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

Findings that BG-12 activated Nrf2 in astrocytes, but not in C6 cells, help explain results that GSH enzymes are induced and GSH levels only increased in astrocytes. [source, 2011]
Finally, since increased GSH levels can reduce the effective concentrations of BG-12 able to react with its protein targets (e.g. p65 and Keap1), our findings suggest a complex relationship in which compensatory responses to BG-12, designed to maintain an anti-oxidative state, may limit its anti-inflammatory properties. [source, 2011]
The study used a second generation fumaric acid derivate (BG-12) that was developed by Fumapharm AG and BiogenIdec Inc. and contains DMF [1, 28] as enteric-coated microtablet to improve gastrointestinal tolerability. [source, 2009]
The 257 patients were randomized in four groups to receive either placebo or BG-12 at 120, 360, 720 mg/d for 6 month, followed by another 6 month of a dose-blinded safety extension study where the placebo group received the highest dose of 720 mg/d. [source, 2009]
In comparison to the placebo group, the high-dose BG-12 group displayed a statistically significant reduction of 69% in the mean number of Gd+ enhancing lesions as measured by monthly MRI between weeks 12 and 24. [source, 2009]
In general, BG-12 appears to have a promising short-term efficacy and safety profile. [source, 2009]
To determine the long-term safety and efficacy of BG-12, a phase III study program already started in Europe and North America. [source, 2009]