Dimethyl fumarate (BG-12) for the treatment of multiple sclerosis

Abstract

Treatments for multiple sclerosis (MS) are only partially effective and most require a parenteral route of administration and/or may have severe side effects. Dimethyl fumarate is the active compound of BG-12 recently licensed for the treatment of relapsing–remitting MS. The pivotal Phase III trials have demonstrated an approximately 50% reduction of relapse rates compared with placebo paralleled by a reduction in new lesion formation on MRI. A dose of 240 mg two-times a day had an optimal effect. Flushing and gastrointestinal symptoms (diarrhea, abdominal pain, nausea) were common adverse events in the first month(s) of treatment. Severe side effects were not more common than in the placebo group for a treatment period of 2 years. The mode of action is not exactly clear and both immunomodulatory effects and an activation of the transcription factor Nrf2 are suggested. This new oral drug will be a welcome addition to existing MS treatments.

Keywords::

• dimethyl fumarate
• fumaric acid
• immunomodulation
• immune treatment
• multiple sclerosis

Financial & competing interests disclosure

M Stangel has received honoraria for scientific lectures or consultancy from Bayer Healthcare, Biogen Idec, CSL Behring, Grifols, Merck-Serono, Novartis, Sanofi-Aventis and Teva. His institution received research support from Bayer Healthcare, Biogen Idec, Merck-Serono, Novartis and Teva. RA Linker has received consultancies and honoraria from Biogen Idec, Genzyme, Merck-Serono, Novartis and Teva. He is involved in patents on BG-12. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.