“Dimethyl-fumarate, DMF or BG12 is an effective DMT. It is given orally as a twice a day dose. One of the main side effects of the drug is facial flushing that comes on shortly after taking the tablet and subsides within 4-6 weeks. Occasionally the flushing is severe and results in MSers stopping BG12. It is therefore welcome to see the paper below that shows aspirin can reduce this side effect. This should make BG12 more tolerable.”
“Us Europeans are still waiting for a decision from Biogen-Idec about if and when the drug will be launched. Let’s hope soon. I have several patients under my care who are waiting patiently to start this medication. It will be a great tragedy if we can’t access the drug.”
BACKGROUND: Delayed-release dimethyl fumarate (DR-DMF) has cytoprotective and antiinflammatory properties and has recently been approved in the United States as an oral treatment for relapsing forms of multiple sclerosis. The most common adverse events associated with DR-DMF are flushing and gastrointestinal (GI) events, the incidences of which diminish over time.
METHODS: Healthy volunteers (N = 56) were randomized to receive different dosing regimens of DR-DMF or matching placebo with or without pretreatment with 325 mg aspirin for 4 days. Plasma levels of the active metabolite monomethyl fumarate were assessed on days 1 and 4. Flushing and GI events were assessed using patient-reported scales. Potential flushing mediators were explored.
CONCLUSIONS: In healthy volunteers, DR-DMF was well tolerated over 4 days of dosing, with a PK profile consistent with that previously reported and no evidence of accumulation. Aspirin pretreatment reduced the incidence and intensity of flushing without affecting GI events or the DR-DMF PK profile. Elevated levels of PGD2 in some DR-DMF-treated individuals suggest that flushing may be, at least in part, prostaglandin mediated.