methotrexate

Methotrexate is a small molecule antimetabolite and antifolate drug used to treat a variety of cancers and autoimmune diseases. It works primarily by inhibiting enzymes involved in nucleotide synthesis—most notably dihydrofolate reductase (DHFR)—which leads to suppression of DNA synthesis and cell division. This mechanism underlies its use as an antineoplastic agent in cancers such as acute lymphoblastic leukemia (ALL), non-Hodgkin's lymphoma (NHL), breast cancer, head and neck cancer, lung cancer, uterine cancer, mycosis fungoides (cutaneous T-cell lymphoma), and others. In autoimmune conditions like rheumatoid arthritis (RA), juvenile idiopathic arthritis (JIA), severe psoriasis, lupus erythematosus, inflammatory myositis, vasculitis and scleroderma it acts through additional mechanisms including inhibition of purine metabolism leading to adenosine accumulation; inhibition of T cell activation; downregulation of B cells; increased sensitivity of activated T cells to apoptosis; suppression of intercellular adhesion molecule expression by T cells; inhibition of methyltransferase activity relevant for immune function; and antagonism at the interleukin 1-beta receptor. Methotrexate was originally developed in the 1940s as an anticancer agent.

Brand names

TrexallXatmepJylamvoMetojectNordimetOtrexupRasuvoReditrex

Other names

Rheumatrex