Dimethyl fumarate

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Dimethyl fumarate
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Vignesh Ponnusamy, M.B.B.S. [2]

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Overview

Dimethyl fumarate is a methyl ester of fumaric acid that is FDA approved for the treatment of relapsing forms of multiple sclerosis. Common adverse reactions include flushing, abdominal pain, diarrhea, and nausea.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Relapsing forms of Multiple Sclerosis
  • Dosing Information
  • The starting dose for Dimethyl fumarate is 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. Dimethyl fumarate should be swallowed whole and intact. Dimethyl fumarate should not be crushed or chewed and the capsule contents should not be sprinkled on food. Dimethyl fumarate can be taken with or without food. Administration with food may reduce the incidence of flushing.

Off-Label Use and Dosage (Adult)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Dimethyl fumarate in adult patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Dimethyl fumarate in adult patients.

Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

There is limited information regarding FDA-Labeled Use of Dimethyl fumarate in pediatric patients.

Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

There is limited information regarding Off-Label Guideline-Supported Use of Dimethyl fumarate in pediatric patients.

Non–Guideline-Supported Use

There is limited information regarding Off-Label Non–Guideline-Supported Use of Dimethyl fumarate in pediatric patients.

Contraindications

None

Warnings

Precautions

  • Dimethyl fumarate may decrease lymphocyte counts. In the MS placebo controlled trials, mean lymphocyte counts decreased by approximately 30% during the first year of treatment with Dimethyl fumarate and then remained stable. Four weeks after stopping Dimethyl fumarate, mean lymphocyte counts increased but did not return to baseline. Six percent (6%) of TEDFIDERA patients and <1% of placebo patients experienced lymphocyte counts <0.5x109/L (lower limit of normal 0.91x109/L). The incidence of infections (60% vs 58%) and serious infections (2% vs 2%) was similar in patients treated with Dimethyl fumarate or placebo, respectively. There was no increased incidence of serious infections observed in patients with lymphocyte counts <0.8x109/L or 0.5x109/L.
  • Before initiating treatment with Dimethyl fumarate, a recent CBC (i.e., within 6 months) should be available. A CBC is recommended annually, and as clinically indicated. Withholding treatment should be considered in patients with serious infections until the infection(s) is resolved. Dimethyl fumarate has not been studied in patients with pre-existing low lymphocyte counts.
  • Dimethyl fumarate may cause flushing (e.g., warmth, redness, itching, and/or burning sensation). In clinical trials, 40% of Dimethyl fumarate treated patients experienced flushing. Flushing symptoms generally began soon after initiating Dimethyl fumarate and usually improved or resolved over time. In the majority of patients who experienced flushing, it was mild or moderate in severity. Three percent (3%) of patients discontinued Dimethyl fumarate for flushing and <1% had serious flushing symptoms that were not life-threatening but led to hospitalization. Administration of Dimethyl fumarate with food may reduce the incidence of flushing.

Adverse Reactions

Clinical Trials Experience

  • Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice.
  • Adverse Reactions in Placebo-Controlled Trials
  • In the two well-controlled studies demonstrating effectiveness, 1529 patients received Dimethyl fumarate with an overall exposure of 2244 person-years.
  • The adverse reactions presented in the table below are based on safety information from 769 patients treated with Dimethyl fumarate 240 mg twice a day and 771 placebo-treated patients.
This image is provided by the National Library of Medicine.
  • Gastrointestinal
  • Dimethyl fumarate caused GI events (e.g., nausea, vomiting, diarrhea, abdominal pain, and dyspepsia). The incidence of GI events was higher early in the course of treatment (primarily in month 1) and usually decreased over time in patients treated with Dimethyl fumarate compared with placebo. Four percent (4%) of patients treated with Dimethyl fumarate and less than 1% of placebo patients discontinued due to gastrointestinal events. The incidence of serious GI events was 1% in patients treated with Dimethyl fumarate.
  • Hepatic Transaminases
  • An increased incidence of elevations of hepatic transaminases in patients treated with Dimethyl fumarate was seen primarily during the first six months of treatment, and most patients with elevations had levels < 3 times the upper limit of normal (ULN). Elevations of alanine aminotransferase and aspartate aminotransferase to ≥ 3 times the ULN occurred in a small number of patients treated with both Dimethyl fumarate and placebo and were balanced between groups. There were no elevations in transaminases ≥ 3 times the ULN with concomitant elevations in total bilirubin > 2 times the ULN. Discontinuations due to elevated hepatic transaminases were < 1% and were similar in patients treated with Dimethyl fumarate or placebo.
  • Eosinophilia
  • A transient increase in mean eosinophil counts was seen during the first 2 months of therapy.
  • Adverse Reactions in Placebo-Controlled and Uncontrolled Studies
  • In placebo-controlled and uncontrolled clinical studies, a total of 2513 patients have received Dimethyl fumarate and been followed for periods up to 4 years with an overall exposure of 4603 person-years. Approximately 1162 patients have received more than 2 years of treatment with Dimethyl fumarate. The adverse reaction profile of Dimethyl fumarate in the uncontrolled clinical studies was consistent with the experience in the placebo-controlled clinical trials.

