Drug information of teriflunomide


Drug group:

Teriflunomide is the active metabolite of leflunomide, and it acts as an immunomodulatory agent by inhibiting pyrimidine synthesis and is indicated for the treatment of multiple sclerosis, specifically relapsing forms.

Mechanism of effect

The exact mechanism by which teriflunomide acts in MS is not known. What is known is that teriflunomide prevents pyrimidine synthesis by inhibiting the mitochondrial enzyme dihydroorotate dehydrogenase, and this may be involved in its immunomodulatory effect in MS.


Teriflunomide is an immunomodulatory agent that decreases the amount of activated CNS lymphocytes, which results in anti-inflammatory and antiproliferative effects.


  • Peak plasma time: 1-4 hr
  • Protein Bound: 99%
  • Vd: 11 L
  • Metabolism: Primary biotransformation to minor (inactive) metabolites by hydrolysis
  • Secondary pathways: oxidation, N-acetylation, sulfate conjugation
  • CYP2C8 inihibitor; CYP1A2 inducer
  • Total body clearance: 30 mL/hr

Drug indications

Multiple sclerosis



Multiple Sclerosis

Indicated for treatment of relapsing forms of multiple sclerosis

7 mg or 14 mg PO qDay


Safety and efficacy not established


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May take an average of 8 months to clear drug from plasma; consider accelerated elimination with cholestyramine or activated charcoal

Decreases in white blood cell count and platelet count have been observed

Not recommended for patients with serious immunodeficiency; do not initiate treatment in patients with active acute or chronic infections

Peripheral neuropathy, including polyneuropathy and mononeuropathy have been reported; evaluate patient and consider discontinuing therapy

May cause an increases in renal uric acid clearance and decreases in serum uric acid

Use caution in hyperkalemia

Anaphylaxis and severe allergic reactions reported; signs and symptoms have included dyspnea, urticaria, and angioedema including lips, eyes, throat, and tongue.

May increase blood pressure; measure blood pressure at treatment initiation and monitor blood pressure during treatment

Interstitial lung disease, including acute interstitial pneumonitis, reported; use with caution in patients with pre-existing respiratory conditions; monitor for new or worsening respiratory symptoms

May decrease WBC; a recent CBC should be available before starting teriflunomide; monitor for signs and symptoms of infection; consider suspending treatment with teriflunomide in case of serious infection; do not start teriflunomide in patients with active infections

Black Box Warnings

Hepatotoxicity: severe liver injury including fatal liver failure has been reported with other drugs in class; monitor liver enzymes monthly for 6 months and discontinue if liver injury is suspected

Risk of teratogenicity: animal data shows major birth defects if used during pregnancy; exclude pregnancy before the start of therapy in females of reproductive potential; advise females of reproductive potential to use effective contraception during therapy and during an accelerated drug elimination procedure after therapy; stop therapy and use an accelerated drug elimination procedure if patient becomes pregnant contraindicated in women of child bearing potential who are not using reliable contraception

Points of recommendation

Follow all directions on your prescription label. Your doctor may occasionally change your dose to make sure you get the best results. Do not use teriflunomide in larger or smaller amounts or for longer than recommended.

You may take teriflunomide with or without food.

Your blood pressure will need to be checked often.

Teriflunomide can lower blood cells that help your body fight infections and help your blood to clot. Your blood will need to be tested often. Your teriflunomide treatment may be stopped for a short time based on the results of these tests.

After you stop taking teriflunomide, you may need to be treated with other medicines to help your body eliminate teriflunomide quickly. If you do not undergo this drug elimination procedure, teriflunomide could stay in your body for up to 2 years. Follow your doctor's instructions.

You will also need to go through this drug elimination procedure if you plan to become pregnant after you stop taking teriflunomide.

Store at room temperature away from moisture and heat.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

Pregnancy level


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