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Academia Mexicana de Neurología, A.C.

2011, Number 5

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Rev Mex Neuroci 2011; 12 (5)

Fingolimod: A novel therapy, a sphingosine 1-phosphate receptor modulator for the treatment of relapsing multiple sclerosis

Flores-Rivera JJ

Language: Spanish
References: 63
Page: 250-261
PDF size: 358.90 Kb.


ABSTRACT

Multiple sclerosis is primarily an inflammatory disorder of the central nervous system in which focal lymphocytic infiltration leads to damage of myelin and axons. The most common course is characterized by episodes of neurological dysfunction that usually recover; however, chronic neurodegeneration is present since the first stages that clinically correlate with progressive accumulation of discapacity. So the research over new treatments is extensive. Fingolimod (FTY720) is the first oral agent approved in the USA for the treatment of relapsing forms of multiple sclerosis, a sphingosine 1-phosphate receptor modulator that crosses blood brain barrier with effect over central nervous system cells and the main action over immunological system binding 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 immune surveillance may be minimally affected, the efficacy in reduction of annual relapse rate is over 50% in the two large-scale Phase III clinical trials (TRANSFORMS and FREEDOMS) that compare Fingolimod with placebo and intramuscular interferon β-1a in relapsing–remitting multiple sclerosis. Fingolimod is expected in Mexico for the last trimester of this year, it is necessary to gain experience with this very useful therapy. One administration recommendation is to take care of some events like first dose bradycardia, therefore, patients should be observed for 6 h at the time of their first dose.


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