Teriflunomide

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.

• 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.ICD-10: G35

• 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.contraindicated

The recommended dose of teriflunomide tablets is 7 mg or 14 mg orally once daily. Teriflunomide tablets can be taken with or without food. Monitoring to Assess Safety: • Obtain transaminase and bilirubin levels within 6 months before initiation of teriflunomide tablets therapy. Monitor ALT levels at least monthly for six months after starting teriflunomide tablets [see Warnings and Precautions (5.1) ] . • Obtain a complete blood cell count (CBC) within 6 months before the initiation of treatment with teriflunomide tablets. Further monitoring should be based on signs and symptoms of infection [see Warnings and Precautions (5.4) ] . • Prior to initiating teriflunomide tablets, screen patients for latent tuberculosis infection with a tuberculin skin test or blood test for mycobacterium tuberculosis infection [see Warnings and Precautions (5.4) ] . • Exclude pregnancy prior to initiation of treatment with teriflunomide tablets in females of reproductive potential [see Warnings and Precautions (5.2) ] . • Check blood pressure before start of teriflunomide tablets treatment and periodically thereafter [see Warnings and Precautions (5.9) ] . 7 mg or 14 mg orally once daily, with or without food. ( 2 )

• 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.

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.

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.

Metabolism

Teriflunomide is the principal active metabolite of leflunomide and is responsible for leflunomide’s activity in vivo . At recommended doses, teriflunomide and leflunomide result in a similar range of plasma concentrations of teriflunomide.

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) ] .

• Sep 12, 2012NDANDA202992Sanofi Aventis Us
• Sep 4, 2018ANDAANDA209700Teva Pharms Usa
• Oct 26, 2018ANDAANDA209638Aurobindo Pharma
• Nov 15, 2018ANDAANDA209663Glenmark Speclt
• Nov 30, 2018ANDAANDA209668Zydus Pharms
• Jan 7, 2019ANDAANDA209690Accord Hlthcare
• Apr 19, 2019ANDAANDA209572Alembic
• Apr 24, 2019ANDAANDA209623Msn

1. 1Alopecia6,06914%
2. 2Multiple Sclerosis Relapse5,22512%
3. 3Fatigue4,75911%
4. 4Diarrhoea4,75211%
5. 5Fall3,3377.4%
6. 6Hypoaesthesia3,1707.1%
7. 7Headache2,9986.7%
8. 8Drug Ineffective2,8196.3%
9. 9Paraesthesia2,8136.3%
10. 10Nausea2,7436.1%
11. 11Gait Disturbance2,4875.5%
12. 12Pain2,2315.0%
13. 13Multiple Sclerosis2,2174.9%
14. 14Condition Aggravated2,0144.5%
15. 15Depression1,7904.0%

The 10 most recently updated of 89 ClinicalTrials.gov registrations naming Teriflunomide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A NIS Evaluating Various Injectable and Oral Treatments in Patients With Relapsing Multiple Sclerosis
  Recruiting · Observational · 800 enrolled · Novartis Pharmaceuticals
  NCT05344469updated 2026-06-01
• Efficacy and Safety of Remibrutinib Compared to Teriflunomide in Participants With Relapsing Multiple Sclerosis (RMS)
  Active not recruiting · Phase 3 · Interventional · 1,007 enrolled · Novartis Pharmaceuticals
  NCT05156281updated 2026-05-29
• Efficacy and Safety of Remibrutinib Compared to Teriflunomide in Participants With Relapsing Multiple Sclerosis (RMS)
  Active not recruiting · Phase 3 · Interventional · 1,000 enrolled · Novartis Pharmaceuticals
  NCT05147220updated 2026-05-29
• A Non-interventional Study Evaluating Clinical Utility and Implications on Improved Patient Management of Serum Neurofilament as a Prognostic Marker for Disease Activity in Patients With Relapsing Multiple Sclerosis
  Recruiting · Observational · 700 enrolled · Novartis Pharmaceuticals
  NCT06551519updated 2026-05-22
• Cognition and MRI Markers in MS Patients With Aubagio® Treatment
  Completed · Interventional · 75 enrolled · University Hospital, Bordeaux
  NCT03768648updated 2026-05-20
• A Study to Evaluate the Efficacy and Safety of Fenebrutinib Compared With Teriflunomide in Relapsing Multiple Sclerosis (RMS)
  Active not recruiting · Phase 3 · Interventional · 746 enrolled · Hoffmann-La Roche
  NCT04586010updated 2026-05-19
• Efficacy and Safety Studies of Frexalimab (SAR441344) in Adults With Relapsing Forms of Multiple Sclerosis
  Active not recruiting · Phase 3 · Interventional · 1,655 enrolled · Sanofi
  NCT06141473updated 2026-05-14
• Leflunomide in Previously Treated Metastatic Triple Negative Cancers
  Completed · Phase 1 · Phase 2 · Interventional · 17 enrolled · Joseph Sparano
  NCT03709446updated 2026-03-19
• Study to Evaluate the Efficacy and Safety of Fenebrutinib Compared With Teriflunomide in Relapsing Multiple Sclerosis (RMS)
  Active not recruiting · Phase 3 · Interventional · 751 enrolled · Hoffmann-La Roche
  NCT04586023updated 2026-03-16
• Teriflunomide in HTLV-1 Associated Myelopathy/Tropical Spastic Paraparesis
  Recruiting · Phase 1 · Phase 2 · Interventional · 24 enrolled · National Institute of Neurological Disorders and Stroke (NINDS)
  NCT04799288updated 2026-03-11

Frequently asked questions

How does Teriflunomide work?

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.

What is Teriflunomide used for?

According to FDA labeling, Teriflunomide carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Teriflunomide?

Teriflunomide is classified as Dihydroorotate dehydrogenase (DHODH) inhibitors, Pyrimidine Synthesis Inhibitor, Dihydroorotate Dehydrogenase Inhibitors.

What are the brand names for Teriflunomide?

Teriflunomide is marketed under brand names including Aubagio.

What are the contraindications for Teriflunomide?

Teriflunomide labeling lists contraindications including: 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.. Always consult the full prescribing information and a clinician.