Latest research on BG-12

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.

Latest findings

This compound, dimethyl fumarate (DMF), which is a methyl ester of fumaric acid, is the only oral administration DMT to be approved by both FDA and the European Medicines Agency (EMA), with the trade name Tecfidera. [source, 2016]
As a consequence, BG-12, a specific oral preparation of DMF, has already been showed in two phase III trials as being able to reduce relapse episodes as well as to delay disease progression in patients affected by RR-MS [87–89]. [source, 2016]
In these trials, BG-12 was well tolerated, the most common side effects being characterized by redness, gastrointestinal symptoms, and headaches. [source, 2016]
Another phase III clinic trial is currently investigating BG-12 long-term safety profile with the main aim of using it in the future as a first-line DMT. [source, 2016]
Although several Nrf2-activating molecules have demonstrated efficacy in a variety of preclinical animal models of brain disease, BG-12 (dimethyl fumarate) has emerged as a particularly promising agent. [source, 2015]
BG-12 is a cytoprotective compound licensed for relapsing remitting multiple sclerosis, which activates Nrf2-mediated gene expression and has a mechanism of action (at least in animal models) that is dependent on Nrf2 (refs 58, 59). [source, 2015]
Tecfidera™ (BG-12) is an oral formulation of the FAE, containing the active metabolite dimethyl fumarate (DMF), which showed remarkable efficacy in lowering relapse rates in two phase III clinical trials of relapsing-remitting MS (RR-MS) treatment [12,13,14,15,16]. [source, 2015]
Besides natalizumab, PML has recently been reported in two MS patients treated with fingolimod [36] and one patient treated with Tecfidera [37] without prior exposure to other immunosuppressants. [source, 2015]
(1)] and, most recently, with the use of drugs containing fumarates (used in the treatment of psoriasis and also the MS drug Tecfidera) (3). [source, 2015]
Successful repurposing of drugs is not new; examples include dimethyl fumarate (Tecfidera)—originally marketed as a therapy for psoriasis, but later developed as a disease modifying therapy for relapsing-remitting MS (RRMS) [11]. [source, 2015]