Catalog No.S4169 Synonyms: A77 1726, HMR-1726
Molecular Weight(MW): 270.21
Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.
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|Description||Teriflunomide is the active metabolite of leflunomide, inhibiting pyrimidine de novo synthesis by blocking the enzyme dihydroorotate dehydrogenase, used as an immunomodulatory agent.|
Teriflunomide primarily acts as an inhibitor of dihydroorotate dehydrogenase (DHODH), a key mitochondrial enzyme involved in the de novo synthesis of pyrimidines in rapidly proliferating cells. By reducing the activity of high-avidity proliferating T lymphocytes and B lymphocytes, teriflunomide likely attenuates the inflammatory response to autoantigens in MS. Thus, teriflunomide can be considered a cytostatic rather than a cytotoxic drug to leukocytes. 
|In vivo||Teriflunomide has demonstrated beneficial effects in two independent animal models of demyelinating disease. In the dark agouti rat model of experimental autoimmune encephalitis (EAE), teriflunomide administration results in clinical, histopathological, and electrophysiological evidence of efficacy both as a prophylactic and therapeutic agent. Similarly, in the female Lewis rat model of EAE, teriflunomide administration results in beneficial prophylactic and therapeutic clinical effects, with a delay in disease onset and symptom severity. |
|In vitro||DMSO||32 mg/mL (118.42 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||A77 1726, HMR-1726|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02792231||Recruiting||Relapsing Multiple Scelrosis||Novartis Pharmaceuticals|Novartis||August 26, 2016||Phase 3|
|NCT02792218||Recruiting||Relapsing Multiple Sclerosis||Novartis Pharmaceuticals|Novartis||September 2016||Phase 3|
|NCT02587195||Not yet recruiting||Multiple Sclerosis||Centre Hospitalier Universitaire de Nice||October 2015||Phase 3|
|NCT02490982||Enrolling by invitation||Relapsing Remitting Multiple Sclerosis||Centre hospitalier de lUniversité de Montréal (CHUM)|Genzyme, a Sanofi Company|Montreal Neurological Institute and Hospital||July 2015||Phase 4|
|NCT02425644||Recruiting||Multiple Sclerosis||Actelion||April 2015||Phase 3|
|NCT02263547||Terminated||Teriflunomide Elimination|Healthy Volunteers||Derrick Scott Robertson|Genzyme, a Sanofi Company|University of South Florida||January 2015||Phase 1|
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Frequently Asked Questions
I am planning to use teriflunomide (S4169) in my in vivo protocol, but I cannot get a homogeneous solution. Could you please provide me with some guidance?
This compound is an oral clinical medicine. For oral administration suspension is fine. In paper http://www.pnas.org/content/108/44/18067.full, they also prepared the stock by DMSO and then diluted into 0.9% sterile saline for animial study.