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       #Post#: 630--------------------------------------------------
       (Abst.) Dimethyl fumarate in the treatment of RRMS: overview
       By: agate Date: January 24, 2015, 6:41 pm
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       From Therapeutic Advances in Neurological Disorders, January 6,
       2015:
       [quote]Dimethyl fumarate in the treatment of relapsing–remitting
       multiple sclerosis: an overview
       Roberto Bomprezzi
       Department of Neurology, University of Massachusetts, 55 Lake
       Avenue North, Worcester, MA 01655, USA
       rbomprez@gmail.com
       Multiple sclerosis (MS) shares an immune-mediated origin with
       psoriasis. Long-term safety and efficacy data generated in
       Europe from usage of fumaric acid formulations in the latter
       disease constituted grounds to investigate their effects in MS
       patients. Dimethyl fumarate (DMF) was found to be the active
       principle in those formulations and in vitro studies have
       demonstrated that DMF has immune-modulatory properties exerted
       through abilities to divert cytokine production toward a Th2
       profile, both on lymphocytes and microglial cells.
       More importantly, DMF was discovered to impact the
       anti-oxidative stress cell machinery promoting the transcription
       of genes downstream to the activation of the nuclear factor
       (erythroid derived 2)-like2 (NRF2). DMF exposure increases the
       cytosol concentrations of NRF2, which besides immune regulatory
       effects, has the potential for cytoprotection on glial cells,
       oligodendrocytes and neurons.
       Extensive and rigorous clinical trials have assessed the
       efficacy and safety of DMF at the dose of 240 mg twice and three
       times a day in relapsing-remitting MS patients during one phase
       IIb and two phase III trials. Robust, positive results were
       obtained across a number of clinical and paraclinical
       parameters.
       In one study (DEFINE), the relative reductions of the adjusted
       annualized relapse rate of the low and high dose regimens in
       comparison with placebo were 53% and 48%, respectively
       (p&#8201;<&#8201;0.001 for both comparisons).
       In the other trial (CONFIRM), DMF decreased the annualized
       relapse rate in comparison with placebo by 44% in the lower and
       by 51% in higher dosage group (also p < 0.001). The number and
       size of lesions as detected by magnetic resonance imaging were
       also significantly decreased in comparison with the patients
       receiving DMF at every dosage. Multiple post hoc and subgroup
       analyses corroborated the clinical data, rendering DMF an
       appealing medication whose potential for impacting the
       degenerative aspects of MS remains to be explored.[/quote]
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