Postmarketing Experience

There is limited information regarding Postmarketing Experience of Dimethyl fumarate in the drug label.

Drug Interactions

There is limited information regarding Dimethyl fumarate Drug Interactions in the drug label.

Use in Specific Populations

Pregnancy

Pregnancy Category (FDA):

  • Pregnancy Category C
  • There are no adequate and well-controlled studies in pregnant women. In animals, adverse effects on offspring survival, growth, sexual maturation, and neurobehavioral function were observed when dimethyl fumarate (DMF) was administered during pregnancy and lactation at clinically relevant doses. Dimethyl fumarate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • In rats administered DMF orally (25, 100, 250 mg/kg/day) throughout organogenesis, embryofetal toxicity (reduced fetal body weight and delayed ossification) were observed at the highest dose tested. This dose also produced evidence of maternal toxicity (reduced body weight). Plasma exposure (AUC) for monomethyl fumarate (MMF), the major circulating metabolite, at the no-effect dose is approximately three times that in humans at the recommended human dose (RHD) of 480 mg/day. In rabbits administered DMF orally (25, 75, and 150 mg/kg/day) throughout organogenesis, embryolethality and decreased maternal body weight were observed at the highest dose tested. The plasma AUC for MMF at the no-effect dose is approximately 5 times that in humans at the RHD.
  • Oral administration of DMF (25, 100, and 250 mg/kg/day) to rats throughout organogenesis and lactation resulted in increased lethality, persistent reductions in body weight, delayed sexual maturation (male and female pups) and reduced testicular weight at the highest dose tested. Neurobehavioral impairment was observed at all doses. A no-effect dose for developmental toxicity was not identified. The lowest dose tested was associated with plasma AUC for MMF lower than that in humans at the RHD.
  • Pregnancy Registry
  • There is a pregnancy registry that monitors pregnancy outcomes in women exposed to Dimethyl fumarate during pregnancy. Encourage patients to enroll by calling 1-800-456-2255.


Pregnancy Category (AUS):

  • Australian Drug Evaluation Committee (ADEC) Pregnancy Category

There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Dimethyl fumarate in women who are pregnant.

Labor and Delivery

There is no FDA guidance on use of Dimethyl fumarate during labor and delivery.

Nursing Mothers

  • It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Dimethyl fumarate is administered to a nursing woman.

Pediatric Use

There is no FDA guidance on the use of Dimethyl fumarate with respect to pediatric patients.

Geriatic Use

There is no FDA guidance on the use of Dimethyl fumarate with respect to geriatric patients.

Gender

There is no FDA guidance on the use of Dimethyl fumarate with respect to specific gender populations.

Race

There is no FDA guidance on the use of Dimethyl fumarate with respect to specific racial populations.

Renal Impairment

There is no FDA guidance on the use of Dimethyl fumarate in patients with renal impairment.

Hepatic Impairment

There is no FDA guidance on the use of Dimethyl fumarate in patients with hepatic impairment.

Females of Reproductive Potential and Males

There is no FDA guidance on the use of Dimethyl fumarate in women of reproductive potentials and males.

Immunocompromised Patients

There is no FDA guidance one the use of Dimethyl fumarate in patients who are immunocompromised.

Administration and Monitoring

Administration

  • Oral

Monitoring

There is limited information regarding Monitoring of Dimethyl fumarate in the drug label.

IV Compatibility

There is limited information regarding IV Compatibility of Dimethyl fumarate in the drug label.

Overdosage

There is limited information regarding Chronic Overdose of Dimethyl fumarate in the drug label.

Pharmacology

Chemical structure of Dimethyl fumarate
Dimethyl fumarate
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Not to be confused with Dimethylformamide.

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.

