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Methotrexate Overview and Indications Methotrexate is a folate antimetabolite used to treat malignant diseases (such as breast cancer, lymphoma, and leukemia) and nonmalignant autoimmune diseases (including rheumatoid arthritis, psoriasis, and juvenile idiopathic arthritis). Because of its high potential for severe and sometimes fatal toxicities, methotrexate must only be prescribed by an experienced clinician.

Mechanism of Action The drug competitively inhibits dihydrofolate reductase, an enzyme required to convert folic acid into reduced folates. This action severely blocks DNA synthesis, repair, an ...