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DIMETHYL FUMARATE

Luhan pharmachem Co., Ltd. supplies Dimethyl Fumarate bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Dimethyl Fumarate is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.

What is Dimethyl fumarate?

Dimethyl fumarate (DMF) is the methyl ester of fumaric acid. DMF was initially recognized as a very effective hypoxic cell radiosensitizer. Later, seek DMF combined with three other fumaric acid esters (FAE) was licensed in Germany as oral therapy for psoriasis (trade name Fumaderm). Other diseases, such as necrobiosis lipoidica, granuloma annulare, and sarcoidosis were also found to respond to treatment with DMF in case reports or small patient series. Phase III clinical trials found that DMF (BG-12) successfully reduced relapse rate and increased time to progression of disability in multiple sclerosis (trade name Tecfidera). DMF is thought to have immunomodulatory properties without significant immunosuppression.

In a non-medical use, sickness DMF was applied as a biocide in furniture or shoes to prevent growths of mold during storage or transport in a humid climate. However, due to incidences of allergic reactions after skin contact the European Union banned DMF in consumer products since 1998, and since January 2009 the import of products containing DMF was also banned.

Tecfidera was shown to have a significant effect on relapse rate and time to progression in phase III clinical trials of multiple sclerosis. Tecfidera was recommended for approval in the European Union as a peroral treatment for MS by EMA on March 21, 2013

Mechanism of action

The precise mechanism of action of dimethyl fumarate is unknown. The compound (and its metabolite, monomethyl fumarate) activates the nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway and has been identified as a nicotinic acid receptor agonist in vitro. Dimethyl fumarate is a lipophilic, highly mobile molecule in human tissue. As a ?,?-unsaturated electrophilic compound, dimethyl fumarate is rapidly attacked by the detoxifying agent glutathione (GSH) in a Michael addition reaction. Dimethyl fumarate is highly reactive: when administered orally, it does not survive long enough to be absorbed into blood without being attacked by GSH. However, part of it is hydrolyzed by esterases to produce monomethylfumarate, which is more resistant.

Adverse Effects

One serious side effect that has been described is progressive multifocal leukoencephalopathy.

Disclaimer:

Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.

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