BG-12 NF-kB Activation Inhibitor Treatment of Multiple Sclerosis

摘要

BG-12 is an oral second-generation formulation of dimethyl fumarate (DMF), a fumarie acid ester (FAE). FAEs are licensed in some countries for the therapy of severe psoriasis. Due to their immunomodulatory effects, FAEs were proposed as a treatment for multiple sclerosis (MS). In a recent phase II clinical trial in patients with relapsing-remitting (RR) MS, BG-12 was shown to reduce Gd+-enhancing lesions and newly enlarging 12 lesions on MRI. To explore the long-term efficacy and safety, two international multicenter phase III trials are ongoing. Here we summarize the findings from clinical trials and many in vivo and in vitro studies on the mechanisms of action of BG-12. Both immunomodulatory and potential neuroprotective mechanisms have been proposed. The results of the phase III clinical trials need to be awaited until the role of BG-12 in the treatment of MS can be definitively assessed.