Product Information
Registration Status: ActiveSIN15053P
TECFIDERA GASTRO-RESISTANT HARD CAPSULE 120mg is approved to be sold in Singapore with effective from 2016-07-26. It is marketed by EISAI (SINGAPORE) PTE LTD, with the registration number of SIN15053P.
This product contains Dimethyl fumarate 120mg in the form of CAPSULE, ENTERIC-COATED. It is approved for ORAL use.
This product is manufactured by Vifor SA (Bulk Production and Secondary Packager) in SWITZERLAND, andJANSSEN CILAG S.P.A. (Primary and Secondary Packaging) in ITALY.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}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.
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
Clearance
MMF clearance was not quantified.
Toxicity
The most common side effects observed were nausea, diarrhea, abdominal pain, and flushing.
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 |
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.