Tecfidera

Tecfidera is the brand name for dimethyl fumarate, a prescription medication used to treat relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults.

Tecfidera is a disease-modifying therapy (DMT) and belongs to the drug class called selective immunosuppressants.

Tecfidera delayed-release capsules are taken by mouth twice daily, with or without food. Taking Tecfidera with food may help reduce flushing. Swallow the capsules whole; do not crush, chew, or open them.

• Starting dose: 120 mg twice daily for 7 days
• Maintenance dose: 240 mg twice daily after the first week.

Tecfidera has been shown to activate a cell pathway called Nrf2, which is involved in how cells respond to oxidative stress. Tecfidera can also lower the number of lymphocytes, a type of white blood cell that is part of the immune system. However, it is not known exactly how Tecfidera works to treat MS.

Yes. Generic Tecfidera is available as dimethyl fumarate delayed-release capsules. Generic dimethyl fumarate contains the same active ingredient as Tecfidera and comes in the same strengths (120 mg and 240 mg).

In clinical studies, Tecfidera 240 mg taken twice daily reduced the yearly relapse rate by 53% and 44% compared with placebo in people with relapsing-remitting multiple sclerosis (RRMS). It also reduced the number of new brain lesions seen on MRI scans.

These results come from two 2-year studies that compared Tecfidera with placebo (an inactive treatment) in adults with RRMS.

Fewer relapses

• In Study 1, 27% of people taking Tecfidera had a relapse, compared with 46% of people taking placebo. This was a 49% reduction in relapse risk.
• In Study 2, 29% of people taking Tecfidera had a relapse, compared with 41% of people taking placebo. This was a 34% reduction in relapse risk.

Fewer new MRI lesions

In both studies, people taking Tecfidera had fewer new or enlarging T2 lesions and fewer new T1 lesions over 2 years. They also had fewer gadolinium-enhancing (active) lesions at 2 years. For example, people taking Tecfidera in Study 1 had an average of 2.6 new or enlarging T2 lesions, compared with 17 for people taking placebo.

Disability progression

In Study 1, 16% of people taking Tecfidera had confirmed disability progression, compared with 27% of people taking placebo, a 38% reduction in risk. In Study 2, Tecfidera did not significantly reduce disability progression (13% vs 17%).

Take Tecfidera exactly as prescribed by your doctor. Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose.

Your doctor will perform blood tests to make sure you do not have conditions that would prevent you from safely using this medication.

You may take Tecfidera with or without food. Taking the medicine with food may help prevent flushing (warmth, redness, itching, or burning).

Swallow the capsule whole, and do not crush, chew, break, or open it.

While using this medicine, you will need frequent blood tests.

Store this medicine in the original container at room temperature, away from moisture, heat, and light.

Serious allergic reactions. Tecfidera can cause anaphylaxis and angioedema, after the first dose or at any time during treatment. Stop taking Tecfidera and get emergency help if you have trouble breathing, hives, or swelling of your throat or tongue.

PML (brain infection). Progressive multifocal leukoencephalopathy (PML) is a rare viral brain infection that usually causes death or severe disability. It has occurred in people taking Tecfidera, mostly in those with low lymphocyte counts lasting more than 6 months. Tell your doctor right away if you have symptoms that get worse over days or weeks, such as weakness on one side of your body, clumsiness, vision problems, confusion, or changes in thinking, memory, or personality.

Shingles and other serious infections. Serious shingles (herpes zoster) and other serious viral, fungal, and bacterial infections have occurred with Tecfidera, even in people with normal lymphocyte counts. Tell your doctor if you have signs of infection. Your doctor may pause Tecfidera until the infection clears.

Low lymphocyte counts. Tecfidera can lower your lymphocyte (white blood cell) count, and it may take months to recover after stopping treatment. Your doctor will check your blood counts before you start, after 6 months, and then every 6 to 12 months.

Liver injury. Tecfidera can cause liver injury, which may start days to months after you begin treatment. Your doctor will check your liver function before and during treatment.

Flushing. Flushing (warmth, redness, itching, or burning) is common, especially when you first start Tecfidera, and usually improves over time. Taking Tecfidera with food may help.

Serious stomach and bowel problems. Serious problems, including bleeding, ulcers, tears (perforation), and blockage of the stomach or intestines, have been reported, most often within the first 6 months of treatment. Some have been fatal. Tell your doctor right away if you have new or worsening severe stomach or bowel symptoms.

