Overview
11 DESCRIPTION Dimethyl fumarate delayed-release capsule contains dimethyl fumarate which is also known by its chemical name, dimethyl (E) butenedioate, (C 6 H 8 O 4 ). It has the following structure: Dimethyl fumarate is a white to off-white powder that is freely soluble in dichloromethane and very slightly soluble in water with a molecular mass of 144.13.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action The mechanism by which dimethyl fumarate (DMF) exerts its therapeutic effect in multiple sclerosis is unknown. DMF and the metabolite, monomethyl fumarate (MMF), have been shown to activate the Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) pathway in vitro and in vivo in animals and humans. The Nrf2 pathway is involved in the cellular response to oxidative stress. MMF has been identified as a nicotinic acid receptor agonist in vitro . 12.2 Pharmacodynamics Potential to prolong the QT interval In a placebo controlled thorough QT study performed in healthy subjects, there was no evidence that dimethyl fumarate caused QT interval prolongation of clinical significance (i.e.
Indications
- 1 INDICATIONS AND USAGE Dimethyl fumarate delayed-release capsules are indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. Dimethyl fumarate is indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults ( 1 )
Common Doses
- 120 mg
- 240 mg
- 325 mg
Dosage
2 DOSAGE AND ADMINISTRATION Starting dose: 120 mg twice a day, orally, for 7 days ( 2.1 ) Maintenance dose after 7 days: 240 mg twice a day, orally ( 2.1 ) Swallow dimethyl fumarate delayed-release capsules whole and intact. Do not crush, chew, or sprinkle capsule contents on food ( 2.1 ) Take dimethyl fumarate delayed-release capsule with or without food ( 2.1 ) 2.1 Dosing Information The starting dose for dimethyl fumarate delayed-release capsules are 120 mg twice a day orally. After 7 days, the dose should be increased to the maintenance dose of 240 mg twice a day orally.
Contraindications
- 4 CONTRAINDICATIONS Dimethyl fumarate is contraindicated in patients with known hypersensitivity to dimethyl fumarate or to any of the excipients of dimethyl fumarate. Reactions have included anaphylaxis and angioedema [see Warnings and Precautions (5.1) ]. Known hypersensitivity to dimethyl fumarate or any of the excipients of dimethyl fumarate. ( 4 )
Side Effects
- 6 ADVERSE REACTIONS The following important adverse reactions are described elsewhere in labeling: Anaphylaxis and Angioedema [see Warnings and Precautions (5.1) ]. Progressive multifocal leukoencephalopathy [see Warnings and Precautions (5.2) ]. Herpes Zoster and Other Serious Opportunistic Infections [ see Warnings and Precautions (5.3) ]. Lymphopenia [ see Warnings and Precautions (5.4) ]. Liver Injury [ see Warnings and Precautions (5.5) ]. Flushing [ see Warnings and Precautions (5.6) ].
Interactions
- No major interactions listed on the FDA label. Always consult a healthcare professional.