TECFIDERA GASTRO-RESISTANT HARD CAPSULE 120mg

Dimethyl fumarate

Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.

Active Ingredient / Synonyms

(E)-But-2-enedioic acid dimethyl ester | 1,2-bis(methoxycarbonyl)-trans-ethylene | dimethyl (E) butenedioate | Dimethyl trans-ethylenedicarboxylate | Fumaric acid, dimethyl ester | trans-1,2-Ethylenedicarboxylic acid dimethyl ester | trans-Butenedioic acid dimethyl ester | Dimethyl fumarate |

Description

Dimethyl fumarate is an anti-inflammatory. It is indicated for multiple sclerosis patients with relapsing forms and is also being investigated for the treatment of psoriasis. The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF) then MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. Dimethyl fumarate is marketed under the brand name Tecfidera.

Indication

Used in multiple sclerosis patients with relapsing forms.

Mechanism of Action

The mechanism of action of dimethyl fumarate in multiple sclerosis is not well understood. It is thought to involve dimethyl fumarate degradation to its active metabolite monomethyl fumarate (MMF). MMF up-regulates the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway that is activated in response to oxidative stress. As well MMF is an agonist at the nicotinic acid receptor, but the relevance of this is not known.

Pharmacodynamics

The physiological effects dimethyl fumarate has on the body is not well understood. It is known that dimethyl fumarate has anti-inflammatory and cytoprotective effects, which both are likely involved in its actions in multiple sclerosis patients.

Pharmacokinetics

Absorption:

Once ingested, dimethyl fumarate is rapidly hydroylyzed by esterases to MMF. Thus there is negligible amount of dimethyl fumarate in the body, and all pharmacokinetic information is quantified with MMF. In multiple sclerosis patients, the time to maximum concentration of MMF is 2 to 2.5 hours and the maximum concentration is 1.87 mg/L.

Distribution:

In healthy people, MMF has a variable volume of distribution of 53 to 73 litres.

Metabolism:

Dimethly fumarate is hydrozlied to its metabolite MMF in the GIT, tissues, and blood by esterases. MMF then undergoes subsequent metabolism in the tricarboxylic acid (TCA) cycle. Altogether the main metabolites formed are MMF, glucose, citric acid, and fumaric.

Elimination:

The main route of elimination is by CO2 exhalation that accounts for 60% of the dose. The other minor routes are through the kidney (16% metabolites and trace amounts of unchanged MMF) and the feces (1%).

Half-life

MMF has a short half life of about 1 hour, and MMF does not accumulate after repeated doses of dimethyl fumarate.

Clearance

MMF clearance was not quantified.

Toxicity

The most common side effects observed were nausea, diarrhea, abdominal pain, and flushing.

References

  1. Health Science Authority of Singapore - Reclassified POM
  2. Drugbank

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Approval Information

TECFIDERA GASTRO-RESISTANT HARD CAPSULE 120mg was registered with Health Science Authority of Singapore by EISAI (SINGAPORE) PTE LTD. It is marketed with the registration number of SIN15053P with effective from 2016-07-26.

This product contains 120mg of Dimethyl fumarate in the form of CAPSULE, ENTERIC-COATED.

The medicine was manufactured by Vifor SA in SWITZERLAND

It is a Presciption Only Medicine which can only be obtained from a doctor or a dentist, or from a pharmacist with a prescription from a Singapore-registered doctor or dentist.

Anatomical Therapeutic Chemical (ATC) Classification

ATC Code: N07XX59

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