Leflunomide: a drug with a potential beyond rheumatology

Immunotherapy. 2010 Sep;2(5):637-50. doi: 10.2217/imt.10.52.

Abstract

Leflunomide, an inhibitor of the dihydroorotase dehydrogenase and thereby pyrimidine synthesis, was introduced and licensed for the treatment of rheumatoid arthritis in 1998. In the following years, its antiviral properties were discovered and the drug was used in solid organ transplantation for polyomavirus type BK or cytomegalovirus infection. Owing to its long half-life and weak interaction with the cytochrome system, special considerations apply in the use of this drug. This article summarizes the clinical experience with leflunomide in rheumatology and in the evolving field of transplantation.

Publication types

  • Review

MeSH terms

  • Animals
  • Antirheumatic Agents / pharmacokinetics*
  • Antirheumatic Agents / pharmacology
  • Antirheumatic Agents / therapeutic use*
  • Biological Availability
  • Contraindications
  • Cytomegalovirus Infections / drug therapy*
  • Dihydroorotate Dehydrogenase
  • Female
  • Fetal Development / drug effects
  • Humans
  • Isoxazoles / pharmacokinetics*
  • Isoxazoles / pharmacology
  • Isoxazoles / therapeutic use*
  • Leflunomide
  • Monitoring, Physiologic
  • Oxidoreductases Acting on CH-CH Group Donors / antagonists & inhibitors
  • Pregnancy
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Pyrimidines / biosynthesis
  • Teratoma / chemically induced
  • Teratoma / prevention & control
  • Transplantation

Substances

  • Antirheumatic Agents
  • Dihydroorotate Dehydrogenase
  • Isoxazoles
  • Pyrimidines
  • Oxidoreductases Acting on CH-CH Group Donors
  • Protein-Tyrosine Kinases
  • Leflunomide