Teriflunomide, sold under the brand name Aubagio.


It is the active metabolite of leflunomide.



An oral disease-modifying therapy for relapsing multiple sclerosis, inhibiting pyrimidine synthesis, reducing T-cell and B-cell activation. 



It is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase. 



It can reduce the annualized relapse rate in MS similar to interferons and glatiramer acetate, but is inferior to other oral and monoclonal antibody treatments for MS.



Teriflunomide was investigated in the Phase III clinical trial TEMSO as a medication for multiple sclerosis (MS). 



The study was completed in July 2010.[3] 2-year results were positive,  however, the subsequent TENERE head-to-head comparison trial reported that permanent discontinuations of therapy were substantially less common among MS patients who received teriflunomide compared with interferon beta-1a, relapses were more common with teriflunomide.



Pregnancy category US: N (Not classified yet)



Protein binding greater than 99.3%.



Elimination half-life 2 weeks



Excretion:  Bile duct/fecal, kidney



It  inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. 



It may decrease the risk of infections compared to chemotherapy-like drugs.



It blocks the transcription factor NF-κB, and also inhibits tyrosine kinase enzymes, but only in high doses not clinically used.



Upon administration of leflunomide, 70% of the drug administered converts into teriflunomide. 



Teriflunomide is the only active metabolite of leflunomide.




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