BG-12 (dimethyl fumarate)
- Oral medication taken daily.
- This drug may have a distinct dual mechanism of action. First, it is an immunomodulator with anti-inflammatory properties. This induces inflammatory cytokines and appears to suppress damaging macrophage activity (immune cells that stimulate lymphocytes) as part of its anti-inflammatory activity. Second, BG-12 may also have neuroprotective effects. This is due to its activation of a substance that is critical for resistance to cellular damage from what is termed "oxidative stress" as well as for normal immune function. BG-12 is being studied in RRMS.
- The ongoing Phase III DEFINE and CONFIRM studies are no longer enrolling participants and these studies will be completed in December 2010 and April 2011, respectively. The DEFINE study is comparing two doses of BG-12 against placebo in 1,011 patients. The primary outcome measure is the proportion of patients who experience relapses. The CONFIRM study is testing two levels of the drug against Copaxone and placebo in 1,232 patients, with the primary measure of the reduction in relapse rate.
- The Phase II EXPLORE trial will evaluate oral BG-12 as a combination therapy for patients who continue to experience disease progression despite ongoing treatment. It will evaluate the safety and tolerability of BG-12 when administered with interferons or Copaxone to 100 people who continue to have evidence of disease activity (despite receiving consistent monotherapy for at least a year). Efficacy endpoints will also be assessed in a subset of participants.
- Trials to date indicate that the drug is safe and that its overall tolerability improves with continued use. A long-term Phase III efficacy and safety study is enrolling approximately 1,700 individuals who participated in earlier trials.
- Side effects include skin flushing and gastrointestinal symptoms.