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Pharmacology

Authoring team

  • isoxazol derivative - a prodrug of A771726 (a malononitrilamide)

  • the principle action of A771726 seems to be via the inhibition of dihydroorotate dehydrogenase - this is a mitochondrial enzyme that is essential for the de-novo synthesis of pyrimidines

  • A771726 prevents proliferation and arrests the replication of activated T-lymphocytes

  • 80% of leflunomide is absorbed - conversion to A771726 occurs in the gut and the liver

  • plasma concentration peaks at around 1-24 hours

  • the half-life of A771726 is long (15-18 days)

Reference:

  • 1) Drug and Therapeutics Bulletin (2000), 38 (7), 52-4.

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