Dimethyl Fumarate

Dimethyl Fumarate Uses, Dosage, Side Effects, Food Interaction and all others data.

Dimethyl Fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF) then MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. Dimethyl Fumarate is marketed under the brand name Tecfidera.

The physiological effects dimethyl fumarate has on the body is not well understood. It is known that dimethyl fumarate has anti-inflammatory and cytoprotective effects, which both are likely involved in its actions in multiple sclerosis patients.

Trade Name Dimethyl Fumarate
Generic Dimethyl fumarate
Dimethyl fumarate Other Names Dimethyl fumarate, Dimethyl trans-ethylenedicarboxylate, Dimethylfumarat
Weight 120mg, 240mg
Type Oral delayed release capsule
Formula C6H8O4
Weight Average: 144.1253
Monoisotopic: 144.042258744
Protein binding

MMF has a plasma protein binding range of 27 to 45%, and the binding is concentration independent.

Groups Approved, Investigational
Therapeutic Class
Manufacturer
Available Country United States
Last Updated: September 19, 2023 at 7:00 am
Dimethyl Fumarate
Dimethyl Fumarate

Uses

Dimethyl Fumarate is a medication used to treat patients with the relapsing-remitting form of multiple sclerosis.

Used in multiple sclerosis patients with relapsing forms.

Dimethyl Fumarate is also used to associated treatment for these conditions: Disseminated Sclerosis

How Dimethyl Fumarate works

The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF). MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. As well MMF is an agonist at the nicotinic acid receptor, but the relevance of this is not known.

Toxicity

The most common side effects observed were nausea, diarrhea, abdominal pain, and flushing.

Food Interaction

  • Take with food. Co-administration with food may reduce gastrointestinal upset and flushing.

Volume of Distribution

In healthy people, MMF has a variable volume of distribution of 53 to 73 litres.

Elimination Route

Once ingested, dimethyl fumarate is rapidly hydroylyzed by esterases to MMF. Thus there is negligible amount of dimethyl fumarate in the body, and all pharmacokinetic information is quantified with MMF. In multiple sclerosis patients, the time to maximum concentration of MMF is 2 to 2.5 hours and the maximum concentration is 1.87 mg/L.

Half Life

MMF has a short half life of about 1 hour, and MMF does not accumulate after repeated doses of dimethyl fumarate.

Clearance

MMF clearance was not quantified.

Elimination Route

The main route of elimination is by CO2 exhalation that accounts for 60% of the dose. The other minor routes are through the kidney (16% metabolites and trace amounts of unchanged MMF) and the feces (1%).

Innovators Monograph

You find simplified version here Dimethyl Fumarate

*** Taking medicines without doctor's advice can cause long-term problems.
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