Teriflunomide: an orally administered disease-modifying drug for the treatment of multiple sclerosis

In October 2011, FDA accepted for review Sanofi's new drug application (NDA) for oral teriflunomide as a potential therapy for patients with relapsing forms of MS.6 Teriflunomide is one of several new oral agents with the ability to improve the convenience and increase the rate of early MS trea...

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Bibliographic Details
Published inFormulary (Cleveland, Ohio) Vol. 47; no. 3; p. 97
Main Authors Wojtusik, Amanda, Feret, Brett
Format Journal Article
LanguageEnglish
Published North Olmsted Intellisphere, LLC 01.03.2012
MultiMedia Healthcare Inc
Subjects
Antimetabolites
Clinical trials
Compliance
Dehydrogenases
Drug dosages
Drug therapy
Enzymes
FDA approval
Kinases
Lymphocytes
Magnetic resonance imaging
Multiple sclerosis
Patients
Pharmaceutical industry
Pharmacokinetics
Plasma
Product development
Studies
Testing
United States
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Summary:In October 2011, FDA accepted for review Sanofi's new drug application (NDA) for oral teriflunomide as a potential therapy for patients with relapsing forms of MS.6 Teriflunomide is one of several new oral agents with the ability to improve the convenience and increase the rate of early MS treatment and overall compliance.7'8 CHEMISTRY AND PHARMACOLOGY Teriflunomide (C^sub 12^H^sub 9^F^sub 3^N^sub 2^O^sub 2^) is the active metabolite of leflunomide (Arava), an agent approved by FDA in 1998 for the treatment of rheumatoid arthritis. Leflunomide is rapidly and almost entirely converted into teriflunomide after oral ingestion, so pharmacologic and pharmacokinetic information can be adapted from what is already known.711 Teriflunomide has a wide range of anti-inflammatory, immunosuppressive, and immunomodulatory properties that range from tyrosine kinase inhibition to interleukin 1, tumor necrosis factor a, and nuclear factor kB suppression.7-10 Its therapeutic effect depends on its reversible inhibition of dihydro-orotate dehydrogenase (DHODH), the enzyme necessary for pyrimidine synthesis.7 DHODH inhibition prevents activated lymphocytes from accumulating a pyrimidine supply adequate to support DNA synthesis.
ISSN:1082-801X
1938-1166