[Methotrexate in rheumatology]

Methotrexate (MTX) is a folate inhibitor which has gained a major role in the treatment of rheumatoid arthritis (RA). MTX is not only the disease modifying anti-rheumatic drug of first choice, a large number of clinical trials moreover show that biologic drugs should be combined with MTX in order to obtain optimal therapeutic efficacy. Therefore, MTX is an anchor drug for the treatment of RA. Large studies show the general safety of the drug for long term treatment. The mechanisms of action of MTX in inflammation are complex but increasingly better understood. Current publications show that first steps have been done towards prediction of therapeutic response and toxicity of MTX by analysis of gene polymorphism. Conjugates of MTX which use endogenous albumin as a drug carrier to synovitis as well as new receptor-specific folate inhibitors are currently tested in pre-clinic investigations. The goal to further develop the most successful principle of folate inhibition for the treatment of rheumatic diseases seems to be feasible.