Dimethyl fumarate
TECFIDERA
What it isNrf2-activating immunomodulator; relapsing multiple sclerosis.
Why this oneIt is more GI-irritating than diroximel fumarate despite producing the same active metabolite.
What limits itMonitor lymphocytes because persistent lymphopenia raises PML risk. Flushing and GI upset are common.
FDA-approved for
- relapsing multiple sclerosis (2013)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Relapsing forms of multiple sclerosis | Adult | 120 mg BID x7d | 240 mg BID | 240 mg BID |
Titration After 7 days at starting dose, increase to maintenance.
Renal Undefined
Hepatic Undefined
Instructions
- Swallow capsules whole; do not crush, chew, or sprinkle on food
- Take with or without food; taking with food or non-enteric aspirin 325 mg 30 min prior may reduce flushing
- Temporary reduction to 120 mg BID if maintenance not tolerated; resume 240 mg BID within 4 weeks or consider discontinuation
- Obtain CBC with lymphocyte count and LFTs (aminotransferases, ALP, bilirubin) before initiation
Cautions
- Anaphylaxis and angioedema — discontinue and do not restart
- Progressive multifocal leukoencephalopathy (PML) — withhold at first sign
- Herpes zoster and other serious opportunistic infections
- Lymphopenia — monitor CBC/lymphocytes, interrupt if <0.5x10^9/L >6 mo
- Liver injury — monitor LFTs
- Flushing
- Serious GI reactions (perforation, ulceration, hemorrhage, obstruction)
Adverse reactions
- Flushing
- Abdominal pain
- Diarrhea
- Nausea
- Vomiting
- Pruritus
- Rash
Pregnancy Registry/observational data have not shown increased birth-defect or miscarriage risk; animal harm at high doses.
Lactation No data on presence in human milk; effects on infant/milk unknown.
NO BOXED WARNINGS
Principal riskLymphopenia raising PML risk
Cost, est. cash$300–$2,500/month
Generic entry2020
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.
Mechanism of action: Dimethyl fumarate ballicule
