Dimethyl fumarate

DB08908ApprovedInvestigationalSmall moleculeAnti-Inflammatory Agents Cytoprotective Agent Immunomodulatory Agents

Dimethyl fumarate is a medication used to treat patients with the relapsing-remitting form of multiple sclerosis. Dimethyl fumarate is an agent indicated for the treatment of relapsing forms of multiple sclerosis.

Mechanism: 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). Both dimethyl fumarate and MMF up-regulate the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. Dimethyl fumarate also suppresses pro-inflammatory genes through nuclear factor kappa B inhibition. Additionally, MMF acts as an agonist at the nicotinic acid receptor, but the relevance of this is unknown.
It has been suggested that dimethyl fumarate exerts its immunomodulatory effects through changes in the composition and phenotype of immune cells. It reduces CNS infiltration and alters the composition of all lymphocyte subpopulations, especially for cytotoxic and effector T cells. This causes a shift from a mainly pro-inflammatory phenotype to an anti-inflammatory one.
Curator reviewed · 3 references
Primary indication: Dimethyl fumarate is indicated for the treatment of relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults.Curator reviewed · 5 structured indications
Formula / weight: C₆H₈O₄ · 144.1253 g/mol (avg)
First approval: Canada, 2013 · United States, 2013 · European Union, 2016
Also known as: Dimethyl trans-ethylenedicarboxylate · Dimethylfumarate
Code names: AZL-O-211089 · BG-00012 · BG-12 · FAG-201 · FP-187 · LAS41008
Brand names: Dimethyl Fumarate Accord
Dimethyl Fumarate Mylan
Dimethyl Fumarate Neuraxpharm
Skilarence
Tecfidera