New oral drugs have considerably enriched the therapeutic armamentarium for the treatment of multiple sclerosis. This review focuses on the molecular pharmacodynamics of fingolimod, dimethyl fumarate (BG-12), laquinimod, and teriflunomide. We specifically comment on the action of these drugs at three levels: 1) the regulation of the immune system; 2) the permeability of the blood-brain barrier;...

BACKGROUND Multiple sclerosis (MS) likely results from an imbalance between regulatory and inflammatory immune processes. CD39 is an ectoenzyme that cleaves ATP to AMP and has been suggested as a novel regulatory T cells (Treg) marker. As ATP has numerous proinflammatory effects, its degradation by CD39 has anti-inflammatory influence. The purpose of this study was to explore regulatory and inf...

UNLABELLED Once-daily fingolimod 0.5 mg (FTY720; Gilenya(®), Novartis Pharma AG, Basel, Switzerland) is a sphingosine 1-phosphate receptor modulator that is approved for the treatment of relapsing multiple sclerosis (MS); currently, this includes approval in 13 Latin American countries. However, despite a well-characterized efficacy and safety profile in a large clinical development program, th...

Jasani KM, et al. BMJ Case Rep 2017. doi:10.1136/bcr-2016-218912 Description A 54-year-old female with history of relapsing remitting multiple sclerosis (MS) was switched from interferon beta-1A (Avonex, Biogen) to fingolimod (Gilenya, Novartis) therapy after having two clinical relapses within 2 years while on treatment. As part of her treatment protocol, she was referred to the local ophthalm...

BACKGROUND Multiple sclerosis patients who discontinue using natalizumab are at risk of a rebound in disease activity. However, the optimal alternative therapy is not currently known. AIMS OF THE STUDY We report on clinical and MRI data and patient safety in a group of relapsing-remitting multiple sclerosis patients who tested seropositive for the JC virus and who have switched from natalizum...

Multiple sclerosis is a demyelinating disease affecting the central nervous system. T cells are known to contribute to this immune-mediated condition. Fingolimod modulates sphingosine-1-phosphate receptors, thereby preventing the egress of lymphocytes, especially CCR7-expressing CD8+ and CD4+ T cells, from lymphoid tissues. Using Affymetrix Human Transcriptome Arrays (HTA 2.0), we performed a t...

Fingolimod (FTY720, 2-amino-2-propane-1,3-diol hydrochloride) is a remarkably efficient immunosuppressive drug that was recently approved as the first oral treatment for multiple sclerosis. Fingolimod prevents lymphocyte egress from lymph nodes by targeting 4 of 5 sphingosine-1-phosphate receptors.1 Two phase 3 trials showed that fingolimod significantly reduced multiple sclerosis disease progr...

We describe posterior reversible encephalopathy syndrome (PRES) in a woman with multiple sclerosis treated with Gilenya(®) (Fingolimod). The first symptoms appeared after 21 months of fingolimod treatment. She experienced headache, altered mental status, cognitive deficits, seizures, and visual disturbances. Not at any time during the course of the disease could any signs of infection or rheuma...

Until fingolimod came along, the first US Food and Drug Administration–approved pill for relapsingremitting multiple sclerosis (RRMS), teratogenicity of multiple sclerosis (MS) drugs had not been a big issue. Strange, for a disease that affects primarily women of childbearing age. Why? Because previously approved MS drugs were all large recombinant protein molecules. Large molecules cross the p...

Fingolimod—an efficacious compound for the treatment of relapsing multiple sclerosis (MS)—functionally antagonizes the S1P receptor. This antagonism inhibits egress of T cells from secondary lymphoid tissues, affects B cell migration, and functionally affects germinal center reactions. Although vaccine-specific antibodies can be induced in patients withMS under fingolimod therapy, the magnitude...