Tecfidera (dimethyl fumarate) for multiple sclerosis
Fact-checked by
What is Tecfidera used for?
Tecfidera (dimethyl fumarate) is an approved oral treatment for multiple sclerosis (MS) that helps to reduce relapse rates, delay disability progression, and slow the development of brain lesions.
The brand-name medication was originally developed and marketed by Biogen. Several generic forms of the therapy are now available in the U.S., including those produced by Cipla, Glenmark Pharmaceuticals, Lupin, Mylan, and Zydus Lifesciences (formerly Zydus Cadila).
Therapy Snapshot
| Brand Name: | Tecfidera |
| Chemical Name: | Dimethyl fumarate |
| Usage: | Disease-modifying therapy for relapsing forms of MS |
| Administration: | Delayed-release capsules |
How does Tecfidera work for MS?
MS is caused by an abnormal inflammatory attack that the immune system launches against healthy parts of the brain and spinal cord. Tecfidera contains an inactive molecule called dimethyl fumarate (DMF). Once inside the body, this molecule is converted into its active form called monomethyl fumarate (MMF).
It’s not entirely clear how MMF works in MS patients, but the therapy is generally believed to reduce MS-driving inflammation by changing the activity of immune cells. It also has antioxidant properties that may protect nerve cells against damage.
MMF also is the active agent in Vumerity (diroximel fumarate), a newer MS treatment by Biogen approved in the U.S. in 2019. Vumerity was designed to deliver a similar amount of MMF as Tecfidera, but with fewer of the gastrointestinal side effects that occur with the older medication.
Who can take Tecfidera?
The U.S. Food and Drug Administration (FDA) approved Tecfidera in 2013 for adults with relapsing forms of MS — which include clinically isolated syndrome (CIS), relapsing-remitting MS (RRMS), and active secondary progressive MS (SPMS).
According to Biogen, Tecfidera is currently approved in 69 countries as an MS therapy and has been used to treat more than 530,000 patients. Notably, however, in certain countries, such as Canada and Australia, and in the European Union, the medication is solely approved to treat RRMS.
Who should not take Tecfidera?
Tecfidera should not be taken by people with a known allergy to the medication or any of its ingredients.
How is Tecfidera administered?
Tecfidera is available as delayed-release capsules that come in two strengths:
- 120 mg capsules, with a green cap and a white body, printed with “BG12 120 mg” in black ink
- 240 mg capsules, with a green cap and body, printed with “BG-12 240 mg” in black ink
The recommended dose of Tecfidera is 240 mg twice a day, but patients should take the 120 mg capsules twice daily over the first week of treatment. The capsules must be swallowed whole and intact (not crushed, chewed, or sprinkled over food).
Tecfidera may be taken with or without food. Taking it with food or with aspirin may reduce the incidence of flushing, or reddening of the skin, a potential side effect.
| Administration | Oral via delayed-release capsules |
| Dosage | 240 mg (120 mg twice daily for first week) |
| Timing | Twice a day |
Tecfidera in clinical trials
Approvals of Tecfidera were supported mainly by data from two large Phase 3 clinical trials — DEFINE (NCT00420212) and CONFIRM (NCT00451451). Each study enrolled more than 1,200 people with RRMS, and participants were randomly selected to receive Tecfidera (240 mg, two or three times per day) or a placebo for about two years. In CONFIRM, one patient group also was randomly assigned to glatiramer acetate, an approved MS treatment sold as Copaxone, among other names.
In both studies, significantly fewer participants given twice-daily Tecfidera experienced relapses, compared with those on a placebo: 27% vs. 46% in DEFINE, and 29% vs. 41% in CONFIRM. The average annual relapse rate was significantly lower with Tecfidera, by approximately 50% in both studies. For comparison, glatiramer acetate lowered the annual relapse rate by 29% compared with a placebo.
Treatment with Tecfidera also significantly decreased brain lesions visible on MRI scans.
In DEFINE, significantly fewer patients given Tecfidera experienced a confirmed worsening in disability over the two years (16% vs. 27%) than those on placebo. The proportion of patients with worsening disability was not significantly different in CONFIRM.
ENDORSE trial
Participants who completed these studies could enroll in a Phase 3 extension trial, called ENDORSE (NCT00835770), in which all were treated with Tecfidera at 240 mg, either two or three times daily. Treatment was due to continue for at least eight years to evaluate Tecfidera’s long-term effects.
Results from ENDORSE, with a total of 13 years of follow-up, showed that the relapse rate remained low with continued treatment. After about a decade in the extension trial, the average annual relapse rate was 0.11 relapses per year, and about three-quarters of patients had no confirmed disability progression.
FOCUS and CONNECTED trials
A Phase 2 study called FOCUS (NCT02410200) investigated six months of Tecfidera use in children and adolescents, ages 10 to 17, with RRMS. Patients could then enroll in an extension study, called CONNECTED (NCT02555215), and continue with Tecfidera treatment for an additional two years.
