Tecfidera (BG-12, dimethyl fumarate, or DMF) is an oral formulation approved by the U.S. Food and Drug Administration (FDA) for relapsing forms of multiple sclerosis (MS). It also has been studied or used to treat several forms of inflammatory diseases, such as sarcoidosis, psoriasis, and the skin condition necrobiosis lipoidica.
Tecfidera was initially developed and marketed by Biogen. Several generic forms of dimethyl fumarate have also been approved in the U.S. at 120 and 240 mg doses including those produced by Cipla, Glenmark Pharmaceuticals, Lupin, Mylan, and Zydus Cadila.
Clinical trials of Tecfidera demonstrated its immunomodulatory effects in MS patients, where it was seen to significantly reduce relapse rates and to increase time to disease progression compared to a placebo. Despite its immunomodulatory properties, it does not induce immune suppression.
Tecfidera is more suitably called a therapeutic agent than a disease-modifying agent. This is because while the drug reduces the exacerbations and flares that progress MS to more severe states, and lead to improvements in disease markers like brain lesions, its continued effects on disease progression are still under investigation.
Biogen presented post-hoc analysis data at the 68th annual meeting of the American Academy of Neurology (AAN) in April 2016 showing strong and sustained effectiveness in newly diagnosed relapsing-remitting multiple sclerosis (RRMS) patients, and further supporting the drug’s long-term safety profile.
Data from 13 years of use for Tecfidera was presented at the MSVirtual2020 conference showing that the treatment continues to be safe and effective at reducing the progression of disability and the frequency of relapses.
The drug was approved as a first-line oral RRMS treatment by the U.S. FDA in March 2013, and similarly approved for use in the European Union in February 2014. It has also been approved for such use in Canada, Australia, and Switzerland.
How Tecfidera works
It was previously hypothesized that Tecfidera acted antagonistically to the inflammation and oxidative stress cycle created within the central nervous system (CNS) that leads to demyelination of nerve fibers, and induced direct cytoprotective responses in CNS cells. Specifically, researchers believed that the therapy affected the Nrf2 (nuclear factor [erythroid-derived 2]-like 2) pathway, which is pivotal in cellular responses to oxidative stress.
However, findings from a 2016 study titled “Chemical proteomic map of dimethyl fumarate–sensitive cysteines in primary human T-cells,” published in the journal Science Signaling, revealed that the drug’s mechanism of action works by reducing the activation of the immune system.
By utilizing a novel mapping system to help detect how a drug interacts with proteins by highlighting the link between a drug and an amino acid called cysteine, the research team determined that Tecfidera interacts with many of the proteins that are involved in activating immune T-cells, which are known contributors to MS, and in doing so prevents T-cell activation by binding to several proteins on the surface of these cells.
Under physician care, this oral drug can be taken with or without food, twice daily. The recommended initial dose is 120 mg twice a day, increased after seven days to the maintenance dose of 240 mg twice daily. The most common side effects include itching, allergies, rashes, and flushing, along with mild to moderate diarrhea, nausea, and dizziness. Any patient with serious infection should consult with a physician before taking Tecfidera, as treatment initially lowers a person’s white blood cell count (lymphocytes), cells that help to protect against infection. The FDA recommends that a patient’s lymphocyte count be assessed while under treatment.
The use or importation of DMF as an anti-fungal formulation in consumer products has been banned in the European Union after reports of allergic reactions due to skin contact.
The most common side effects of Tecfidera include redness, flushing, itching, rash, nausea, vomiting, stomach pain, diarrhea, and indigestion.
Last updated: Nov. 14, 2020
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