You should not use Tecfidera if you have ever had a severe allergic reaction (such as anaphylaxis or angioedema) to dimethyl fumarate or any of the inactive ingredients in this medication.

To make sure this medication is safe for you, tell your doctor if you have ever had:

• an active infection; or
• low white blood cell (WBC) counts.

Tecfidera is not approved for use by anyone younger than 18 years old.

Pregnancy

Tell your doctor if you are pregnant or plan to become pregnant, as it is not known if Tecfidera will harm your unborn baby. You and your doctor will have to decide if you should take this medicine while you are pregnant or if you plan to become pregnant.

Breastfeeding

Tell your doctor if you are breastfeeding or plan to breastfeed. It is not known if Tecfidera passes into your breast milk. You and your doctor should decide if you will take this medicine or breastfeed.

Tecfidera pregnancy and breastfeeding warnings (more detail)

The most common Tecfidera side effects are flushing, stomach pain, diarrhea, and nausea. Other common side effects include vomiting, itching, rash, and indigestion. Flushing and stomach side effects are most common in the first month of treatment and usually improve over time.

Flushing

Flushing is the most common Tecfidera side effect, affecting about 40% of people in clinical trials. It can cause warmth, redness, itching, or a burning sensation. Flushing usually begins soon after starting Tecfidera and usually improves or goes away over time. It is usually mild or moderate. Less than 1% of people had serious flushing that led to hospitalization, and 3% of people stopped Tecfidera because of flushing.

How to reduce Tecfidera flushing

Taking Tecfidera with food may help reduce flushing. In healthy volunteers, taking Tecfidera with food reduced flushing by about 25%. Your doctor may also suggest taking non-enteric-coated aspirin (up to 325 mg) 30 minutes before Tecfidera to reduce flushing.

Gastrointestinal side effects

Tecfidera's gastrointestinal (GI) side effects include nausea, vomiting, diarrhea, stomach pain, and indigestion (dyspepsia). GI side effects were more common at the start of treatment (usually in the first month) and usually decreased over time. In clinical trials, 4% of people taking Tecfidera and less than 1% of people taking placebo stopped treatment because of GI side effects.

Serious Tecfidera side effects

Get emergency medical help if you have signs of an allergic reaction to this medication, such as hives, difficulty breathing, or swelling of your face, lips, tongue, or throat.

Dimethyl fumarate may cause a serious brain infection called progressive multifocal leukoencephalopathy (PML) that can lead to disability or death. Call your doctor right away if you have problems with speech, thought, vision, or muscle movement. These symptoms may start gradually and get worse quickly.

Also, call your doctor at once if you have:

• symptoms of herpes virus infection: flu-like symptoms, cold sores around your mouth, a tingly or painful blistering rash, or burning pain in your thigh or lower back
• low white blood cell counts: fever, mouth sores, skin sores, sore throat, cough, or trouble breathing
• liver problems: severe tiredness, loss of appetite, pain on the upper right side of your stomach, dark or tea-colored urine, or yellowing of your skin or the whites of your eyes (jaundice)
• pancreatitis: severe pain in your upper stomach spreading to your back, nausea, or vomiting
• serious stomach or bowel problems, including bleeding, ulcers, blockage, and tears (perforation) of the stomach or intestines: stomach pain that does not go away, bright red or black stools (that look like tar), severe vomiting, severe diarrhea, coughing up blood or blood clots, or vomiting blood or vomit that looks like coffee grounds

Also, see the Warnings section.

This is not a complete list of side effects, and others may occur. Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Usual Adult Dose for Multiple Sclerosis:

• Initial dose: 120 mg orally twice a day for 7 days
• Maintenance dose: 240 mg orally twice a day
• For patients who do not tolerate the maintenance dose, a temporary dose reduction to 120 mg twice a day may be considered. The 240 mg twice-a-day dose should be resumed within 4 weeks.

Approved indication: The treatment of adult patients with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.

Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

Do not take Tecfidera together with diroximel fumarate (Vumerity), which is converted to the same active form in the body.

Other drugs may interact with dimethyl fumarate, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell your doctor about all your current medicines and any medicine you start or stop using.

Click the link below to check for interactions with this medicine.

• Store at 15°C to 30°C (59°F to 86°F).
• Protect the capsules from light.
• Store in the original container.

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.

Manufactured for: Biogen Inc., Cambridge, MA 02142. For more information, go to www.TECFIDERA.com or call 1-800-456-2255.