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
anti-inflammatory cytokines (small proteins that
may stimulate or inhibit the function of other
cells) and appears to suppress damaging
macrophage cell 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 initially being studied
- The Phase III DEFINE study, which compared
two doses of BG-12 against placebo in 1,200
patients, was completed in February 2011. After
two years of treatment, BG-12 reduced relapses
by 49 percent, and decreased the rate of
disability progression by 38 percent.
- The Phase III CONFIRM study, completed in
September 2011, tested two dose levels against
Copaxone and placebo in 1,232 patients. The
primary measure was a reduction in relapse rate.
- A Phase III continuation study of 1,700 patients
who participated in the DEFINE and CONFIRM
studies will evaluate the long-term safety profile
of BG-12 as well as its long-term efficacy on
clinical outcomes, MRI scans, and quality-of-life.
The study will be completed in June 2013.
- The Phase II EXPLORE trial is evaluating 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 in combination with interferons or
Copaxone to 100 people (who continue to have
evidence of disease activity despite receiving
consistent monotherapy for at least one year).
Efficacy endpoints will also be assessed in a
subset of participants. The study began in May
2010 and will be completed in October 2011.
- Trials to date indicate that BG-12 is safe and that
its overall tolerability improves with continued
use. Side effects include skin flushing and