Important: This page is general information, not medical advice. It does not recommend or prescribe any treatment. Always consult your doctor or pharmacist before starting, stopping or changing any medicine.
Quick facts
- Drug class
- Pyrimidine Synthesis Inhibitor [EPC], Dihydroorotate Dehydrogenase Inhibitors [MoA]
- How it is given
- oral
- Type
- human prescription drug
- RxNorm ID
- 1310525
We do not publish dosing. How much of this medicine to take, how often, and for how long depends on your age, weight, kidney and liver function, other conditions and other medicines. That is a decision for the person who prescribes or dispenses it. Follow the directions on your own pack and ask your pharmacist if anything is unclear.
What it is used to treat
Teriflunomide tablets are indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. Teriflunomide tablets are a pyrimidine synthesis inhibitor indicated for the treatment of relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. ( 1 )
About this medicine
Teriflunomide is an oral de novo pyrimidine synthesis inhibitor of the DHO-DH enzyme, with the chemical name (Z)-2-Cyano-α,α,α-trifluoro-3-hydroxy-4-crotonotoluidide. Its molecular weight is 270.21, and the molecular formula is C 12 H 9 F 3 N 2 O 2 with the following chemical structure: Teriflunomide is a white to almost white powder that is sparingly soluble in acetone, slightly soluble in polyethylene glycol and ethanol, very slightly soluble in isopropanol and practically insoluble in water. Teriflunomide is formulated as film-coated tablets for oral administration. Teriflunomide tablets contain 7 mg or 14 mg of teriflunomide and the following inactive ingredients: colloidal silicon dioxide, corn starch, hydroxypropyl cellulose, hypromellose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, polyethylene glycol, sodium starch glycolate (potato) and titanium dioxide. The 7 mg tablets also contain FD&C Blue No. 2 Aluminum Lake and FD&C Yellow No. 6 Aluminum Lake and the 14 mg tablets also contain red iron oxide and yellow iron oxide. Teriflunomide Structural Formula
How it works
12.1 Mechanism of Action Teriflunomide, an immunomodulatory agent with anti-inflammatory properties, inhibits dihydroorotate dehydrogenase, a mitochondrial enzyme involved in de novo pyrimidine synthesis. The exact mechanism by which teriflunomide exerts its therapeutic effect in multiple sclerosis is unknown but may involve a reduction in the number of activated lymphocytes in CNS.
Who should not take it
Teriflunomide tablets are contraindicated in/with: • Patients with severe hepatic impairment [see Warnings and Precautions (5.1) ] . • Pregnant women and females of reproductive potential not using effective contraception. Teriflunomide tablets may cause fetal harm [see Warnings and Precautions (5.2 , 5.3) and Use in Specific Populations (8.1) ] . • Patients with a history of a hypersensitivity reaction to teriflunomide, leflunomide, or to any of the inactive ingredients in teriflunomide tablets. Reactions have included anaphylaxis, angioedema, and serious skin reactions [see Warnings and Precautions (5.5) ]. • Coadministration with leflunomide [see Clinical Pharmacology (12.3) ]. • Severe hepatic impairment ( 4 , 5.1 ) • Pregnancy ( 4 , 5.2 , 8.1 ) • Hypersensitivity ( 4 , 5.5 ) • Current leflunomide treatment ( 4 )
Warnings and cautions
• Elimination of teriflunomide tablets can be accelerated by administration of cholestyramine or activated charcoal for 11 days. ( 5.3 ) • Teriflunomide tablets may decrease WBC. A recent CBC should be available before starting teriflunomide tablets. Monitor for signs and symptoms of infection. Consider suspending treatment with teriflunomide tablets in case of serious infection. Do not start teriflunomide tablets in patients with active infections. ( 5.4 ) • Stop teriflunomide tablets if patient has anaphylaxis, angioedema, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug reaction with eosinophilia and systemic symptoms; initiate rapid elimination. ( 5.3 , 5.5 , 5.6 , 5.7 ) • If patient develops symptoms consistent with peripheral neuropathy, evaluate patient and consider discontinuing teriflunomide tablets. ( 5.8 ) • Teriflunomide tablets may increase blood pressure. Measure blood pressure at treatment initiation and monitor blood pressure during treatment. ( 5.9 ) 5.1 Hepatotoxicity Clinically significant and potentially life-threatening liver injury, including acute liver failure requiring transplant, has been reported in patients treated with teriflunomide tablets in the postmarketing setting. Patients with pre-existing liver disease and patients taking other hepatotoxic drugs may be at increased risk for developing liver injury when taking teriflunomide tablets. Clinically significant liver injury can occur at any time during treatment with teriflunomide tablets. Patients with pre-existing acute or chronic liver disease, or those with serum alanine aminotransferase (ALT) greater than two times the upper limit of normal (ULN) before initiating treatment, should not normally be treated with teriflunomide tablets. Teriflunomide tablets are contraindicated in patients with severe hepatic impairment [see Contraindications (4) ] . In placebo-controlled trials in adult patients, ALT greater than three times the ULN occurred in 61/1045 (5.8%) and 62/1002 (6.2%) of patients receiving teriflunomide tablets 7 mg and 14 mg, respectively, and 38/997 (3.8%) of patients receiving placebo, during the treatment period. […]
Reported side effects
