aminopterin

Aminopterin is a synthetic derivative of folic acid and an antimetabolite drug with antineoplastic and immunosuppressive properties. It acts as a potent antifolate by competitively inhibiting the enzyme dihydrofolate reductase (DHFR), thereby blocking the synthesis of tetrahydrofolate. This inhibition leads to depletion of nucleotide precursors required for DNA, RNA, and protein synthesis. Aminopterin was first used in 1947 to induce remission in pediatric leukemia and was later marketed for this indication from 1953 to 1964 before being supplanted by methotrexate due to manufacturing difficulties and a better therapeutic index for methotrexate. Off-label uses included treatment of psoriasis and research applications in cancer therapy and autoimmune diseases. Aminopterin has also been explored as an abortifacient but is associated with severe teratogenic effects known as fetal aminopterin syndrome[1][2][3][5][7].

Other names

4-aminofolic acidaminopterineaminopteridineaminopterin sodiumdisodium salt aminopterin