Tecfidera Dimethyl Fumarate Enteric Capsules

1. Indications and Usage
Relapsing Forms of Multiple Sclerosis (RMS):
Treatment of adult patients with RMS, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.
2. Dosage and Administration
Route of Administration:
For Oral Use ONLY.
Recommended Dosage:
Titration (Weeks 0–4): 120 mg taken orally twice daily for the first 7 days.
Maintenance (Week 5 onwards): 240 mg taken orally twice daily.
Management of Intolerance: If the maintenance dose is not tolerated, the dose may be temporarily reduced to 120 mg twice daily for up to 4 weeks.
Administration:
Swallow capsules whole; do not crush, chew, or open.
Taking with food may reduce flushing and gastrointestinal symptoms.
3. Mechanism of Action
Nrf2 Pathway Activation:
Dimethyl fumarate (DMF) is a small molecule that, upon conversion to mono-methyl fumarate (MMF), activates the Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) pathway.
Cytoprotective Effects:
Activation of the Nrf2 pathway induces an antioxidant and cytoprotective response, protecting cells from oxidative stress and inflammation.
Immunomodulation:
DMF modulates immune responses by shifting T-cell immunity from pro-inflammatory Th1/Th17 phenotypes to anti-inflammatory Th2/Treg phenotypes.
4. Safety and Warnings
Anaphylaxis and Angioedema:
Serious hypersensitivity reactions have occurred. Discontinue immediately if signs (e.g., difficulty breathing, throat swelling) appear.
Progressive Multifocal Leukoencephalopathy (PML):
Cases of fatal PML (a brain infection caused by JC virus) have been reported, particularly in patients with prolonged, severe lymphopenia (lymphocyte count < 0.5 × 10⁹/L for > 6 months).
Lymphopenia:
Monitor complete blood count (CBC) before starting, after 6 months, and every 6–12 months thereafter.
Serious Infections:
Monitor for signs of serious infections, including Herpes Zoster (Shingles).
5.Adverse Reactions
Most Common (Incidence ≥10%):
Flushing (redness/warmth of skin), diarrhea, nausea, abdominal pain, and gastroesophageal reflux.
6.Drug Interactions
CYP450 System:
DMF is metabolized by esterases and does not involve the CYP450 system.
Interaction Potential:
No clinically significant drug-drug interactions have been observed.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Dimethyl fumarate.
Available Strength: 120 mg and 240 mg enteric-coated capsules.
Appearance: Hard gelatin capsules containing white to off-white powder.
Storage: Store at 20°C to 25°C (68°F to 77°F).