The following serious adverse reactions are described elsewhere in the prescribing information: • Hepatotoxicity [see Contraindications (4) and Warnings and Precautions (5.1) ] • Bone Marrow Effects/Immunosuppression Potential/Infections [see Warnings and Precautions (5.4) ] • Hypersensitivity Reactions [see Contraindications (4) and Warnings and Precautions (5.5) ] • Serious Skin Reactions [see Warnings and Precautions (5.6) ] • Drug Reaction with Eosinophilia and Systemic Symptoms [see Warnings and Precautions (5.7) ] • Peripheral Neuropathy [see Warnings and Precautions (5.8) ] • Increased Blood Pressure [see Warnings and Precautions (5.9) ] • Respiratory Effects [see Warnings and Precautions (5.10) ] • Pancreatitis in Pediatric Patients [see Warnings and Precautions (5.11) ] Most common adverse reactions (≥ 10% and ≥ 2% greater than placebo): headache, diarrhea, nausea, alopecia, increase in ALT. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Mylan at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in clinical practice. A total of 2047 patients receiving teriflunomide tablets (7 mg or 14 mg once daily) constituted the safety population in the pooled analysis of placebo-controlled studies in patients with relapsing forms of multiple sclerosis; of these, 71% were female. The average age was 37 years. Table 1 lists adverse reactions in placebo-controlled trials with rates that were at least 2% for teriflunomide tablets patients and also at least 2% above the rate in placebo patients. The most common were headache, an increase in ALT, diarrhea, alopecia, and nausea. The adverse reaction most commonly associated with discontinuation was an increase in ALT (3.3%, 2.6%, and 2.3% of all patients in the teriflunomide tablets 7 mg, teriflunomide tablets 14 mg, and placebo treatment arms, respectively). […]
Interactions with other medicines
Effect of Teriflunomide Tablets on CYP2C8 Substrates Teriflunomide is an inhibitor of CYP2C8 in vivo . In patients taking teriflunomide tablets, 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 [see Clinical Pharmacology (12.3) ] . Effect of Teriflunomide Tablets on Warfarin Coadministration of teriflunomide tablets with warfarin requires close monitoring of the international normalized ratio (INR) because teriflunomide tablets may decrease peak INR by approximately 25%. Effect of Teriflunomide Tablets on Oral Contraceptives Teriflunomide tablets may increase the systemic exposures of ethinylestradiol and levonorgestrel. Consideration should be given to the type or dose of contraceptives used in combination with teriflunomide tablets [see Clinical Pharmacology (12.3) ] . Effect of Teriflunomide Tablets on CYP1A2 Substrates Teriflunomide may be a weak inducer of CYP1A2 in vivo . In patients taking teriflunomide tablets, exposure of drugs metabolized by CYP1A2 (e.g., alosetron, duloxetine, theophylline, tizanidine) may be reduced. Monitor these patients and adjust the dose of the concomitant drug(s) metabolized by CYP1A2 as required [see Clinical Pharmacology (12.3) ] . Effect of Teriflunomide Tablets on Organic Anion Transporter 3 (OAT3) Substrates Teriflunomide inhibits the activity of OAT3 in vivo . In patients taking teriflunomide tablets, exposure of drugs which are OAT3 substrates (e.g., cefaclor, cimetidine, ciprofloxacin, penicillin G, ketoprofen, furosemide, methotrexate, zidovudine) may be increased. Monitor these patients and adjust the dose of the concomitant drug(s) which are OAT3 substrates as required [see Clinical Pharmacology (12.3) ] . Effect of Teriflunomide Tablets on BCRP and Organic Anion Transporting Polypeptide B1 and B3 (OATP1B1/1B3) Substrates Teriflunomide inhibits the activity of BCRP and OATP1B1/1B3 in vivo . For a patient taking teriflunomide tablets, the dose of rosuvastatin should not exceed 10 mg once daily. […]
Use in specific groups
8.1 Pregnancy Risk Summary Teriflunomide tablets are 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 [see Contraindications (4) and Warnings and Precautions (5.2) ] . In animal reproduction studies in rat and rabbit, oral administration of teriflunomide during organogenesis caused teratogenicity and embryolethality at plasma exposures (AUC) lower than that at the maximum recommended human dose (MRHD) of 14 mg/day [see Data ]. Available human data from pregnancy registries, clinical trials, pharmacovigilance cases, and published literature are too limited to draw any conclusions, but they do not clearly indicate increased birth defects or miscarriage associated with inadvertent teriflunomide exposure in the early first trimester when followed by an accelerated elimination procedure [see Clinical Considerations and Data ] . There are no human data pertaining to exposures later in the first trimester or beyond. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2%-4% and 15%-20%, respectively. The background risk of major birth defects and miscarriage in the indicated population is unknown. Clinical Considerations Fetal/Neonatal Adverse Reactions Lowering the plasma concentration of teriflunomide by instituting an accelerated drug elimination procedure as soon as pregnancy is detected may decrease the risk to the fetus from teriflunomide tablets. The accelerated drug elimination procedure includes verification that the plasma teriflunomide concentration is less than 0.02 mg/L [see Warnings and Precautions (5.3) and Clinical Pharmacology (12.3) ] . Data Human Data Available human data are limited. […]
If too much is taken
There is no experience regarding teriflunomide overdose or intoxication in humans. Teriflunomide 70 mg daily up to 14 days was well tolerated by healthy subjects. In the event of clinically significant overdose or toxicity, cholestyramine or activated charcoal is recommended to accelerate elimination [see Warnings and Precautions (5.3) ] .
Before you take anything new
Tell your pharmacist or doctor about every medicine you take — including ones bought without a prescription, herbal products and supplements. Interactions are one of the most common avoidable causes of harm from medicines, and a pharmacist can check your full list in a couple of minutes.
This page is built from the openFDA record of the U.S. Food and Drug Administration's approved labelling for this product, effective 24 August 2022. Label text has been shortened and reformatted for readability; safety wording has not been altered in meaning. FDA labelling describes products approved in the United States — brand names, strengths, formulations and approved uses may differ in your country. Always read the leaflet that comes with your own pack. PocketsInfo is not affiliated with, and is not endorsed by, the FDA. Retrieved 2026-07-30.