What is Tecfidera (dimethyl fumarate)?
Tecfidera is a brand name for dimethyl fumarate and is used to treat relapsing forms of multiple sclerosis (MS). It is available as delayed-release capsules in strengths of 120 mg 240 mg, which are taken orally.
Tecfidera is classed as a disease-modifying therapy (DMT) for MS. This means that, although it is not a cure, it can reduce the number of relapses a person has and slow down the progression of the disease.
Although it is not entirely understood how Tecfidera works, research suggests it may both:
- Reduce inflammation caused by the immune system attacking myelin, limiting the damage caused
- Protect nerve cells from damage caused by chemicals released during the immune attack
You can read more about how Tecfidera is believed to work in question 3.
What is Tecfidera (dimethyl fumarate) used for?
Tecfidera is used to treat relapsing forms of multiple sclerosis. In all cases, the recommended regimen consists of 240 mg capsules taken twice per day, meaning a total daily dosage of 480 mg. There is a one-week ‘titration’ period at the start of treatment, during which time the regimen consists of 120 mg capsules taken twice per day, meaning a total daily dosage of 240 mg.
The relapsing forms of MS that Tecfidera is approved to treat are:
Clinically isolated syndrome
Clinically isolated syndrome (CIS) refers to a single episode of neurological symptoms that lasts at least 24 hours. Because CIS is a single episode of symptoms, it is sometimes considered to be a different condition from MS; others consider it to be the earliest form of relapsing-remitting MS (RRMS).
Regardless, the purpose of Tecfidera therapy is to prevent or slow down the progression to RRMS.
Relapsing-remitting disease
Whereas a single episode of neurological symptoms is called clinically isolated syndrome, the second episode of symptoms means the condition has progressed to relapsing-remitting MS or relapsing-remitting disease.
Nonetheless, the purpose of Tecfidera therapy in people living with RRMS is to slow down disease progression and reduce the number of relapses.
Active secondary progressive disease
Secondary progressive MS (SPMS) or secondary progressive disease is characterized by a steady worsening of symptoms rather than distinct relapses (although relapses can also occur). SPMS is considered ‘active’ when either relapses occur or there is MRI evidence of new legions.
As is the case with CIS and RRMS, Tecfidera therapy is intended to slow down disease progression.
How does Tecfidera (dimethyl fumarate) work?
Tecfidera is believed to:
- Reduce inflammation caused by the immune system attacking myelin, limiting the damage caused
- Protect nerve cells from damage caused by chemicals released during the immune attack
Although the exact way in which it works is not completely understood, there is evidence that it is linked to what is called the Nrf2 pathway. Both the active ingredient of Tecfidera, dimethyl fumarate, and its main metabolite (substances released once your body metabolizes or ‘breaks down’ the drug), monomethyl fumarate, have been found to activate the Nrf2 pathway.
The Nrf2 pathway is involved in the cellular response to oxidative stress (the imbalance of free radicals and antioxidants in your body). Activation of the Nrf2 pathway may trigger the release of antioxidants that help regulate the immune system’s inflammatory response that mistakenly attacks myelin and causes the symptoms associated with MS.
However, research has also been performed that suggests Tecfidera might have a different mechanism of action, possibly independent of the Nrf2 pathway entirely.
For example, a study published in 2016 found that Tecfidera acts upon around 50 different proteins, including those involved in the activation of immune T-cells (including those linked to MS). Preventing the production of such T-cells could be what makes Tecfidera effective.
Learning more about the mechanism of action of Tecfidera and other MS treatments is of key importance to researchers. Not only can it help develop new drugs with greater efficacy, it can help develop drugs with fewer or less serious side effects.
What are the side effects of Tecfidera (dimethyl fumarate)?
Common side effects
Common side effects include:
- Flushing and feeling hot
- Gastrointestinal problems such as nausea, stomach pains, vomiting, diarrhea, and indigestion
These symptoms are more likely to occur at the start of your treatment and often ease off as your body adjusts. If these symptoms are severe, you should contact your doctor immediately. If the symptoms are not severe but are bothersome, you should speak to your healthcare provider or pharmacist about ways of dealing with them. This may include taking over-the-counter medicines such as aspirin (for flushing) or antacids (for gastrointestinal symptoms).
Less common side effects
Less common side effects include:
Like flushing, these symptoms are more likely to occur at the beginning of your treatment and often ease off as your body adjusts.
