Tecfidera

Chinese name: Dimethyl fumarate

Trade name: Tecfidera

Indications:

Dimethyl fumarate enteric-coated capsules are suitable for the treatment of relapsing multiple sclerosis (MS) in adults, including clinically isolated syndrome, relapsing-remitting disease and active secondary progressive disease.

Usage and Dosage:

The starting dose of dimethyl fumarate is 120 mg orally twice daily. After 7 days, the dose should be increased to a maintenance dose of 240 mg orally twice daily. For individuals who cannot tolerate the maintenance dose, a temporary dose reduction to 120 mg twice daily may be considered. Within 4 weeks, the recommended dose of 240 mg twice daily should be resumed. Discontinuation of dimethyl fumarate should be considered in patients who cannot tolerate return to maintenance doses. Dimethyl fumarate may reduce the incidence of flushing when administered with food. Alternatively, administration of non-enteric-coated aspirin (up to 325 mg) 30 minutes before dimethyl fumarate administration may reduce the incidence or severity of flushing.

The most common adverse reactions of dimethyl fumarate (incidence ≥10% and ≥2% more than placebo) are flushing, abdominal pain, diarrhea and nausea.

The mechanism by which dimethyl fumarate (DMF) exerts its therapeutic effect in multiple sclerosis is unclear. DMF and the metabolite monomethyl fumarate (MMF) have been shown to activate the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in cellular responses to oxidative stress. MMF has been identified as a nicotinic acid receptor agonist in vitro.