REVIEW - Understanding the mechanisms of action of MTX: implications for the treatment of RA

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Bull NYU Hosp Jt Dis. 2007;65(3):168-73.

Understanding the mechanisms of action of methotrexate: implications

for the treatment of rheumatoid arthritis.

Tian H, Cronstein BN.

Division of Endocrinology, Diabetes, and Metabolism, NYU Medical

Center, New York, NY 10016, USA.

Methotrexate has been widely used for the treatment of rheumatoid

arthritis (RA). The mechanisms of action of methotrexate are complex.

Developed as a folic acid analogue, methotrexate inhibits purine and

pyrimidine synthesis, which accounts for its efficacy in the therapy

of cancer as well as for some of its toxicities. Recently, many

studies have focused on the adenosine-mediated antiinflammatory

effects of methotrexate. Certain aspects of methotrexate toxicities

are also attributed to adenosine release. A better understanding of

the mechanisms of action and toxicities of methotrexate will direct

clinicians in their treatment approach and toxicity monitoring. Toward

that objective, the latest developments in the pharmacokinetics,

mechanism of action, pharmacogenetics, and toxicity of methotrexate

are herein discussed.

PMID: 17922664

http://www.ncbi.nlm.nih.gov/pubmed/17922664

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