Methotrexate: first-line or second-line immunomodulator?

Eur J Gastroenterol Hepatol. 2003 Mar;15(3):225-31. doi: 10.1097/01.meg.0000049994.68425.dd.


Methotrexate is established as an effective treatment for inducing remission or preventing relapse in Crohn's disease. This review discusses the mechanisms of action, pharmacokinetics and clinical trials as well as considering the comparative efficacy between thiopurines and methotrexate. Comparisons are made with the treatment of rheumatoid arthritis. Its role in ulcerative colitis and potential toxicity are addressed. At present, the role of methotrexate is in the treatment of active or relapsing Crohn's disease for patients who are refractory to, or intolerant of, azathioprine or 6-mercaptopurine.

Publication types

  • Review

MeSH terms

  • Arthritis, Rheumatoid / drug therapy
  • Colitis, Ulcerative / drug therapy*
  • Colitis, Ulcerative / metabolism
  • Crohn Disease / drug therapy*
  • Crohn Disease / metabolism
  • Humans
  • Immunosuppressive Agents / pharmacokinetics
  • Immunosuppressive Agents / therapeutic use*
  • Liver Cirrhosis / chemically induced
  • Methotrexate / pharmacokinetics
  • Methotrexate / therapeutic use*


  • Immunosuppressive Agents
  • Methotrexate