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Leflunomide

An Immunomodulatory Drug for the Treatment of Rheumatoid Arthritis

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Book cover Modern Therapeutics in Rheumatic Diseases

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Abstract

Leflunomide is a new disease-modifying anti-rheumatic drug (DMARD) that is classified as an isoxazol, and is rapidly converted from its prodrug form to its active metabolite, A77 1726, by first-pass metabolism in the gut and liver. At therapeutic doses (20 mg/d) in rheumatoid arthritis (RA) patients, A77 1726 blocks the de novo synthesis of pyrimidines by inhibiting dihydroorotate dehydrogenase (DHODH), the rate-limiting enzyme in pyrimidine production (1–4) necessary for the clonal expansion of activated T and B lymphocytes. The following overview will address the mode of action and the preclinical and clinical experience with leflunomide in the treatment of RA.

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Authors
  1. Paul Emery
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  2. David L. Scott
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  3. Vibeke Strand
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Editor information

Editors and Affiliations

  1. Uniformed Services University of the Health Sciences, Bethesda, MD, USA

    George C. Tsokos

  2. Walter Reed Army Institute of Research, Silver Spring, MD, USA

    George C. Tsokos

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© 2002 Humana Press, Inc., Totowa, NJ

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Emery, P., Scott, D.L., Strand, V. (2002). Leflunomide. In: Tsokos, G.C. (eds) Modern Therapeutics in Rheumatic Diseases. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-59259-239-5_8

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  • DOI: https://doi.org/10.1007/978-1-59259-239-5_8

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-4684-9708-3

  • Online ISBN: 978-1-59259-239-5

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