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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › IMMUNOSUPPRESSANTS › IMMUNOSUPPRESSANTS › Dihydroorotate dehydrogenase (DHODH) inhibitors
teriflunomide
L04AK02
Forms & Strengths
- Tablets: 7 mg, 14 mg
- Film-coated tablets
Adult Dosing
- Treatment of relapsing forms of multiple sclerosis: 14 mg orally once daily
- Dosage reduction may be necessary in patients with severe renal impairment
Pediatric Dosing
- Safety and efficacy not established in patients less than 18 years old
- Not recommended for use in pediatric patients due to potential risk of liver toxicity
Indications
- Treatment of relapsing forms of multiple sclerosis
- Reduction of frequency of relapses and delaying progression of physical disability
Mechanism of Action
- Inhibits mitochondrial dihydroorotate dehydrogenase (DHODH), an enzyme necessary for pyrimidine synthesis
- Reducing T cell and B cell proliferation and activation
Contraindications
- Severe hepatic impairment
- Pregnancy and lactation
- Hypersensitivity to teriflunomide or leflunomide
Adverse Reactions
- Diarrhea
- Hair loss
- Increased liver enzymes (ALT, AST)
- Nausea and vomiting
- Headache
- Neutropenia and thrombocytopenia
Drug Interactions
- Cholestyramine, activated charcoal, and bile acid sequestrants: decrease teriflunomide exposure
- Warfarin: increased risk of bleeding due to potential effects on INR
- Repaglinide: increased risk of hypoglycemia
- Rosiglitazone and pioglitazone: potential increased risk of liver injury
Curated Content: Needs Vetting Before Put to Clinical Use