II. Background
- Generic in 2020
III. Indications
- Multiple Sclerosis (relapsing)
IV. Mechanism
- Dimethyl Fumarate key effects
- Immunosuppressant that decreases CD8 T Cells as well as Cytokine production
- Dimethyl Fumarate effects are neuroprotective and immunomodulating
- Dimethyl Fumarate is orally Bioavailable
- Converted in vivo to active metabolite monomethyl fumarate (MMF)
- Monomethyl fumarate (MMF)
- MMF binds and activates nuclear factor erythroid 2 (NF-E2) and nuclear related factor 2 (Nrf2)
- Nuclear related factor 2 (Nrf2)
- Nrf2 on activation, translocates to the nucleus and binds antioxidant response element (ARE)
- Triggers a cascade of expression of cytoprotective genes
V. Medications
- Dimethyl Fumarate (Tecfidera) Delayed-release capsules: 120 mg and 240 mg
VI. Dosing: Adults
- Start: 120 mg orally twice daily for 7 days
- Maintenance: 240 mg orally twice daily
- If not tolerated, may decrease dose to 120 mg orally twice daily for 4 weeks, then retrial higher dose
VII. Adverse Effects
- Serious
- Anaphylaxis or Angioedema
- Progressive Multifocal Leukoencephalopathy (PML)
- Opportunistic infections (e.g. Herpes Zoster)
- Gastrointestinal
- Hematologic
- Lymphopenia
- Hepatotoxicity
- Elevated liver transaminases
- Cardiovascular
VIII. Safety
- Unknown safety in pregnancy
- Toxicity demonstrated in animals
- Unknown safety in Lactation
- Monitoring
- Complete Blood Count (at baseline and every 6 months)
- Liver Function Tests (at baseline and periodically)
- MRI Brain (for signs of PML)
- Consider yearly testing for JCV Antibodies
IX. Efficacy
- Compared with other oral agents for MS
- Better tolerated than Fingolimod
- May be more effective than Teriflunomide
X. Resources
- Dimethyl Fumarate (DailyMed)
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Related Studies
| dimethyl fumarate (on 11/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing) | ||
| DIMETHYL FUMARATE DR 240 MG CP | Generic | $2.40 each |