Over the 2.5 years of treatment, results from FOCUS and CONNECTED showed that patients had, on average, 0.2 relapses per year. That represented an 84.5% decrease from before starting on Tecfidera. Most patients showed no signs of disability progression.
Of note, Tecfidera is currently not approved for use in children and adolescents under 18 years of age.
Ongoing trials
A pair of ongoing Phase 3 trials are investigating Tecfidera in children and adolescents with RRMS, ages 10 to 17. In both studies, treatment will last for 96 weeks, or about two years.
The CONNECT trial (NCT02283853) is testing Tecfidera against Avonex (interferon beta-1a), an injectable MS medication approved only for adults, in 156 patients. In a first part, researchers will determine if Tecfidera slows the development of brain lesions over two years. Children and adolescents who complete this part will then be followed for up to seven years to determine the medication’s long-term safety and efficacy.
The second, larger trial (NCT03870763) is set to evaluate both Tecfidera and the MS injectable medication Plegridy (peginterferon beta-1a) — which also is not approved for use in children. In this study, involving 260 participants, the two therapies will be tested against a placebo. The main goal is to determine if either MS therapy extends the time to a first relapse. Changes in relapse rates and brain lesions will be examined as secondary measures, along with any other side effects.
Common side effects of Tecfidera
The most common side effects associated with Tecfidera use are:
- flushing
- abdominal pain
- diarrhea
- nausea
Liver problems and decreases in white blood cell count
Tecfidera may result in liver injury or a substantial decrease in the number of immune cells in the blood. Liver health and blood cell counts should be monitored before starting on Tecfidera and regularly during treatment. The therapy may be discontinued if persistent low immune counts or liver injury occurs.
Infections
Treatment with Tecfidera may increase the risk of certain viral infections, such as serious cases of shingles (herpes zoster). If such an infection develops, the medication may be withheld until the infection resolves.
PML
Progressive multifocal leukoencephalopathy (PML), a serious brain infection caused by the John Cunningham virus, also may occur with Tecfidera treatment. The medication should be stopped immediately if patients show signs of PML.
Allergic reactions
Some people experience an allergic or swelling reaction to Tecfidera. The treatment should be discontinued if such a reaction occurs, and patients should seek immediate medical care.
Pregnancy and breastfeeding
There are no well-controlled studies of Tecfidera use during pregnancy in people. However, animal data suggest that using the medication could harm a developing fetus. Patients should talk with their healthcare professionals, and only continue Tecfidera during pregnancy if the potential benefit justifies the potential fetal risks. Those who become pregnant while on Tecfidera may enroll in a pregnancy registry (NCT01911767), sponsored by Biogen, that is monitoring outcomes in pregnancies with Tecfidera exposure.
While Tecfidera has been found in breast milk, it remains unknown if the medication increases the risk of side effects in infants. According to Tecfidera’s label, the medication should not be used during breastfeeding; patients should discuss with their healthcare provider whether to take Tecfidera or to breastfeed.
Multiple Sclerosis News Today is strictly a news and information website about the disease. It does not provide medical advice, diagnosis, or treatment. This content is not intended to be a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition. Never disregard professional medical advice or delay in seeking it because of something you have read on this website.
FAQs about Tecfidera
In the U.S., Tecfidera was approved in March 2013 for treating adults with relapsing forms of MS. Approved indications include clinically isolated syndrome, relapsing-remitting MS, and active secondary progressive MS. Since 2020, when the patent on Tecfidera’s active ingredient expired, more than a dozen Tecfidera generics have been cleared by the U.S. Food and Drug Administration.
Based on animal studies, Tecfidera use during pregnancy can cause harm to a developing fetus. But a large registry study conducted by Biogen, the therapy’s developer, to monitor outcomes in pregnancies exposed to Tecfidera, suggests that taking the medication just before conception or at any time during pregnancy is not associated with worse pregnancy outcomes. Nonetheless, patients on Tecfidera who become or plan to become pregnant should discuss this topic with their healthcare team.
Alcohol may potentially interfere with Tecfidera, especially if consumed within one hour of taking the medication. Drinking alcohol also can potentially exacerbate some side effects associated with the medication, including nausea, flushing, and diarrhea. Patients on Tecfidera should discuss safe alcohol use with their healthcare provider, who can make the best recommendation based on their medical history.
As each person can respond differently to a medication, there is no standard timeline for when Tecfidera starts to work. In the trials that supported Tecfidera’s approval, a significant reduction in relapse rates in Tecfidera-treated patients could be observed within the first 12 weeks (about three months) of treatment. But patients are advised to talk with their healthcare team on how Tecfidera can help in their particular case.
Weight gain and hair loss were not reported in clinical trials as side effects of Tecfidera, but some people who received the medication after its approval have experienced hair loss, according to post-marketing reports. Patients should talk with their healthcare team if such events occur.
Related Articles
