Tecfidera Dimethyl Fumarate Enteric Capsules

1. Indications and Usage
Relapsing Forms of Multiple Sclerosis (RMS): Treatment of adults with RMS, including clinically isolated syndrome (CIS), relapsing-remitting MS (RRMS), and active secondary progressive MS (SPMS) .
2. Dosage and Administration
Administration: Oral administration. Capsules must be swallowed whole and not chewed, crushed, or dissolved.
Food Requirement: Can be taken with or without food. Taking the medication with food may reduce the incidence of flushing and gastrointestinal symptoms .
Titration (Dose Escalation): To improve gastrointestinal tolerability, treatment is initiated with a 7-day titration period:
Days 1–7: 120 mg twice daily.
Day 8 onwards: Recommended maintenance dose of 240 mg twice daily.
If the patient cannot tolerate the 240 mg dose, it may be temporarily reduced to 120 mg twice daily .
Missed Dose: If a dose is missed, take it as soon as possible and resume the normal schedule. Do not take a double dose .
3. Mechanism of Action
Dimethyl fumarate is an Nrf2 pathway activator.
It inhibits the enzyme NAD(P)H:quinone oxidoreductase 1 (NQO1) and activates the Nrf2 pathway, which mediates the cellular response to oxidative stress.
This results in anti-inflammatory and cytoprotective effects, reducing the accumulation of physical disability and frequency of clinical exacerbations in MS .
4. Safety and Warnings
Lymphocytopenia: Can cause a reduction in lymphocyte count. Monitor complete blood counts (CBC) regularly. Discontinue if severe lymphocytopenia (<500 cells/mm³) persists for more than 6 months .
Progressive Multifocal Leukoencephalopathy (PML): A rare but serious brain infection (JC virus) has been reported, primarily in patients with prolonged severe lymphocytopenia. Discontinue immediately if PML is suspected .
Serious Allergic Reactions: Anaphylaxis and angioedema have been reported. Discontinue if these occur .
Hepatotoxicity: Monitor liver enzymes (ALT, AST) periodically, especially during the first 6 months of treatment .
Gastrointestinal Events: Flushing, abdominal pain, diarrhea, and nausea are common, especially during the first month .
5. Adverse Reactions
Common adverse reactions (incidence ≥10%) include:
General: Flushing (redness of the face/neck).
Gastrointestinal: Abdominal pain, Diarrhea, Nausea.
Dermatologic: Rash, Pruritus, Hot flush .
6. Drug Interactions
N-acetyl-L-cysteine (NAC): Co-administration is not recommended as it may reduce the efficacy of Dimethyl Fumarate by binding to it .
CYP450 Interactions: It is not metabolized by CYP450 enzymes, and drug interactions via this pathway are unlikely .
7. Pharmaceutical Information
Chemical Name: Dimethyl (E)-but-2-enedioate.
Molecular Formula: C6H8O4.
Storage: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) .