How does Vumerity (diroximel fumarate) work?
Medically reviewed by N. France, BPharm. Last updated on Dec 6, 2020.
Vumerity contains diroximel fumarate. Diroximel fumarate is rapidly converted in the body to monomethyl fumarate (MMF), which is the same active metabolite Tecfidera (dimethyl fumarate) has.
It is not yet known exactly how Vumerity works - what its mechanism of action is - in the treatment of MS.
MS is a condition in which a person’s own immune system mistakenly attacks the central nervous system (CNS), causing inflammation and damage to myelin, which forms fatty sheaths around nerve cells to protect them.
It is thought that Vumerity may modulate the immune system to reduce the amount of inflammation it causes. It is also thought to have anti-oxidative properties that help protect key parts of the CNS from damage, including the brain and spinal cord.
MMF, the active metabolite of Vumerity, activates the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway. The Nrf2 protein’s antioxidant properties are thought to reduce damage caused by oxidative stress, which contributes to the nerve damage caused by MS.
MMF also activates the hydroxycarboxylic acid receptor 2 (HCAR2). This interaction with HCAR2 results in anti-inflammatory activity, especially in immune cells.
It’s unclear whether it plays a role in its ability to help in the treatment of MS, but MMF is also a nicotinic acid receptor agonist.
- National Multiple Sclerosis Society. FDA Approves Oral Vumerity (Drioximel Fumarate), Similar to Tecfidera, for Relapsing MS. October 30, 2019. Available from: https://www.nationalmssociety.org/About-the-Society/News/FDA-Approves-Oral-Vumerity%E2%84%A2-(Diroximel-Fumarate),. [Accessed December 7, 2020].
- Biogen. Biogen and Almermes announce FDA approval of Vulmerity (Diroximel Fumarate) for Multiple Sclerosis. October 30, 2019. Available from: https://investors.biogen.com/news-releases/news-release-details/biogen-and-alkermes-announce-fda-approval-vumeritytm-diroximel. [Accessed December 7, 2020].
- National Multiple Sclerosis Society. Vumerity. Available from: https://www.nationalmssociety.org/Treating-MS/Medications/Vumerity. [Accessed December 7, 2020].
- National Institute for Health Research (NIHR). Diroximel fumarate for relapsing-remitting multiple sclerosis. May 2019. Available from: http://www.io.nihr.ac.uk/report/diroximel-fumarate-for-relapsing-remitting-multiple-sclerosis/. [Accessed December 7, 2020].
- Parodi B, Rossi S, Morando S, et al. Fumarates modulate microglia activation through a novel HCAR2 signaling pathway and rescue synaptic dysregulation in inflamed CNS. Acta Neuropathol. 2015;130(2):279-295. doi:10.1007/s00401-015-1422-3.
- Yadav SK, Soin D, Ito K, Dhib-Jalbut S. Insight into the mechanism of action of dimethyl fumarate in multiple sclerosis. J Mol Med (Berl). 2019 Apr;97(4):463-472. doi: 10.1007/s00109-019-01761-5. Epub 2019 Feb 28. PMID: 30820593.
- Kourakis, S.; Timpani, C.A.; de Haan, J.B.; Gueven, N.; Fischer, D.; Rybalka, E. Dimethyl Fumarate and Its Esters: A Drug with Broad Clinical Utility? Pharmaceuticals 2020, 13(10), 306; https://doi.org/10.3390/ph13100306.
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