The clinical pharmacology of methotrexate: new applications of an old drug

Cancer. 1978 Jan;41(1):36-51. doi: 10.1002/1097-0142(197801)41:1<36::aid-cncr2820410108>;2-i.


Methotrexate is now used widely for the treatment of acute leukemia, non-Hodgkin's lymphoma, osteogenic sarcoma, choriocarcinoma, breast carcinoma, pulmonary and epidermoid carcinoma, and intrathecal chemotherapy. It is also useful in bone marrow transplantation, severe psoriasis, rheumatoid arthritis, dermatomyositis, Wegener's granulomatosis and sarcoidosis. The recent dramatic intensification of methotrexate therapy can be attributed in part to advances in our understanding of the clinical pharmacology of the folate antagonists, as well as to the combination of positive results and their effective dissemination to medical oncologists. The review summarizes the pharmacologic findings and illustrates how they are currently being applied to the treatment of malignant disease.

Publication types

  • Historical Article
  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Absorption
  • Bone Marrow / drug effects
  • Cell Cycle / drug effects
  • Drug Interactions
  • Drug Resistance
  • Folic Acid Antagonists
  • History, 20th Century
  • Humans
  • Injections, Intravenous
  • Injections, Spinal
  • Leucovorin / therapeutic use
  • Methotrexate / history
  • Methotrexate / metabolism
  • Methotrexate / pharmacology*
  • Neoplasms / drug therapy*
  • Nervous System / drug effects
  • Research Design
  • Tissue Distribution
  • United States


  • Folic Acid Antagonists
  • Leucovorin
  • Methotrexate