Cell lines

Human synoviocytes

Reaction Conditions

10^-7 ~ 10^-4 M teriflunomide for 50 h incubation

Applications

Teriflunomide inhibited the production of prostaglandin E₂ in TNF-α- or IL-1α-stimulated isolated human synoviocytes (IC50s = 7 and 3 μM, respectively). At higher concentrations (> 10 μM), teriflunomide also reduced the production of matrix metalloproteinase 1 and IL-6 due to the known inhibitory effect of teriflunomide on pyrimidine synthesis, which could be reversed by the addition of uridine.

Animal models

Male Dark Agouti (DA) rat, 6-week old

Dosage form

3 and 10 mg/kg

Once daily by oral route

Applications

Teriflunomide (3 and 10 mg/kg) delayed disease onset and decreased neurological deficits in a rat model of experimental autoimmune encephalomyelitis induced by complete Freund’s adjuvant and Mycobacterium tuberculosis.

Note

The technical data provided above is for reference only.

References:

1. Burger D, Begué-Pastor N, Benavent S, et al. The active metabolite of leflunomide, A77 1726, inhibits the production of prostaglandin E(2), matrix metalloproteinase 1 and interleukin 6 in human fibroblast-like synoviocytes. Rheumatology (Oxford), 2003, 42(1): 89-96.

2. McMonagle-Strucko K. Teriflunomide reduces behavioral, electrophysiological, and histopathological deficits in the Dark Agouti rat model of experimental autoimmune encephalomyelitis. Journal of Neurology, 2009, 256(1): 89-103.