Structure

  • Dimethyl fumarate contains dimethyl fumarate which is also known by its chemical name, dimethyl (E) butenedioate, (C6H8O4). It has the following structure:
This image is provided by the National Library of Medicine.
  • Dimethyl fumarate is a white to off-white powder that is highly soluble in water with a molecular mass of 144.13.
  • Dimethyl fumarate is provided as hard gelatin delayed-release capsules for oral administration, containing 120 mg or 240 mg of dimethyl fumarate consisting of the following inactive ingredients: microcrystalline cellulose, silicified microcrystalline cellulose, croscarmellose sodium, talc, silica colloidal silicon dioxide, magnesium stearate, triethyl citrate, methacrylic acid copolymer - Type A, methacrylic acid copolymer dispersion, simethicone (30% emulsion), sodium lauryl sulphate, and polysorbate 80. The capsule shell, printed with black ink, contains the following inactive ingredients: gelatin, titanium dioxide, FD&C blue 1; brilliant blue FCF, yellow iron oxide and black iron oxide.

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., the upper bound of the 90% confidence interval for the largest placebo-adjusted, baseline-corrected QTc was below 10 ms).

Pharmacokinetics

  • After oral administration of Dimethyl fumarate, dimethyl fumarate undergoes rapid presystemic hydrolysis by esterases and is converted to its active metabolite, monomethyl fumarate (MMF). Dimethyl fumarate is not quantifiable in plasma following oral administration of Dimethyl fumarate. Therefore all pharmacokinetic analyses related to Dimethyl fumarate were performed with plasma MMF concentrations. Pharmacokinetic data were obtained in subjects with multiple sclerosis and healthy volunteers.
  • Absorption
  • The median Tmax of MMF is 2-2.5 hours. The peak plasma concentration (Cmax) and overall exposure (AUC) increased approximately dose proportionally in the dose range studied (120 mg to 360 mg). Following administration of Dimethyl fumarate 240 mg twice a day with food, the mean Cmax of MMF was 1.87 mg/L and AUC was 8.21 mg.hr/L in MS patients.
  • A high-fat, high-calorie meal did not affect the AUC of MMF but decreased its Cmax by 40%. The Tmax was delayed from 2.0 hours to 5.5 hours. In this study, the incidence of flushing was reduced by approximately 25% in the fed state.
  • Distribution
  • The apparent volume of distribution of MMF varies between 53 and 73 L in healthy subjects. Human plasma protein binding of MMF is 27-45% and independent of concentration.
  • Metabolism
  • In humans, dimethyl fumarate is extensively metabolized by esterases, which are ubiquitous in the gastrointestinal tract, blood, and tissues, before it reaches the systemic circulation. Further metabolism of MMF occurs through the tricarboxylic acid (TCA) cycle, with no involvement of the cytochrome P450 (CYP) system. MMF, fumaric and citric acid, and glucose are the major metabolites in plasma.
  • Elimination
  • Exhalation of CO2 is the primary route of elimination, accounting for approximately 60% of the Dimethyl fumarate dose. Renal and fecal elimination are minor routes of elimination, accounting for 16% and 1% of the dose respectively. Trace amounts of unchanged MMF were present in urine.
  • The terminal half-life of MMF is approximately 1 hour and no circulating MMF is present at 24 hours in the majority of individuals. Accumulation of MMF does not occur with multiple doses of Dimethyl fumarate.
  • Specific Populations
  • Body weight, gender, and age do not require dosage adjustment.
  • No studies have been conducted in subjects with hepatic or renal impairment. However, neither condition would be expected to affect exposure to MMF and therefore no dosage adjustment is necessary.
  • Drug Interaction Studies