Less common side effects that are more serious include:
- Decreases in your white blood cell count (your healthcare provider should test this before and throughout your treatment)
- Liver problems, signs of which include severe tiredness, loss of appetite, pain on the right side of your stomach, dark or brown urine, and yellowing of your skin or white of your eyes
You should speak to your doctor immediately if you experience any symptoms of liver problems.
Other serious side effects of Tecfidera include:
- Progressive multifocal leukoencephalopathy (PML), a rare viral infection of the brain that usually leads to death or severe disability
- Herpes zoster (shingles) and other serious opportunistic infections
Although these side effects are uncommon, you should discuss the risks associated with Tecfidera with your healthcare provider.
Serious allergic reaction
Although serious allergic reactions to Tecfidera are rare, they can occur. Signs of a serious allergic reaction should be treated as a medical emergency. They include:
- Skin rash – for example itchy, red, or swollen skin
- Wheezing
- Tightness in the chest or throat
- Trouble breathing or talking
- Swollen mouth, face, lips, tongue, or throat
This is not a complete list of the possible side effects of Tecfidera. It is important to speak to your healthcare professional to gain information about the risk of side effects and steps you can take to help prevent or control them.
Why does Tecfidera (dimethyl fumarate) cause flushing and how long does it last?
It is believed that Tecfidera (and other medications containing dimethyl fumarate) cause flushing by activating a receptor called hydroxycarboxylic acid receptor 2 (HCA₂, also known as niacin receptor 1 (NIACR1) and GPR109A) in the cells of the epidermis (outer layer of skin).
This is the same mechanism of action as niacin-induced flushing, which is a common side effect of high-dose niacin (vitamin B3) supplements often used to treat high cholesterol.
Aspirin may help prevent this mechanism of action from occurring and can reduce the prevalence or severity of flushing if taken around 30 minutes before your dose of Tecfidera.
However, aspirin may not be suitable for everyone and can interact with other medications, so you should speak to your healthcare provider before taking it.
Aside from aspirin, taking Tecfidera after eating can also help prevent flushing.
You are more likely to experience flushes when you start taking Tecfidera and it may ease off after several weeks of treatment. If you experience severe or persistent flushes, you should speak to your healthcare provider about the best course of action.
Are Tecfidera, Vumerity, Fumaderm, and Skilarence the same?
Tecfidera, Fumaderm, and Skilarence are all brand names for drugs containing the active ingredient dimethyl fumarate, while Vumerity contains the active ingredient diroximel fumarate. Differences between the drugs include chemical structures and approved uses (which also varies by country).
Tecfidera
Tecfidera is approved by the FDA in the US, the EMA in the European Union, and in other markets around the world to treat relapsing forms of multiple sclerosis. It contains the active ingredient dimethyl fumarate and is taken orally twice a day (starting with 120 mg capsules for the first 7 days of treatment and 240 mg capsules thereafter).
Skilarence
Skilarence is a brand name for another drug containing dimethyl fumarate. However, it is approved by the EMA for the treatment of plaque psoriasis and is not (at the time of writing) approved to treat multiple sclerosis. Skilarence has a maximum dose of 240 mg tablets taken 3 times per day, although not everyone requires this if lower doses prove effective.
Fumaderm
Fumaderm is a brand name for dimethyl fumarate that also contains calcium, zinc, and magnesium salts of monoethyl fumarate. It is approved in Germany for the treatment of psoriasis.
Vumerity
Vumerity is the brand name for diroximel fumarate (rather than dimethyl fumarate), produced by the same pharmaceutical company (Biogen) as Tecfidera. Although it shares chemical similarities with Tecfidera, Biogen claims that Vumerity is less likely to cause gastrointestinal side effects. Vumerity has not (at the time of writing) been approved outside of the US.
Generics and biosimilars
Generic dimethyl fumarate and biosimilars (such as monomethyl fumarate, sold under the brand name Bafiertam) may also be available as alternative treatments in some countries.
Other oral medications for relapsing forms of MS are also available. To get a full understanding of the options available and to help decide which is the best for you, you should speak to your doctor and MS care team.
What should I do if I miss a dose of Tecfidera (dimethyl fumarate)?
If you miss a dose of Tecfidera, it is recommended that you take it as soon as you remember unless it is almost time for your next dose, in which case you should skip the missed dose and continue taking it as normal. You should never double dose to make up for a missed dose and should allow at least 4 hours between two doses.
The content on this page is provided for informational purposes only. If you have any questions or concerns about your treatment, you should talk to your doctor, pharmacist, or healthcare professional. This is particularly important if you are taking multiple medications or have any existing medical conditions.
