Pyrimidine synthesis inhibitor Pregnancy: Contraindicated in pregnancy and in breast-feeding (§4.3). Teriflunomide may cause serious birth defects; there are limited data in pregnant women and animal studies have shown reproductive toxicity. Pregnancy must be excluded before starting treatment. Women of childbearing potential must use effective contraception during treatment and afterwards for as long as plasma concentration is above 0.02 mg/l. Women wishing to become pregnant should stop the medicine and undergo the accelerated elimination procedure; plasma concentration should be confirmed below 0.02 mg/l on two occasions at least 14 days apart.

Teriflunomide

Brand names: Aubagio

Teriflunomide is an oral disease-modifying agent for relapsing-remitting multiple sclerosis.

Auto-extracted from the source labelling — not yet independently clinician-verified. These values were distilled from the UK SPC (or the US label where noted) but have not had a clinician sign-off. Confirm against the current SmPC before prescribing.

Adult dose

Dose: 14 mg once daily

Route: Oral — film-coated tablets swallowed whole with some water; can be taken with or without food

Frequency: Once daily

Treatment should be initiated and supervised by a physician experienced in the management of multiple sclerosis. Paediatric population (10 years and older): the recommended dose depends on body weight — body weight >40 kg: 14 mg once daily; body weight ≤40 kg: 7 mg once daily; paediatric patients who reach a stable body weight above 40 kg should be switched to 14 mg once daily. Safety and efficacy in children below 10 years have not been established (no data available). Elderly: use with caution in patients aged 65 years and over due to insufficient data on safety and efficacy. Hepatic impairment: no dose adjustment for mild or moderate impairment; contraindicated in severe hepatic impairment. Monitoring — before treatment assess blood pressure, ALT/SGPT and a complete blood cell count including differential white cell and platelet count; during treatment check blood pressure periodically and assess liver enzymes every two weeks during the first 6 months and at least every 8 weeks thereafter for at least 2 years from initiation (weekly monitoring for ALT elevations between 2- and 3-fold the upper limit of normal); discontinue if elevated liver enzymes greater than 3-fold ULN are confirmed. Accelerated elimination procedure: teriflunomide is eliminated slowly — without an accelerated elimination procedure it takes on average 8 months (up to 2 years) to reach plasma concentrations below 0.02 mg/l; cholestyramine 8 g three times daily for 11 days (or cholestyramine 4 g three times a day if 8 g is not tolerated), or alternatively 50 g of activated powdered charcoal, may be used at any time after discontinuation (§4.4/§4.6).

Dose adjustments

Renal

No dose adjustment is necessary for mild, moderate or severe renal impairment not undergoing dialysis. Patients with severe renal impairment undergoing dialysis were not evaluated and teriflunomide is contraindicated in this population.

Dose auto-extracted from UK Summary of Product Characteristics (SPC) via the eMC; US FDA prescribing information (openFDA / DailyMed) — cross-check; US labelling may differ from UK — not yet clinician-verified. Always confirm against the product SmPC and your local formulary before prescribing.

Contraindications

Hypersensitivity to the active substance or to any of the excipients
Severe hepatic impairment (Child-Pugh class C)
Pregnant women, or women of childbearing potential not using reliable contraception during treatment and thereafter as long as plasma levels are above 0.02 mg/l; pregnancy must be excluded before starting treatment
Breast-feeding women
Severe immunodeficiency states, e.g. acquired immunodeficiency syndrome (AIDS)
Significantly impaired bone marrow function, or significant anaemia, leukopenia, neutropenia or thrombocytopenia
Severe active infection until resolution
Severe renal impairment undergoing dialysis (insufficient clinical experience)
Severe hypoproteinaemia, e.g. in nephrotic syndrome

Side effects

Headache (17.8% at 7 mg, 15.7% at 14 mg) — very common
Diarrhoea (13.1%, 13.6%) and nausea (8%, 10.7%) — very common/common
Alanine aminotransferase (ALT) increase (13%, 15%) — very common
Alopecia (9.8%, 13.5%)
Hypertension; neutropenia and anaemia; infections including influenza and upper respiratory tract infection (severe infections including sepsis reported)

Interactions

Cholestyramine and activated powdered charcoal markedly accelerate teriflunomide elimination — used deliberately in the accelerated elimination procedure (§4.4/§4.6)
Other potentially hepatotoxic medicinal products, pre-existing liver disorder and consumption of substantial quantities of alcohol — higher risk of liver enzyme increases and drug-induced liver injury; consider additional monitoring (§4.4)
CYP2C8 substrates (e.g. paclitaxel, pioglitazone, repaglinide, rosiglitazone) — exposure may be increased; monitor and adjust the dose of the concomitant drug as required (US label §7)
Warfarin — teriflunomide may decrease peak INR by approximately 25%; close INR monitoring required (US label §7)
Oral contraceptives — systemic exposures of ethinylestradiol and levonorgestrel may be increased; consider the type or dose of contraceptive used (US label §7)
CYP1A2 substrates (e.g. alosetron, duloxetine, theophylline, tizanidine) — exposure may be reduced; monitor and adjust as required (US label §7)
Leflunomide — coadministration is contraindicated in the US labelling (US label §4)

Clinical monograph

How it works

It inhibits dihydro-orotate dehydrogenase, reducing de novo pyrimidine synthesis in rapidly dividing lymphocytes and thereby limiting the proliferation of activated T and B cells involved in the autoimmune attack on myelin.

Prescribing in practice

It is teratogenic and contraindicated in pregnancy; effective contraception is essential and, because of prolonged retention, an accelerated elimination procedure is used before conception or if serious toxicity occurs.
It can cause hepatotoxicity, so liver function should be checked before and during treatment.
Hypertension, hair thinning and diarrhoea are recognised effects.

Monitoring

Monitor liver transaminases, full blood count and blood pressure before and periodically during treatment, and screen for latent tuberculosis beforehand.

Counselling the patient

Use reliable contraception throughout treatment and tell your clinician at once if you might be pregnant.
Report yellowing of the skin or eyes, dark urine or persistent nausea, as these may signal a liver problem.

Evidence & guidelines

Efficacy in relapsing MS was established in the TEMSO and TOWER randomised controlled trials, and its use is consistent with NICE guidance.

Reference: NICE TA303; SmPC; Drug verified in RxNorm (NLM); confirm dosing against the manufacturer SPC (eMC). Verify against your local formulary and current prescribing references before prescribing. The structured dose values shown have been reviewed by a clinician. Monograph status: clinician-reviewed (2026-07-04).

Curated clinical cross-links plus same-class fallbacks.

Calculators

Pathways