Aminopterin is a chemical compound primarily known for its use in medical and biochemical applications, particularly as an antineoplastic agent and in chemotherapy regimens. It acts as a folic acid antagonist, inhibiting the enzyme dihydrofolate reductase, which is crucial in DNA synthesis. This mechanism makes it effective in slowing down the growth of rapidly dividing cancer cells. However, due to its high toxicity and severe side effects, its clinical use has been largely supplanted by less toxic derivatives like methotrexate.

Application Areas

  • Cancer Treatment: Historically used in some forms of leukemia and other cancers.
  • Medical Research: Utilized in laboratory settings for cancer research and studies on cell growth.
  • Psoriasis Treatment: Previously considered for severe cases of psoriasis.
  • Rheumatoid Arthritis: Investigated for its potential in treating rheumatoid arthritis.

Well-known Examples

While aminopterin itself is not widely used today due to its toxicity, it paved the way for the development of similar compounds:

  • Methotrexate: A less toxic derivative that is widely used in treating various types of cancer, psoriasis, and rheumatoid arthritis.
  • Research Studies: Aminopterin has been used in historical cancer treatment studies, particularly in the mid-20th century.


  • High Toxicity: Its potential to cause severe side effects limits its clinical use.
  • Side Effects: Includes damage to the liver, kidney, and bone marrow, among others.
  • Developmental Effects: Known teratogenic effects, posing risks in pregnancy.

Recommendations and Industry Usage

Due to its high toxicity, aminopterin is not commonly recommended or used in current medical practice. Its role has been largely historical, serving as a stepping stone for the development of safer alternatives like methotrexate.

History and Legal Basics

Aminopterin was one of the first antifolate chemotherapy agents discovered in the 1940s. It played a significant role in the early treatment of childhood leukemia. However, its clinical use was limited by its toxicity, leading to the development and preferential use of methotrexate. Legal regulations for aminopterin are stringent, reflecting its potential risks and limited therapeutic window.

Examples of Sentences

  • Aminopterin was a precursor in the development of modern chemotherapy agents.
  • The toxic profile of aminopterin led to the search for safer alternatives.
  • Aminopterin's mechanism of action involves the inhibition of dihydrofolate reductase.
  • Research on aminopterin contributed significantly to our understanding of antifolate drugs.

Similar Things or Synonyms

  • Antifolate Agents
  • Methotrexate
  • Chemotherapy Drugs
  • Dihydrofolate Reductase Inhibitors


Aminopterin, while historically important in the development of chemotherapy, is no longer commonly used due to its high toxicity and severe side effects. Its discovery and initial use in cancer treatment were pivotal in advancing medical understanding of antifolate agents, leading to the development of safer and more effective treatments such as methotrexate. The story of aminopterin illustrates the ongoing evolution and refinement of cancer treatment modalities.


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