Recent advances in the biomedical applications of fumaric acid and its ester derivatives: The multifaceted alternative therapeutics

Pharmacol Rep. 2016 Apr;68(2):404-14. doi: 10.1016/j.pharep.2015.10.007. Epub 2015 Nov 2.

Abstract

Several lines of evidence have demonstrated the potential biomedical applications of fumaric acid (FA) and its ester derivatives against many human disease conditions. Fumaric acid esters (FAEs) have been licensed for the systemic treatment of the immune-mediated disease psoriasis. Biogen Idec Inc. announced about the safety and efficacy of the formulation FAE (BG-12) for treating RRMS (relapsing-remitting multiple sclerosis). Another FAE formulation DMF (dimethyl fumarate) was found to be capable of reduction in inflammatory cardiac conditions, such as autoimmune myocarditis and ischemia and reperfusion. DMF has also been reported to be effective as a potential neuroprotectant against the HIV-associated neurocognitive disorders (HAND). Many in vivo studies carried out on rat and mice models indicated inhibitory effects of fumaric acid on carcinogenesis of different origins. Moreover, FAEs has emerged as an important matrix ingredient in the fabrication of biodegradable scaffolds for tissue engineering applications. Drug delivery vehicles composed of FAEs have shown promising results in delivering some leading drug molecules. Apart from these specific applications and findings, many more studies on FAEs have revealed new therapeutic potentials with the scope of clinical applications. However, until now, this scattered vital information has not been written into a collective account and analyzed for minute details. The aim of this paper is to review the advancement made in the biomedical application of FA and FAEs and to focus on the clinical investigation and molecular interpretation of the beneficial effects of FA and FAEs.

Keywords: Anti-cancer; Fumaric acid esters; Immunomodulatory; Tecfidera; Tissue engineering.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Dimethyl Fumarate / pharmacology
  • Dimethyl Fumarate / therapeutic use
  • Esters / pharmacology*
  • Esters / therapeutic use*
  • Fumarates / pharmacology*
  • Fumarates / therapeutic use*
  • Humans
  • Multiple Sclerosis, Relapsing-Remitting / drug therapy
  • Neuroprotective Agents / pharmacology
  • Neuroprotective Agents / therapeutic use
  • Psoriasis / drug therapy

Substances

  • Esters
  • Fumarates
  • Neuroprotective Agents
  • fumaric acid
  • Dimethyl Fumarate