Dimethyl fumarate: a novel drug for multiple sclerosis


  • Jatinder Singh Department of Pharmacology, Dayanand Medical College and Hospital, Ludhiana, Punjab, India
  • Bharti Mahajan Department of Pharmacology, Dayanand Medical College and Hospital, Ludhiana, Punjab, India
  • Sandeep Kaushal Department of Pharmacology, Dayanand Medical College and Hospital, Ludhiana, Punjab, India


Dimethyl fumarate, Fumaric acids, Multiple sclerosis, Nuclear factor-erythroid 2-related factor 2


Dimethyl fumarate (DMF) is a novel oral immunomodulatory and neuroprotective drug that was approved by FDA for relapsing forms of multiple sclerosis (MS). The initial use of DMF was for the treatment of psoriasis where its long-term use was safe and efficacious, and it also got German approval for the same. It was found that the anti-inflammatory actions of DMF contributed to its efficacy in psoriasis. This anti-inflammatory action of DMF created interest using DMF in other auto-immune or inflammatory diseases, including MS. DMF acts by decreasing production and release of inflammatory molecules. DMF also activates the nuclear factor-erythroid 2 related factor pathway which induces the transcription of various genes, including anti-oxidative ones, reduces oxidative neuronal death and helps maintain myelin integrity. Thus, DMF acts via two pathways: by down-regulating oxidative stress and corresponding cellular injury, as well as by inhibiting pro-inflammatory cytokines. DMF is an orally administered, enteric-coated microtablet preparation. There was a 44-53% reduction in annualized relapse rate with the use of DMF in patients with relapsing form of MS. The most common adverse reactions reported are flushing, abdominal pain, diarrhea, and nausea, which are more prominent during initial treatment and usually decrease over time. No serious adverse events were seen during the phase II and III trials, including no increased risk of opportunistic infections or cancer. DMF seems to approach the ideal combination of safety, efficacy and well-tolerability to other approved oral therapies for MS.


Tecfidera [package insert]. Cambridge, MA: Biogen Idec Inc.; 2013. Available at http://www.dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=665d7e74-036c-5f68-5b67-ab84b9b49151. Accessed 19 Jun 2014.

Temple R. NDA approval letter: Tecfidera (dimethyl fumarate NDA 204063). US Food and Drug Administration; 2013. Available at http://www.accessdata.fda.gov/drugsatfda_docs/appletter/2013/204063Orig1s000ltr.pdf. Accessed 19 Jun 2014.

Hoefnagel JJ, Thio HB, Willemze R, Bouwes Bavinck JN. Long-term safety aspects of systemic therapy with fumaric acid esters in severe psoriasis. Br J Dermatol. 2003;149(2):363-9.

Weiner HL. Multiple sclerosis is an inflammatory T-cell-mediated autoimmune disease. Arch Neurol 2004;61(10):1613-5.

Goldenberg MM. Multiple sclerosis review. P T. 2012;37(3):175-84.

Gilenya [package insert]. East Hanover, NJ: Novartis Pharmaceuticals Corporation; 2012. Available at http://www.fda.gov/downloads/drugs/drugsafety/postmarketdrugsafetyinformationforpatientsandproviders/ucm227965.pdf. Accessed 19 Jun 2014.

Gold R. Oral therapies for multiple sclerosis: a review of agents in phase III development or recently approved. CNS Drugs. 2011;25(1):37-52.

Hauser SL, Goodin DS. Multiple sclerosis and other demylenating disease. In: Longo DL, Kasper DL, Jameson JL, Fauci SA, Hauser SL, Loscalzo J, editors. Harrisons Principles of Internal Medicine. 18th Edition. New York, NY: McGraw-Hill; 2012:3395-410.

Minagar A. Current and future therapies for multiple sclerosis. Scientifica (Cairo). 2013;2013:249101.

Litjens NH, Burggraaf J, van Strijen E, van Gulpen C, Mattie H, Schoemaker RC, et al. Pharmacokinetics of oral fumarates in healthy subjects. Br J Clin Pharmacol. 2004;58(4):429-32.

Gold R, Kappos L, Arnold DL, Bar-Or A, Giovannoni G, Selmaj K, et al. Placebo-controlled phase 3 study of oral BG-12 for relapsing multiple sclerosis. N Engl J Med. 2012;367(12):1098-107.

Kappos L, Radue EW, O’Connor P, Polman C, Hohlfeld R, Calabresi P, et al. A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. N Engl J Med. 2010;362(5):387-401.

Damal K, Stoker E, Foley JF. Optimizing therapeutics in the management of patients with multiple sclerosis: a review of drug efficacy, dosing, and mechanisms of action. Biologics. 2013;7:247-58.

Polman CH, O’Connor PW, Havrdova E, Hutchinson M, Kappos L, Miller DH, et al. A randomized, placebo-controlled trial of natalizumab for relapsing multiple sclerosis. N Engl J Med. 2006 2;354(9):899-910.

O’Connor P, Wolinsky JS, Confavreux C, Comi G, Kappos L, Olsson TP, et al. Randomized trial of oral teriflunomide for relapsing multiple sclerosis. N Engl J Med. 2011;365(14):1293-303.




How to Cite

Singh, J., Mahajan, B., & Kaushal, S. (2017). Dimethyl fumarate: a novel drug for multiple sclerosis. International Journal of Basic & Clinical Pharmacology, 3(6), 1101–1105. Retrieved from https://www.ijbcp.com/index.php/ijbcp/article/view/1199



New Drug Update