THERAPEUTICS

Brands

• Tecfidera

Generic?

• No

Class

• Immunomodulator

Commonly Prescribed for

(FDA approved in bold)

• Patients with relapsing forms of multiple sclerosis (MS)

• Psoriasis

How the Drug Works

• The mechanism of action is unclear. The active metabolite, monomethyl fumarate (MMF), can suppress nuclear factor kappa B (NF-κB)-dependent transcription, regulate astrocyte histone deacetylase expression, activate Nrf2 pathway, reduce transendothelial migration of activated leukocytes, and induce detoxification enzymes in astrocytes and microglial cells. All of these play certain roles in anti-inflammation and antioxidation

How Long Until It Works

• It may take several months for the effect to be visible

If It Works

• Continue the drug. Monitor any AEs

If It Doesn't Work

• Switch to other disease-modifying agents

Best Augmenting Combos for Partial Response or Treatment-Resistance

• For acute relapse, corticosteroid has the fastest response

Tests

• Obtain a CBC when initiating treatment, then every 6–12 months

ADVERSE EFFECTS (AEs)

How the Drug Causes AEs

• Serious AEs are related partially to anti-inflammation

Notable AEs

• Flushing (40%), abdominal pain, diarrhea, nausea

• Mildly elevated hepatic transaminases

Life-Threatening or Dangerous AEs

• Anaphylaxis and angioedema

• Progressive multifocal leukoencephalopathy (PML) (one case report)

• Lymphopenia

Weight Gain

• Unusual

Sedation

• Unusual

What to Do About AEs

• Stop the drug if severe AEs develop

Best Augmenting Agents to Reduce AEs

• Flushing may improve by dosing after a meal, especially with fatty foods. Aspirin may improve flushing reaction. AEs generally lower when taken after a meal, especially high-fat meals

DOSING AND USE

Usual Dosage Range

• 240mg twice daily

Dosage Forms

• Capsule, extended release: 120, 240mg

How to Dose

• Start at 120mg twice daily for 7 days

• Maintain at 240mg twice daily after 7 days

Dosing Tips

• Capsule should be swallowed whole

Overdose

• Not well established