富马酸二甲酯 (Tecfidera, Skilarence, Dimethyl fumarate Neuraxpharm +3)

概览

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

作用机制

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.

适应症

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.

• Clinically Isolated Syndrome (CIS)
• Relapsing Forms of MS
• Relapsing Remitting Multiple Sclerosis (RRMS)
• Active Secondary Progressive Multiple Sclerosis (SPMS)