Products
Dimethyl fumarate is commercially available in the form of capsules with enteric-coated microtablets (Tecfidera). It has been approved in many countries since 2014. Dimethyl fumarate is also approved for the treatment of psoriasis (Skilarence). This article is related to MS therapy. In 2019, a new prodrug of the active ingredient was approved; see diroximelfumarate (Vumerity).
Structure and properties
Dimethyl fumarate (C6H8O4, Mr = 144.1 g/mol) exists as a white powder that is readily soluble in water. It is a derivative of fumaric acid. Monomethyl fumarate is the active metabolite of dimethyl fumarate. This is also formed from diroximel fumarate.
Effects
Dimethyl fumarate (ATC N07XX09) has immunomodulatory, anti-inflammatory, and neuroprotective properties. It reduces the frequency of relapses, the appearance of MS lesions in the brain, and slows disease progression. The effects are thought to be due to activation of the Nrf2 (nuclear 1 factor (erythroid-derived 2)-like 2 antioxidant response pathway). This is an important cellular mechanism against the cell-damaging effects of oxidative stress and the inflammatory response.
Indications
For the treatment of multiple sclerosis.
Dosage
According to the SmPC. Capsules are taken twice daily with a meal. Taking with food may reduce the occurrence of flushing.
Contraindications
Full details of precautions and interactions can be found in the drug label.
Adverse effects
The most common possible adverse effects include flushing (redness of the skin and feeling of heat) and digestive disturbances such as abdominal pain, diarrhea, and nausea. Dimethyl fumarate may cause lymphopenia (reduction in the number of lymphocytes), leading to the occurrence of infectious diseases.
