Teriflunomide
AUBAGIO
What it isDihydroorotate dehydrogenase inhibitor; relapsing multiple sclerosis.
Why this oneOral once daily, and it is the active metabolite of leflunomide so the safety profile is well characterized.
What limits itHepatotoxicity and teratogenicity with a half-life of months — cholestyramine washout is needed before conception. Hair thinning.
FDA-approved for
- relapsing multiple sclerosis (2012)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Relapsing forms of multiple sclerosis | Adults | 7 mg or 14 mg QD | 7 mg or 14 mg QD | 14 mg QD |
Renal No adjustment needed
Hepatic No adjustment for mild–moderate; contraindicated in severe hepatic impairment
Instructions
- Take with or without food
- Obtain transaminase & bilirubin within 6 months before start; monitor ALT at least monthly for 6 months
- Obtain CBC within 6 months before start
- Screen for latent TB before starting
- Check blood pressure before start and periodically
- If liver injury suspected or pregnancy occurs, stop drug and start accelerated elimination (cholestyramine 8 g q8h or activated charcoal 50 g q12h x 11 days)
Contraindications
- Severe hepatic impairment
- Pregnancy, or females of reproductive potential not using effective contraception (fetal harm)
- Coadministration with leflunomide
Cautions
- Hepatotoxicity — potentially life-threatening liver injury
- Bone marrow effects/immunosuppression; risk of serious/opportunistic infection and TB
- Hypersensitivity, severe skin reactions (SJS/TEN), DRESS
- Cutaneous/mucocutaneous ulcers, impaired wound healing
- Peripheral neuropathy
- Increased blood pressure
- Interstitial lung disease
- Pancreatitis (higher frequency in pediatric patients)
Adverse reactions
- Headache
- Diarrhea
- Nausea
- Alopecia
- ALT increase
Pregnancy Contraindicated — teratogenic and embryolethal in animals at exposures at/below human; exclude pregnancy and use effective contraception; accelerated elimination if pregnancy occurs
Lactation Do not breastfeed during treatment
⚠ BOXED WARNINGS
- Hepatotoxicity
- Embryo-fetal toxicity
Cost, est. cash$100–$5,000/month
Generic entry2018
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
Mechanism of action: Teriflunomide ballicule
