Teriflunomide

What it is and how it works

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.

Mechanism class: Dihydroorotate Dehydrogenase Inhibitors

Indications

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.

Dosage and administration (summary)

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 . • 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 .

Contraindications

Teriflunomide tablets are contraindicated in/with: • Patients with severe hepatic impairment . • Pregnant women and females of reproductive potential not using effective contraception. Teriflunomide tablets may cause fetal harm . • 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 . • Coadministration with leflunomide .

Warnings and precautions

• Elimination of teriflunomide tablets can be accelerated by administration of cholestyramine or activated charcoal for 11 days. • 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.

Pregnancy

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 .

Storage and supply

Teriflunomide Tablets are available containing 7 mg or 14 mg of teriflunomide. The 7 mg tablets are light blue, film-coated, round, unscored tablets debossed with A on one side and 7 on the other side.

Source: Teriflunomide (Teriflunomide) — US FDA prescribing information, 2022-08-24, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.