How does teriflunomide work?

Teriflunomideis an immunomodulator that reduces the number of activated central nervous system lymphocytes, resulting in anti-inflammatory and anti-proliferative effects.

Teriflunomide(teriflunomide) is an immunomodulator with anti-inflammatory properties that 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 (ms) is unknown but may involve a reduction in the number of activated lymphocytes in the central nervous system.

Teriflunomide is the main active metabolite of leflunomide and is the source of leflunomide activity in living organisms. Teriflunomide plasma concentration ranges are similar for teriflunomide and leflunomide at recommended doses. Mediant based on population analysis of teriflunomide in healthy adult volunteers and adult MSpatients. 1/2approximately 18 and 19 days after repeated doses of 7 mg and 14 mg respectively. It takes approximately3 months respectively to reach steady-state concentrations. After repeated doses of 7 or 14 mg, the estimated AUC accumulation ratio is approximately 30. After oral administration of teriflunomide, the median time to reach maximum plasma concentrations ranges from 1 to 4 hours after dosing. Food has no clinically relevant effect on the pharmacokinetics of teriflunomide. Teriflunomide is extensively bound to plasma proteins (》99%) and is mainly distributed in plasma. The volume of distribution after a single intravenous (IV) dose is 11 L. Teriflunomide was the major circulating fraction detected in plasma. The major biotransformation pathway for the minor metabolites of teriflunomide is hydrolysis, with oxidation being a minor pathway. Secondary pathways include oxidation, N-acetylation, and sulfate conjugation. Teriflunomide is eliminated primarily by direct biliary excretion of unchanged drug and renal excretion of metabolites. Over 21 days, 60.1% of the administered dose passed through feces (37.5%) and urine (22.6%) discharge. After an accelerated elimination procedure with cholestyramine, 23.1% was recovered (mainly in feces). After a single intravenous dose, the overall internal clearance of teriflunomide was 30.5 ml/ hours. IndiaNATCOpharmaceutical retail price14mg*30 tablets800yuan. If you want to get more high-quality information, you can contact YaDE. YaDE will do its best to learn more about high-quality overseas drugs for you.

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