Drug intelligence / Profile preview

dimethyl fumarate

Development stage
Approved
Lead developer
Biogen
Modality
Small Molecules
Administration
Oral
01

Overview

Dimethyl fumarate is an oral small molecule drug primarily used to treat relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome (CIS), relapsing-remitting MS (RRMS), and active secondary progressive MS. It was originally developed by Biogen and approved by the FDA in 2013 for MS. In Europe and China it is also approved for these indications. The drug acts as a prodrug that is rapidly converted to its active metabolite monomethyl fumarate after oral administration. Its mechanism involves activation of the Nrf2 pathway—a key regulator of cellular antioxidant response—leading to immunomodulatory and cytoprotective effects such as reduced inflammation and protection against oxidative stress-induced neuronal damage. Additionally, it inhibits nuclear factor kappa B (NF-κB) signaling and shifts immune cell phenotypes from pro-inflammatory to anti-inflammatory states[1][3][6][8][9]. In Germany, a combination product containing dimethyl fumarate with other esters is used for psoriasis; however, pure dimethyl fumarate has also been studied for this indication[2][3].

Brand names
TecfideraSkilarenceDimethyl Fumarate AccordDimethyl Fumarate MylanDimethyl Fumarate Neuraxpharm
Other names
富马酸二甲酯dimethyl fumaric acid ester
02

Targets

HCAR2 (Hydroxycarboxylic acid receptor 2)KEAP1 (Kelch-like ECH-associated protein 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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