Teriflunomide

Teriflunomide is a prescription medication used to treat relapsing forms of multiple sclerosis (MS). Teriflunomide belongs to a group of drugs called immunomodulatory agents. These are believed to work by reducing inflammation and decreasing the action of immune cells that may cause nerve damage.

This medication comes in tablet form and is taken once a day, with or without food.

Common side effects of teriflunomide include increases in liver blood test results, hair thinning or loss (alopecia), and diarrhea.

Teriflunomide is a prescription medication used to treat relapsing forms of multiple sclerosis (MS). Teriflunomide can decrease the number of MS flare-ups (relapses). Teriflunomide does not cure MS, but it can help slow down the physical problems that MS causes.

It is not known if teriflunomide is safe and effective in children.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Teriflunomide may be found in some form under the following brand names:

• Aubagio

The most common side effects of teriflunomide include:

• increases in the results of blood tests to check your liver
• hair thinning or loss (alopecia)
• diarrhea
• flu
• nausea
• burning or prickling feeling in your skin (paraesthesia)

Tell your doctor if you have any side effect that bothers you or that does not go away.

These are not all the possible side effects of teriflunomide. For more information, ask your doctor or pharmacist.

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-332-1088.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• medications that stop an enzyme called BCRP such as cyclosporine (Gengraf, Neoral, Sandimmune), eltrombopag (Promacta), gefitinib (Iressa)
• ethinylestradiol and levonorgestrel (such as Climara, Daysee, Seasonique, Quartette, Seasonale)
• medications that use an enzyme CYP2C8 such as amiodarone (Cordarone), cabazitaxel (Jevtana), carbamazepine (Tegretol), chloroquine (Aralen), diclofenac (Voltaren), ibuprofen (Advil), paclitaxel (Taxol), rosiglitazone (Avandia), repaglinide (Prandin), treprostinil (Tyvaso)
• medications that use the enzyme CYP1A2 such as alosetron (Lotronex), caffeine, clozapine (Clozaril), flutamide (Eulexin), frovatriptan (Frova), melatonin, mexiletine (Mexitil),  mirtazapine (Remeron), olanzapine (Zyprexa), ramelteon (Rozerem), rasagiline (Azilect), ropinirole (Requip), tacrine (Cognex), theophylline, tizanidine (Zanaflex), triamterene (Dyrenium), zolmitriptan (Zomig)
• warfarin (Jantoven, Coumadin)

This is not a complete list of teriflunomide drug interactions. Ask your doctor or pharmacist for more information.

What is the most important information I should know about teriflunomide?

Teriflunomide may cause serious side effects, including:

• Liver problems: Teriflunomide may cause serious liver problems that may lead to death. Your risk of liver problems may be higher if you take other medicines that also affect your liver. Your doctor should do blood tests to check your liver:
  • within 6 months before you start taking teriflunomide
  • 1 time a month for 6 months after you start taking teriflunomide
  Call your doctor right away if you have any of the following symptoms of liver problems:
  • nausea
  • vomiting
  • stomach pain
  • loss of appetite
  • tiredness
  • your skin or the whites of your eyes turn yellow
  • dark urine
• Harm to your unborn baby: Teriflunomide may cause harm to your unborn baby. Do not take teriflunomide if you are pregnant. Do not take teriflunomide unless you are using effective birth control.
  • If you are a female, you should have a pregnancy test before you start taking teriflunomide. Use effective birth control during your treatment with teriflunomide.
  • After stopping teriflunomide, continue using effective birth control until you have blood tests to make sure your blood levels of teriflunomide are low enough. If you become pregnant while taking teriflunomide or within 2 years after you stop taking it, tell your doctor right away.
  • Teriflunomide Pregnancy Registry. If you become pregnant while taking teriflunomide or during the 2 years after you stop taking teriflunomide, talk to your doctor about enrolling in the teriflunomide pregnancy registry at 1-800-745-4447, option 2. The purpose of this registry is to collect information about your health and your baby's health.
  • For men taking teriflunomide:
    • If your female partner plans to become pregnant, you should stop taking teriflunomide and ask your doctor how to quickly lower the levels of teriflunomide in your blood.
    • If your female partner does not plan to become pregnant, you and your female partner should use effective birth control during your treatment with teriflunomide. teriflunomide remains in your blood after you stop taking it, so continue using effective birth control until teriflunomide blood levels have been checked and they are low enough.

Teriflunomide may stay in your blood for up to 2 years after you stop taking it. Your doctor can prescribe a medicine to help lower your blood levels of teriflunomide more quickly. Talk to your doctor if you want more information about this.

