期刊
EXPERT REVIEW OF NEUROTHERAPEUTICS
卷 11, 期 2, 页码 165-183出版社
TAYLOR & FRANCIS LTD
DOI: 10.1586/ERN.10.193
关键词
administration recommendations; efficacy; fingolimod; immunomodulatory; mechanism of action; oral; relapsing-remitting multiple sclerosis; safety; sphingosine 1-phosphate receptor
资金
- Novartis
- Bayer
- Biogen-Idec
- GSK
- Teva
- Acorda
- Serono
- Pfizer
- Shire
- EMD Serono
- ONO
Fingolimod is the first oral agent approved in the USA for the treatment of relapsing forms of multiple sclerosis. Fingolimod is a sphingosine 1-phosphate receptor modulator that binds to sphingosine 1-phosphate receptors on lymphocytes, resulting in a downregulation of the receptor and a reversible sequestration of lymphocytes in lymphoid tissue. Effector memory T cells are not sequestered so that immune surveillance may be minimally affected. Two large-scale Phase Ill clinical trials have demonstrated the efficacy of fingolimod compared with placebo and intramuscular interferon beta-1a in relapsing remitting multiple sclerosis. Due to its mechanism of action, fingolimod administration may be associated with first-dose bradycardia and macular edema. Therefore, patients should be observed for 6 h at the time of their first dose and undergo ophthalmologic evaluation prior to treatment initiation and at 3-4 months after initiation.
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