Текфидера
Текфидера Uses, Dosage, Side Effects, Food Interaction and all others data.
Текфидера 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. Текфидера is marketed under the brand name Tecfidera.
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.
| Trade Name | Текфидера |
| Generic | Dimethyl fumarate |
| Dimethyl fumarate Other Names | Dimethyl fumarate, Dimethyl trans-ethylenedicarboxylate, Dimethylfumarat |
| Type | |
| Formula | C6H8O4 |
| Weight | Average: 144.1253 Monoisotopic: 144.042258744 |
| Protein binding | MMF has a plasma protein binding range of 27 to 45%, and the binding is concentration independent. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Russia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Текфидера is a medication used to treat patients with the relapsing-remitting form of multiple sclerosis.
Used in multiple sclerosis patients with relapsing forms.
Текфидера is also used to associated treatment for these conditions: Disseminated Sclerosis
How Текфидера works
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.
Toxicity
The most common side effects observed were nausea, diarrhea, abdominal pain, and flushing.
Food Interaction
- Take with food. Co-administration with food may reduce gastrointestinal upset and flushing.
Volume of Distribution
In healthy people, MMF has a variable volume of distribution of 53 to 73 litres.
Elimination Route
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.
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.
Elimination Route
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%).
Innovators Monograph
You find simplified version here Текфидера
