Tecfidera (Dimethyl Fumarate) has been approved since January 2014 for the treatment of relapsing-remitting multiple sclerosis. Many patients have been waiting for this medication due to positive study results, while others are excited about the possibility of treating their multiple sclerosis with a tablet. Moreover, the medication is considered to have relatively few side effects, making it a popular choice among many MS patients for the therapy of their disease.From a medical perspective, this can be confirmed. Tecfidera is an expansion of the therapeutic possibilities for MS, and many patients manage well with Tecfidera and show good stabilization of the disease. Nevertheless, there are always questions about side effects and the tolerance of the medication (especially since the report of a PML case in the past, see blog from 06.03.15 “First PML case under Tecfidera”).
Tecfidera is an interesting substance in that it contains the active ingredient Dimethyl Fumerate, which plays a role in the body’s energy metabolism, namely in the so-called citric acid cycle. Therefore, the metabolism of Tecfidera takes place via the so-called respiratory chain, i.e., the drug is not metabolized in the liver like many other drugs, but is “exhaled”. Therefore, few interactions with other medications are to be expected when taking Tecfidera.
The half-life of Tecfidera is also relatively low, i.e., about 4 hours after taking the medication, the active ingredient can no longer be detected. This is advantageous in that after discontinuation of the medication, the active ingredient is quickly removed from the body, which can be significant, for example, in relation to a planned pregnancy. On the other hand, this requires regular intake of the tablets.
Patients taking Tecfidera usually complain about two significant side effects of the medication. These are gastrointestinal (stomach/intestine) side effects on the one hand and the so-called flush symptomatology – a sensation of heat and redness of the body and face – on the other hand. These two side effects are directly linked to the intake of the active ingredient and occur particularly in the first weeks of intake. According to the results from the licensing studies, it must be expected that about 30% of the patients who take Tecfidera for the first time complain about these side effects. On the other hand, the study data also show that these side effects completely disappear in most patients after the first few months.
What can be done against these side effects? With regard to the gastrointestinal side effects, it has been shown that it is very helpful if Tecfidera is not taken on an empty stomach, but together with a meal. The simultaneous intake does not affect the absorption of Tecfidera, but significantly improves the tolerance – i.e., patients who have a good breakfast in the morning, for example, are clearly at an advantage. The gastrointestinal side effects are probably due to a local irritation of the stomach and intestinal wall, which is why dilution by simultaneous intake with meals is a sensible concept.
In the event that simultaneous intake of food does not help, the dose can be temporarily reduced to 2 x 120 mg/per day. However, this should not be carried out for too long, as a daily dose of 240 mg is probably not sufficiently effective. In addition, classic medications for the treatment of heartburn can be used.
As far as the flush symptomatology is concerned, many patients find this much less disturbing than the gastrointestinal side effects. Nevertheless, this side effect can also be burdensome. Here too, a temporary dose reduction can help. An American study has also shown that the simultaneous intake of aspirin can reduce the severity of the flush symptomatology. However, since aspirin affects the function of platelets, it is certainly not a concept that should be applied permanently.
Other side effects worth mentioning are an increased protein excretion in the urine, which is why it makes sense to have a regular urine check. Another important point that came into discussion due to the PML case is the reduction of white blood cells by Tecfidera.
The intake of Tecfidera leads on average to a slight decrease in the so-called lymphocytes, a subgroup of white blood cells. In some patients (probably about 10% can be assumed), there is a significant drop in lymphocytes. According to current knowledge, we would recommend discontinuing the medication if the values for the lymphocytes are repeatedly measured below 500/µl. Therefore, regular control of the differential blood count should take place under Tecfidera – i.e., in the first weeks, a 2-week control of the blood count should take place, later monthly controls.