  • No potential drug interactions with dimethyl fumarate or MMF were identified in in vitro CYP inhibition and induction studies, or in P-glycoprotein studies. Single doses of interferon beta-1a or glatiramer acetate did not alter the pharmacokinetics of MMF. Aspirin, when administered approximately 30 minutes before Dimethyl fumarate, did not alter the pharmacokinetics of MMF.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility
  • Carcinogenesis
  • Carcinogenicity studies of dimethyl fumarate (DMF) were conducted in mice and rats. In mice, oral administration of DMF (25, 75, 200, and 400 mg/kg/day) for up to two years resulted in an increase in nonglandular stomach (forestomach) and kidney tumors: squamous cell carcinomas and papillomas of the forestomach in males and females at 200 and 400 mg/kg/day; leiomyosarcomas of the forestomach at 400 mg/kg/day in males and females; renal tubular adenomas and carcinomas at 200 and 400 mg/kg/day in males; and renal tubule adenomas at 400 mg/kg/day in females. Plasma MMF exposure (AUC) at the highest dose not associated with tumors in mice (75 mg/kg/day) was similar to that in humans at the recommended human dose (RHD) of 480 mg/day.
  • In rats, oral administration of DMF (25, 50, 100, and 150 mg/kg/day) for up to two years resulted in increases in squamous cell carcinomas and papillomas of the forestomach at all doses tested in males and females, and in testicular interstitial (Leydig) cell adenomas at 100 and 150 mg/kg/day. Plasma MMF AUC at the lowest dose tested was lower than that in humans at the RHD.
  • Mutagenesis
  • Dimethyl fumarate (DMF) and monomethyl fumarate (MMF) were not mutagenic in the in vitro bacterial reverse mutation (Ames) assay. DMF and MMF were clastogenic in the in vitro chromosomal aberration assay in human peripheral blood lymphocytes in the absence of metabolic activation. DMF was not clastogenic in the in vivo micronucleus assay in the rat.
  • Impairment of Fertility
  • In male rats, oral administration of DMF (75, 250, and 375 mg/kg/day) prior to and throughout the mating period had no effect on fertility; however, increases in non-motile sperm were observed at the mid and high doses. The no-effect dose for adverse effects on sperm is similar to the recommended human dose (RHD) of 480 mg/day on a body surface area (mg/m2) basis.
  • In female rats, oral administration of DMF (20, 100, and 250 mg/kg/day) prior to and during mating and continuing to gestation day 7 caused disruption of the estrous cycle and increases in embryolethality at the highest dose tested. The highest dose not associated with adverse effects (100 mg/kg/day) is twice the RHD on a mg/m2 basis.
  • Testicular toxicity (germinal epithelial degeneration, atrophy, hypospermia, and/or hyperplasia) was observed at clinically relevant doses in mice, rats, and dogs in subchronic and chronic oral toxicity studies of DMF, and in a chronic oral toxicity study evaluating a combination of four fumaric acid esters (including DMF) in rats.
  • Animal Toxicology and/or Pharmacology
  • Kidney toxicity was observed after repeated oral administration of dimethyl fumarate (DMF) in mice, rats, dogs, and monkeys. Renal tubule epithelia regeneration, suggestive of tubule epithelial injury, was observed in all species. Renal tubular hyperplasia was observed in rats with dosing for up to two years. Cortical atrophy and interstitial fibrosis were observed in dogs and monkeys at doses above 5 mg/kg/day. In monkeys, the highest dose tested (75 mg/kg/day) was associated with single cell necrosis and multifocal and diffuse interstitial fibrosis, indicating irreversible loss of renal tissue and function. In dogs and monkeys, the 5-mg/kg/day dose was associated with plasma MMF exposures less than or similar to that in humans at the recommended human dose (RHD).
  • A dose-related increase in incidence and severity of retinal degeneration was observed in mice following oral administration of DMF for up to two years at doses above 75 mg/kg/day, a dose associated with plasma MMF exposure (AUC) similar to that in humans at the RHD.