Teriflunomide may cause serious side effects including:

• decreases in your white blood cell count. Your white blood cell counts should be checked before you start taking teriflunomide. When you have a low white blood cell count you:
  • may have more frequent infections. You should have a skin test for TB (Tuberculosis) before you start taking teriflunomide. Tell your doctor if you have any of these symptoms of an infection:
    • fever
    • tiredness
    • body aches
    • chills
    • nausea
    • vomiting
  • should not receive certain vaccinations during your treatment with teriflunomide and for 6 months after your treatment with teriflunomide ends.
• numbness or tingling in your hands or feet that is different from your MS symptoms. You have a greater chance of getting peripheral neuropathy if you:
  • are over 60 years of age
  • take certain medicines that affect your nervous system
  • have diabetes
  Tell your doctor if you have numbness or tingling in your hands or feet that is different from your MS.
• kidney problems. Tell your doctor if you have pain in your side (flank pain).
• high potassium levels in your blood. Tell your doctor if you have nausea that does not go away or a racing heartbeat.
• serious skin problems. Tell your doctor if you have any skin problems such as redness and peeling.
• new or worsening breathing problems. Tell your doctor if you have shortness of breath or coughing with or without fever.
• high blood pressure. Your doctor should check your blood pressure before you start taking teriflunomide and while you are taking teriflunomide.

Do not take teriflunomide if you:

• have severe liver problems
• are pregnant or are of childbearing age and not using effective birth control
• take a medicine called leflunomide

Medications can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of teriflunomide, there are no specific foods that you must exclude from your diet when receiving this medication.

Before you take teriflunomide, tell your doctor if you:

• have liver or kidney problems
• have a fever or infection, or you are unable to fight infections
• have numbness or tingling in your hands or feet that is different from your MS symptoms
• have diabetes
• have had serious skin problems when taking other medicines
• have breathing problems
• have high blood pressure
• are breastfeeding or plan to breastfeed. It is not known if teriflunomide passes into your breast milk. You and your doctor should decide if you will take teriflunomide or breastfeed. You should not do both at the same time.

Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements.

Using teriflunomide and other medicines may affect each other causing serious side effects. Teriflunomide may affect the way other medicines work, and other medicines may affect how teriflunomide works.

Especially tell your doctor if you take medicines that could raise your chance of getting infections, including medicines used to treat cancer or to control your immune system.

Ask your doctor or pharmacist for a list of these medicines if you are not sure.

Know the medicines you take. Keep a list of them to show your doctor or pharmacist when you get a new medicine.

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

This medication falls into category X. Teriflunomide may cause harm to your unborn baby. Do not take teriflunomide if you are pregnant. Do not take teriflunomide unless you are using effective birth control.

• If you are a female, you should have a pregnancy test before you start taking teriflunomide. Use effective birth control during your treatment with teriflunomide.
• After stopping teriflunomide, continue using effective birth control until you have blood tests to make sure your blood levels of teriflunomide are low enough. If you become pregnant while taking teriflunomide or within 2 years after you stop taking it, tell your doctor right away.
• Teriflunomide Pregnancy Registry. If you become pregnant while taking teriflunomide or during the 2 years after you stop taking teriflunomide, talk to your doctor about enrolling in the teriflunomide pregnancy registry at 1-800-745-4447, option 2. The purpose of this registry is to collect information about your health and your baby's health.
• For men taking teriflunomide:
  • If your female partner plans to become pregnant, you should stop taking teriflunomide and ask your doctor how to quickly lower the levels of teriflunomide in your blood.
  • If your female partner does not plan to become pregnant, you and your female partner should use effective birth control during your treatment with teriflunomide. teriflunomide remains in your blood after you stop taking it, so continue using effective birth control until teriflunomide blood levels have been checked and they are low enough.

It is not known if teriflunomide crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with use of this medication, a choice should be made whether to stop nursing or stop the use of this medication. Your doctor and you will decide if the benefits outweigh the risk of using teriflunomide.

• Take teriflunomide exactly as your doctor tells you to take it.
• Take teriflunomide 1 time each day.
• Take teriflunomide with or without food.

If you take too much this medication, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.

If this medication is administered by a healthcare provider in a medical setting, it is unlikely that an overdose will occur. However, if overdose is suspected, seek emergency medical attention.

• Store teriflunomide at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep teriflunomide and all medicines out of reach of children.

Hepatotoxicity

Severe liver injury including fatal liver failure has been reported in patients treated with leflunomide, which is indicated for rheumatoid arthritis. A similar risk would be expected for teriflunomide because recommended doses of teriflunomide and leflunomide result in a similar range of plasma concentrations of teriflunomide. Concomitant use of teriflunomide with other potentially hepatotoxic drugs may increase the risk of severe liver injury. Obtain transaminase and bilirubin levels within 6 months before initiation of teriflunomide therapy. Monitor ALT levels at least monthly for six months after starting teriflunomide. If drug induced liver injury is suspected, discontinue teriflunomide and start an accelerated elimination procedure with cholestyramine or charcoal. Teriflunomide is contraindicated in patients with severe hepatic impairment. Patients with pre-existing liver disease may be at increased risk of developing elevated serum transaminases when taking teriflunomide.

Risk of Teratogenicity

Based on animal data, teriflunomide may cause major birth defects if used during pregnancy. Pregnancy must be excluded before starting teriflunomide. teriflunomide is contraindicated in pregnant women or women of childbearing potential who are not using reliable contraception. Pregnancy must be avoided during teriflunomide treatment or prior to the completion of an accelerated elimination procedure after teriflunomide treatment