Dimethyl Fumarate

Dimethyl Fumarate
File:Dimethyl fumarate.svg
INN
Drug class
Routes of administration	Oral
Pregnancy category
Bioavailability	2-3%
Metabolism	Hydrolysis, then CYP-independent metabolism
Elimination half-life	0.5-1 hour
Excretion	CO2 (60%), renal (16%), fecal (1%)
Legal status
CAS Number	624-49-7
PubChem	637568
DrugBank	DB08908
ChemSpider	553679
KEGG	D03630

Dimethyl fumarate (DMF) is a medication primarily used to treat multiple sclerosis (MS) and psoriasis. It is marketed under the brand name Tecfidera among others. DMF is an oral medication that modulates the immune system and has anti-inflammatory properties.

Medical Uses

Dimethyl fumarate is used in the treatment of relapsing-remitting multiple sclerosis (RRMS), a form of multiple sclerosis characterized by episodes of new or increasing neurological symptoms. It is also used for the treatment of moderate to severe psoriasis, a chronic autoimmune skin condition.

Mechanism of Action

The exact mechanism by which dimethyl fumarate exerts its effects in multiple sclerosis is not fully understood. However, it is believed to involve the activation of the Nrf2 pathway, which leads to a reduction in oxidative stress and inflammation. This pathway is thought to protect against neurodegeneration and promote cellular homeostasis.

Side Effects

Common side effects of dimethyl fumarate include flushing, gastrointestinal events such as diarrhea, nausea, and abdominal pain. Serious side effects may include progressive multifocal leukoencephalopathy (PML), a rare brain infection, and lymphopenia, a decrease in white blood cells.

Pharmacokinetics

Dimethyl fumarate is rapidly absorbed after oral administration and is extensively metabolized by esterases to its active metabolite, monomethyl fumarate (MMF). The drug has a short half-life of approximately 0.5 to 1 hour and is primarily excreted as carbon dioxide through exhalation, with minor renal and fecal excretion.

History

Dimethyl fumarate was approved for medical use in the United States in 2013 and in the European Union in 2014. It was initially developed as a treatment for psoriasis before being repurposed for multiple sclerosis.

See Also

• Multiple sclerosis treatment
• Psoriasis treatment

References

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External Links

• Tecfidera on Drugs.com
• National MS Society - Tecfidera