Clinical Studies

  • The efficacy and safety of Dimethyl fumarate were demonstrated in two studies (Studies 1 and 2) that evaluated Dimethyl fumarate taken either twice or three times a day in patients with relapsing-remitting multiple sclerosis (RRMS). The starting dose for Dimethyl fumarate was 120 mg twice or three times a day for the first 7 days, followed by an increase to 240 mg twice or three times a day. Both studies included patients who had experienced at least 1 relapse over the year preceding the trial or had a brain Magnetic Resonance Imaging (MRI) scan demonstrating at least one gadolinium-enhancing (Gd+) lesion within 6 weeks of randomization. The Expanded Disability Status Scale (EDSS) was also assessed and patients could have scores ranging from 0 to 5. Neurological evaluations were performed at baseline, every 3 months, and at the time of suspected relapse. MRI evaluations were performed at baseline, month 6, and year 1 and 2 in a subset of patients (44% in Study 1 and 48% in Study 2).
  • Study 1: Placebo-Controlled Trial in RRMS
  • Study 1 was a 2-year randomized, double-blind, placebo-controlled study in 1234 patients with RRMS. The primary endpoint was the proportion of patients relapsed at 2 years. Additional endpoints at 2 years included the number of new or newly enlarging T2 hyperintense lesions, number of new T1 hypointense lesions, number of Gd+ lesions, annualized relapse rate (ARR), and time to confirmed disability progression. Confirmed disability progression was defined as at least a 1 point increase from baseline EDSS (1.5 point increase for patients with baseline EDSS of 0) sustained for 12 weeks.
  • Patients were randomized to receive Dimethyl fumarate 240 mg twice a day (n=410), Dimethyl fumarate 240 mg three times a day (n=416), or placebo (n=408) for up to 2 years. The median age was 39 years, median time since diagnosis was 4 years, and median EDSS score at baseline was 2. The median time on study drug for all treatment arms was 96 weeks. The percentages of patients who completed 96 weeks on study drug per treatment group were 69% for patients assigned to Dimethyl fumarate 240 mg twice a day, 69% for patients assigned to Dimethyl fumarate 240 mg three times a day and 65% for patients assigned to placebo groups.
  • Dimethyl fumarate had a statistically significant effect on all of the endpoints described above and the 240 mg three times daily dose showed no additional benefit over the Dimethyl fumarate 240 mg twice daily dose. The results for this study (240 mg twice a day vs. placebo) are shown in Table 2 and Figure 1.
This image is provided by the National Library of Medicine.
This image is provided by the National Library of Medicine.
  • Study 2: Placebo-Controlled Trial in RRMS
  • Study 2 was a 2-year multicenter, randomized, double-blind, placebo-controlled study that also included an open-label comparator arm in patients with RRMS. The primary endpoint was the annualized relapse rate at 2 years. Additional endpoints at 2 years included the number of new or newly enlarging T2 hyperintense lesions, number of T1 hypointense lesions, number of Gd+ lesions, proportion of patients relapsed, and time to confirmed disability progression as defined in Study 1.
  • Patients were randomized to receive Dimethyl fumarate 240 mg twice a day (n=359), Dimethyl fumarate 240 mg three times a day (n=345), an open-label comparator (n=350), or placebo (n=363) for up to 2 years. The median age was 37 years, median time since diagnosis was 3 years, and median EDSS score at baseline was 2.5. The median time on study drug for all treatment arms was 96 weeks. The percentages of patients who completed 96 weeks on study drug per treatment group were 72% for patients assigned to Dimethyl fumarate 240 mg twice a day, 70% for patients assigned to Dimethyl fumarate 240 mg three times a day and 64% for patients assigned to placebo groups.
  • Dimethyl fumarate had a statistically significant effect on the relapse and MRI endpoints described above. There was no statistically significant effect on disability progression. The Dimethyl fumarate 240 mg three times daily dose resulted in no additional benefit over the Dimethyl fumarate 240 mg twice daily dose. The results for this study (240 mg twice a day vs. placebo) are shown in Table 3.
This image is provided by the National Library of Medicine.

How Supplied

  • Dimethyl fumarate is available as hard gelatin delayed-release capsules in two strengths containing either 120 mg or 240 mg of dimethyl fumarate. The green and white 120 mg capsules are printed with “BG-12 120 mg” in black ink. The green 240 mg capsules are printed with “BG-12 240 mg” in black ink. Dimethyl fumarate is available as follows:
  • 30-day Starter Pack, (NDC 64406-007-03):
  • 7-day bottle 120 mg capsules, quantity 14
  • 23-day bottle 240 mg capsules, quantity 46
  • 120 mg capsules:
  • 7-day bottle of 14 capsules (NDC 64406-005-01)
  • 240 mg capsules:
  • 30-day bottle of 60 capsules (NDC 64406-006-02)
  • Store at 15°C – 30°C (59-86°F). Protect the capsules from light. Store in original container. Once opened, discard bottles of Dimethyl fumarate after 90 days.

Storage

There is limited information regarding Dimethyl fumarate Storage in the drug label.

Images

Drug Images

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Patient Counseling Information

