multiple Sclerosis Centre of Catalonia (CEM-Cat), Vall d'Hebron University Hospital, Passeig Vall d'Hebron, 119-129, 08035 Barcelona, Spain. ahorga@cem-cat.orgNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

20367536

Citation

Horga, Alejandro, et al. "Fingolimod for Relapsing Multiple Sclerosis: an Update." Expert Opinion On Pharmacotherapy, vol. 11, no. 7, 2010, pp. 1183-96.
Horga A, Castilló J, Montalban X. Fingolimod for relapsing multiple sclerosis: an update. Expert Opin Pharmacother. 2010;11(7):1183-96.
Horga, A., Castilló, J., & Montalban, X. (2010). Fingolimod for relapsing multiple sclerosis: an update. Expert Opinion On Pharmacotherapy, 11(7), 1183-96. https://doi.org/10.1517/14656561003769866
Horga A, Castilló J, Montalban X. Fingolimod for Relapsing Multiple Sclerosis: an Update. Expert Opin Pharmacother. 2010;11(7):1183-96. PubMed PMID: 20367536.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Fingolimod for relapsing multiple sclerosis: an update. AU - Horga,Alejandro, AU - Castilló,Joaquín, AU - Montalban,Xavier, PY - 2010/4/7/entrez PY - 2010/4/7/pubmed PY - 2010/7/10/medline SP - 1183 EP - 96 JF - Expert opinion on pharmacotherapy JO - Expert Opin Pharmacother VL - 11 IS - 7 N2 - IMPORTANCE OF THE FIELD: Multiple sclerosis (MS) is the most common inflammatory demyelinating disease of the CNS. There is a large unmet need for new disease-modifying therapies with improved convenience, safety and efficacy. Fingolimod is an oral sphingosine-1-phosphase (S1P) receptor modulator under clinical investigation for the treatment of relapsing-remitting and primary progressive MS. AREAS COVERED IN THIS REVIEW: This review provides an update on the mechanism of action, pharmacological properties and efficacy and safety of fingolimod in patients with relapsing MS, with a particular emphasis on clinical trials. WHAT THE READER WILL GAIN: The reader will gain a comprehensive overview of the mechanism of action of fingolimod, particularly how the drug inhibits lymphocyte egress from secondary lymphoid organs by modulation of S1P receptors, and its pharmacokinetic and pharmacodynamic properties. Results from Phase II studies and pivotal Phase III trials of fingolimod for relapsing MS are discussed in depth. TAKE HOME MESSAGE: Randomized clinical trials have demonstrated the superior efficacy of fingolimod in reducing relapse rates and MRI measures of disease activity, as compared with placebo and intramuscular IFN-beta-1a. Fingolimod also lowered the risk of disability progression compared with placebo. Adverse events included bradycardia and atrioventricular block, respiratory and herpesvirus infections, increased liver enzyme levels, hypertension and macular edema. Fingolimod 0.5 mg seems to provide the best risk-benefit ratio. SN - 1744-7666 UR - https://www.unboundmedicine.com/medline/citation/20367536/Fingolimod_for_relapsing_multiple_sclerosis:_an_update_ L2 - http://www.tandfonline.com/doi/full/10.1517/14656561003769866 DB - PRIME DP - Unbound Medicine ER -