Fingolimod: a novel immunosuppressant for multiple sclerosis.
OBJECTIVE
To review the pharmacology, pharmacokinetics, efficacy, and safety of fingolimod, a novel immune modulator.


METHODS
Information was obtained through a MEDLINE search (1966-February 2007) and from published abstracts. Search terms included fingolimod, FTY720, FTY-720, and sphingosine-1-phosphate receptor agonist.


METHODS
All English-language studies and abstracts pertaining to fingolimod were considered for inclusion. Preference was given to human data.


RESULTS
Fingolimod is the first in a new class of immune modulators known as the sphingosine-1-phosphate receptor agonists. It is administered orally once daily and causes a dose-related reduction in the number of circulating lymphocytes by preventing their egress from secondary lymph organs, but it does not alter T-cell activation or proliferation. Bradycardia and lymphopenia are the most common adverse effects. Clinical trials have evaluated the efficacy of fingolimod in renal transplantation and multiple sclerosis (MS). Further research for renal transplantation will not take place, but Phase 3 studies in MS are underway, as Phase 2 study results are favorable.


CONCLUSIONS
Due to its distinct mechanism of action and its oral administration, fingolimod may be a useful therapeutic option for patients with relapsing forms of MS. More data are needed to assess the safety and clinical utility of fingolimod.
Brown
Brandon A
BA
Partners Multiple Sclerosis Center, Brookline, MA 02445, USA. bbrown8@partners.org
Kantesaria
Pranish P
PP
McDevitt
Lisa M
LM
D000818:Animals; D015507:Drugs, Investigational / Q000009:adverse effects / Q000627:therapeutic use*; D000068876:Fingolimod Hydrochloride; D006801:Humans; D007166:Immunosuppressive Agents / Q000009:adverse effects / Q000276:immunology / Q000627:therapeutic use*; D009103:Multiple Sclerosis / Q000188:drug therapy* / Q000276:immunology; D011409:Propylene Glycols / Q000009:adverse effects / Q000276:immunology / Q000627:therapeutic use*; D013110:Sphingosine / Q000009:adverse effects / Q000031:analogs & derivatives* / Q000276:immunology / Q000627:therapeutic use