Description
Dimethyl fumarate is a fumaric acid methyl ester that is clinically used to treat psoriasis and under investigation as a potential treatment for multiple sclerosis (MS). Dimethyl fumarate exhibits immunomodulatory, antioxidative, and anti-inflammatory activities. In vitro, dimethyl fumarate increases expression of heme oxygenase 1 (HO-1) and Nrf2 and decreases proliferation of T cells and release of inflammatory cytokines. Dimethyl fumarate activates nicotinic acetylcholine receptors (nAChRs), although the relevance of this activity is unknown. Previously, this compound has been used as a radiosensitizer. Recently, dimethyl fumarate has displayed efficacy in models of multiple sclerosis, decreasing relapse and improving neurologic outcomes.
References
Fox RJ, Miller DH, Phillips JT, et al. Placebo-controlled phase 3 study of oral BG-12 or glatiramer in multiple sclerosis. N Engl J Med. 2012 Sep 20;367(12):1087-97. Erratum in: N Engl J Med. 2012 Oct 25;367(17):1673. PMID: 22992072.
Scannevin RH, Chollate S, Jung MY, et al. Fumarates promote cytoprotection of central nervous system cells against oxidative stress via the nuclear factor (erythroid-derived 2)-like 2 pathway. J Pharmacol Exp Ther. 2012 Apr;341(1):274-84. PMID: 22267202.
Lehmann JC, Listopad JJ, Rentzsch CU, et al. Dimethylfumarate induces immunosuppression via glutathione depletion and subsequent induction of heme oxygenase 1. J Invest Dermatol. 2007 Apr;127(4):835-45. PMID: 17235328.
Held KD, Epp ER, Clark EP, et al. Effect of dimethyl fumarate on the radiation sensitivity of mammalian cells in vitro. Radiat Res. 1988 Sep;115(3):495-502. PMID: 3174933.