BACKGROUND A 6-month phase 2 study of fingolimod demonstrated efficacy and safety in Japanese patients with relapsing-remitting multiple sclerosis (MS). Here we report a 6-month observational extension that evaluated efficacy and safety in patients who received fingolimod continuously for 12 months or who switched from placebo to fingolimod. METHODS Of 147 patients who completed the 6-month c...

The functional relevance of brain-derived neurotrophic factor (BDNF) is beginning to be well appreciated not only in mice, but also in humans. Because reduced levels typically correlate with impaired neuronal function, increasing BDNF levels with well-tolerated drugs diffusing into the central nervous system may help in ameliorating functional deficits. With this objective in mind, we used the ...

Fingolimod (FTY720) is a first-in-class orally bioavailable compound that has shown efficacy in advanced clinical trials for the treatment of multiple sclerosis (MS). In vivo, fingolimod is phosphorylated to form fingolimod-phosphate, which resembles naturally occurring sphingosine 1-phosphate (S1P), an extracellular lipid mediator whose major effects are mediated by cognate G protein-coupled r...

Fingolimod is a sphingosine-1-phosphate (S1P) analogue that has been used in clinical trials as a systemic immunomodulatory therapy for multiple sclerosis. Fingolimod readily accesses the central nervous system, raising the issue of its direct effects on neural cells. We assessed the effects of active fingolimod on dissociated cultures of mature, myelin-producing oligodendrocytes (OLGs) derived...

BACKGROUND Fingolimod is a disease modifying therapy (DMT) in highly active relapsing remitting multiple sclerosis (RRMS), as is natalizumab. Fingolimod decreases annual relapse rates and gadolinium enhancing lesions on MRI as compared to either interferon beta (IFNβ) or placebo. The effect of fingolimod on MRI outcomes compared to natalizumab treatment has not been investigated in (head to hea...

Fingolimod 0.5-mg once-daily is an approved therapy for patients with relapsing-remitting multiple sclerosis (MS). Several pivotal and real-world studies have demonstrated that fingolimod is associated with the development of macular edema (ME). Herein, we present a case of a diabetic MS patient who developed severe bilateral ME during fingolimod treatment. By means of this case study we provid...

Because of its potent efficacy and oral route of administration, the approval of fingolimod as treatment for relapsing-remitting multiple sclerosis (MS) was highly anticipated. The therapeutic and adverse effects are mediated by modulation of sphingosine 1-phosphate receptors. Fingolimod inhibits the egress of lymphocytes from lymph nodes and may also have direct effects on the central nervous ...

The solubilizing effect of β-cyclodextrin on fingolimod, a new generation immunosuppressant, is studied for the first time. A possible 20× increase in solubility fingolimod due to penetration hydrophobic fragment drug molecule into macrocyclic cavity cyclodextrin shown. Data driven 1H NMR spectroscopy and computer modeling suggest configuration resulting inclusion complexes. constant complex’s ...

BACKGROUND Fingolimod is an oral drug approved for multiple sclerosis (MS) with an ability to trap central memory T cells in secondary lymphoid tissues; however, its variable effectiveness in individual patients indicates the need to evaluate its effects on other lymphoid cells. OBJECTIVE To clarify the effects of fingolimod on B-cell populations in patients with MS. METHODS We analysed blo...

BACKGROUND Fingolimod 0.5mg once daily is the first approved oral therapy for relapsing multiple sclerosis (MS). OBJECTIVE To report integrated long-term safety data from phase 2/3 fingolimod studies. METHODS Descriptive safety data are reported from the FTY720 Research Evaluating Effects of Daily Oral Therapy in Multiple Sclerosis (FREEDOMS) study, a 24-month, randomized, double-blind stud...