Teriflunomide

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

[4] Teriflunomide is an immunomodulatory drug inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase.

[12] Teriflunomide inhibits rapidly dividing cells, including activated T cells, which are thought to drive the disease process in MS. Teriflunomide may decrease the risk of infections compared to chemotherapy-like drugs because of its more-limited effects on the immune system.

[14] The branded drug teriflunomide is the main active in vivo metabolite of the generically available leflunomide.

[15] "Regardless of the substance administered (leflunomide or teriflunomide), it is the same molecule (teriflunomide)—the one exerting the pharmacological, immunological or metabolic action in view of restoring, correcting or modifying physiological functions, and does not present, in clinical use, a new chemical entity to patients.

Teriflunomide is the only active metabolite of leflunomide , completely responsible for its therapeutic actions. It results from the reaction of isoxazole ring opening, which occurs in vivo . Teriflunomide then can interconvert between the E and Z enolic forms (and the corresponding keto-amide), the Z -enol being the most stable and therefore most predominant form. [ 16 ] [ 17 ]