  • Dosage
  • Inform patients that they will be provided two strengths of Dimethyl fumarate when starting treatment: 120 mg capsules for the 7 day starter dose and 240 mg capsules for the maintenance dose, both to be taken twice daily. Inform patients to swallow Dimethyl fumarate capsules whole and intact. Inform patients to not crush, chew, or sprinkle capsule contents on food. Inform patients that Dimethyl fumarate can be taken with or without food.
  • Flushing and Gastrointestinal (GI) Reactions
  • Flushing and GI reactions (abdominal pain, diarrhea, and nausea) are the most common reactions, especially at the initiation of therapy, and may decrease over time. Advise patients to contact their healthcare provider if they experience persistent and/or severe flushing or GI reactions, as taking Dimethyl fumarate with food may help.
  • Pregnancy and Pregnancy Registry
  • Instruct patients that if they are pregnant or plan to become pregnant while taking Dimethyl fumarate they should inform their physician.
  • Encourage patients to enroll in the Dimethyl fumarate Pregnancy Registry if they become pregnant while taking Dimethyl fumarate. Advise patients to call 1-800-456-2255 for more information.
  • Lymphocyte Counts
  • Inform patients that Dimethyl fumarate may decrease lymphocyte counts. A recent blood test (i.e., within 6 months) should be available before they start therapy to identify patients with pre-existing low lymphocyte counts. Blood tests are also recommended annually and as clinically indicated.
Patient Information
Dimethyl fumarate™ (tek" fi de' rah)
(dimethyl fumarate) delayed-release capsules
What is Dimethyl fumarate?
  • Dimethyl fumarate is a prescription medicine used to treat people with relapsing forms of multiple sclerosis (MS)
  • It is not known if Dimethyl fumarate is safe and effective in children under 18 years of age
  • Before taking and while you take Dimethyl fumarate, tell your doctor if you have or have had:
  • low white blood cell counts or an infection
  • any other medical conditions
  • Tell your doctor if you are:
  • pregnant or plan to become pregnant. It is not known if Dimethyl fumarate will harm your unborn baby.
  • If you become pregnant while taking Dimethyl fumarate, talk to your doctor about enrolling in the Dimethyl fumarate Pregnancy Registry. You can enroll in this registry by calling 1-800-456-2255. The purpose of this registry is to monitor the health of you and your baby.
  • breastfeeding or plan to breastfeed. It is not known if Dimethyl fumarate passes into your breast milk. You and your doctor should decide if you will take Dimethyl fumarate or breastfeed.
  • taking prescription or over-the-counter medicines, vitamins, or herbal supplements
How should I take Dimethyl fumarate?
  • Take Dimethyl fumarate exactly as your doctor tells you to take it
  • The recommended starting dose is one 120 mg capsule taken by mouth 2 times a day for 7 days
  • The recommended dose after 7 days is one 240 mg capsule taken by mouth 2 times a day
  • Dimethyl fumarate can be taken with or without food
  • Swallow Dimethyl fumarate whole. Do not crush, chew, or sprinkle capsule contents on food.
  • Protect Dimethyl fumarate from light. You can do this by storing the capsules in their original container. Throw away opened Dimethyl fumarate after 90 days.
What are the possible side effects of Dimethyl fumarate?
  • Dimethyl fumarate may cause serious side effects including:
  • decreases in your white blood cell count
  • The most common side effects of Dimethyl fumarate include:
  • Flushing and stomach problems are the most common reactions, especially at the start of therapy, and may decrease over time. Call your doctor if you have any of these symptoms and they bother you or do not go away.
  • These are not all the possible side effects of Dimethyl fumarate. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088. For more information go to dailymed.nlm.nih.gov.
General Information about the safe and effective use of Dimethyl fumarate
  • Medicines are sometimes prescribed for purposes other than those listed in this Patient Information. Do not use Dimethyl fumarate for a condition for which it was not prescribed. Do not give Dimethyl fumarate to other people, even if they have the same symptoms that you have. It may harm them.
  • If you would like more information, talk to your doctor or pharmacist. You can ask your doctor or pharmacist for information about Dimethyl fumarate that is written for healthcare professionals.
What are the ingredients in Dimethyl fumarate?
  • Active ingredient: dimethyl fumarate
  • Inactive ingredients: microcrystalline cellulose, silicified microcrystalline cellulose, croscarmellose sodium, talc, silica colloidal silicon dioxide, magnesium stearate, triethyl citrate, methacrylic acid copolymer - Type A, methacrylic acid copolymer dispersion, simethicone (30% emulsion), sodium lauryl sulphate, and polysorbate 80. Capsule Shell: gelatin, titanium dioxide, FD&C blue 1; brilliant blue FCF, yellow iron oxide and black iron oxide.

Precautions with Alcohol

  • Alcohol-Dimethyl fumarate interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

Look-Alike Drug Names

There is limited information regarding Dimethyl fumarate Look-Alike Drug Names in the drug label.

Drug Shortage Status

Price

References

The contents of this FDA label are provided by the National Library of Medicine.

  1. ↑ "TECFIDERA (dimethyl fumarate) kit Dimethyl fumarate (dimethyl fumarate) capsule [Biogen Idec Inc.]".

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