Teriflunomide

What is Teriflunomide?

• Teriflunomide (AUBAGIO) is a pyrimidine synthesis inhibitor used to treat relapsing multiple sclerosis.

Teriflunomide

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What are the uses of this medicine?

• AUBAGIO is a prescription medicine used to treat relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults.

How does this medicine work?

• Teriflunomide (ter" i floo' noe mide) is the active metabolite of leflunomide, an immunomodulatory agent similar to thalidomide, and is used in the treatment of rheumatoid arthritis.
• The mechanism of action of teriflunomide appears to be based, at least in part, upon inhibition of the enzyme dihydro-orotate dehydrogenase, which is an important step in pyrimidine synthesis.
• The activation and proliferation of lymphocytes are dependent upon pyrimidine synthesis and is acutely sensitive to its inhibition, resulting in suppression of ongoing immune reactivity.
• Teriflunomide has other activities including inhibition of NF-kappa B pathways that may contribute to its immunomodulatory actions.
• In animal models of multiple sclerosis, teriflunomide was shown to have beneficial effects which led to its critical evaluation in this disease.
• In several large, randomized controlled trials, teriflunomide was found to reduce relapse rates and improve neuro-radiologic outcomes in adult patients with relapsing-remitting multiple sclerosis.

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have severe liver problems.
• are pregnant or are of childbearing age and not using effective birth control.
• have had an allergic reaction to leflunomide, teriflunomide, or any other ingredients in AUBAGIO.
• take a medicine called leflunomide.

What drug interactions can this medicine cause?

• In patients taking AUBAGIO, exposure of drugs metabolized by CYP2C8 (e.g., paclitaxel, pioglitazone, repaglinide, rosiglitazone) may be increased. Monitor these patients and adjust the dose of the concomitant drug(s) metabolized by CYP2C8 as required.
• Coadministration of AUBAGIO with warfarin requires close monitoring.
• AUBAGIO may increase the systemic exposures of ethinylestradiol and levonorgestrel. Consideration should be given to the type or dose of contraceptives used in combination with AUBAGIO.
• In patients taking AUBAGIO, exposure of drugs metabolized by CYP1A2 (e.g., alosetron, duloxetine, theophylline, tizanidine) may be reduced.
• In patients taking AUBAGIO, exposure of drugs which are OAT3 substrates (e.g., cefaclor, cimetidine, ciprofloxacin, penicillin G, ketoprofen, furosemide, methotrexate, zidovudine) may be increased.
• For a patient taking AUBAGIO, the dose of rosuvastatin should not exceed 10 mg once daily. For other substrates of BCRP (e.g., mitoxantrone) and drugs in the OATP family (e.g., methotrexate, rifampin), especially HMG-Co reductase inhibitors (e.g., atorvastatin, nateglinide, pravastatin, repaglinide, and simvastatin), consider reducing the dose.

Is this medicine FDA approved?

• Teriflunomide was approved for use for multiple sclerosis in the United States in 2012 and is now available in tablets of 7 and 14 mg under the brand name Aubagio.

How should this medicine be used?

Recommended dosage:

• The recommended dose of AUBAGIO is 7 mg or 14 mg orally once daily. AUBAGIO can be taken with or without food.

Administration:

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

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 7 mg and 14 mg film-coated tablets

This medicine is available in fallowing brand namesː

• AUBAGIO

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache
• diarrhea
• nausea
• hair thinning or loss (alopecia)
• increases in the results of blood tests to check your liver function

AUBAGIO may cause serious side effects, including:

• Liver problems
• Harm to your unborn baby
• decreases in your white blood cell count
• allergic reactions
• serious skin reactions
• allergic reactions
• numbness or tingling in your hands or feet that is different from your MS symptoms
• high blood pressure
• new or worsening breathing problems

What special precautions should I follow?

• Clinically significant and potentially life-threatening liver injury, including acute liver failure requiring transplant, has been reported in patients treated with AUBAGIO. Obtain serum transaminase and bilirubin levels within 6 months before initiation of AUBAGIO therapy. Monitor ALT levels at least monthly for six months after starting AUBAGIO. Consider additional monitoring when AUBAGIO is given with other potentially hepatotoxic drugs.
• AUBAGIO may cause fetal harm when administered to a pregnant woman. Exclude pregnancy before starting treatment with AUBAGIO in females of reproductive potential. Advise females of reproductive potential to use effective contraception during AUBAGIO treatment and during an accelerated drug elimination procedure after AUBAGIO treatment.
• Elimination of AUBAGIO can be accelerated by administration of cholestyramine or activated charcoal for 11 days.
• AUBAGIO may decrease WBC. A recent CBC should be available before starting AUBAGIO. Monitor for signs and symptoms of infection. Consider suspending treatment with AUBAGIO in case of serious infection. Do not start AUBAGIO in patients with active infections.
• Stop AUBAGIO if patient has anaphylaxis, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms; initiate rapid elimination.
• If patient develops symptoms consistent with peripheral neuropathy, evaluate patient and consider discontinuing AUBAGIO.
• AUBAGIO may increase blood pressure. Measure blood pressure at treatment initiation and monitor blood pressure during treatment.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• There is no experience regarding teriflunomide overdose or intoxication in humans.

Management of overdosage:

• In the event of clinically significant overdose or toxicity, cholestyramine or activated charcoal is recommended to accelerate elimination

Can this medicine be used in pregnancy?

• AUBAGIO is contraindicated for use in pregnant women and females of reproductive potential not using effective contraception because of the potential for fetal harm based on animal data.
• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to AUBAGIO during pregnancy. Healthcare providers and patients are encouraged to report pregnancies by calling 1-800-745-4447.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

• Active ingredient: teriflunomide
• Inactive ingredients in 7 mg and 14 mg tablets: lactose monohydrate, corn starch, hydroxypropyl cellulose, microcrystalline cellulose, sodium starch glycolate, magnesium stearate, hypromellose, titanium dioxide, talc, polyethylene glycol and indigo carmine aluminum lake.

In addition, the 7 mg tablets also contain iron oxide yellow.

Who manufactures and distributes this medicine?

• Manufactured for:

Genzyme Corporation Cambridge, MA A SANOFI COMPANY

What should I know about storage and disposal of this medication?

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

Multiple sclerosis drugs

Disease modifying agents

• Alemtuzumab
• Dimethyl Fumarate
• Fingolimod
• Glatiramer Acetate
• Interferon Beta
• Interferon Beta-1a
• Interferon Beta-1b
• Peginterferon Beta-1a
• Mitoxantrone
• Natalizumab
• Ocrelizumab
• Teriflunomide

Symptomatic Therapies

• Dalfampridine

• Dailymed label info on Teriflunomide
• FDA Teriflunomide

Teriflunomide Resources
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