Aminopterin (a Folic Acid Antagonist) in the Treatment of Leukemia

Aminopterin in the Treatment of Acute Leukaemia

“…Similar but less striking results have been reported after the use of aminopterin and other antagonists by Pierce and Alt (1948), Stickney et al (1948), Dameshek (1948), Meyer et al (1949), and Wolman et al (1949. In a more recent report, Farber (1949), using aminopterin, 4 amethopterin " (4-amino-N1O-methylpteroylglutamic acid), and "amino-an-fol" (4-aminopteroylaspartic acid), has reported a 50% remission rate in 60 children with acute leukaemia treated for three months or more, including remissions of 16 and 23 months.…”

“…The first report of the use of folic acid antagonists in acute leukaemia was that of Meyer (1948), who obtained temporary clinical and haematological improvement in four of five cases treated with pteroylaspartic acid and methylpteroic acid. Subsequently, Farber et al (1948) reported important remissions in 10 out of 16 children with acute leukaemia treated with aminopterin.…”

Part VIII. Folic acid antagonists

“…Some activity of folic acid antagonists has been seen in chronic myelocytic leukemia by several authors, but the consensus is that remissions are short and inferior to those obtained with many other drugs." 59,164,165 A study of folic acid antagonists in lymphomas has recently been undertakent in an effort to see if chemotherapeutiC data from L-1210 lymphocytic neoplasm of mice""6 could serve as a useful prediction index. One can say at this time that amethopterin and dichloramethopterin have recognizable antitumor activity in lymphosarcoma and reticulum cell sarcoma.…”

Acute Leukaemia Treated with A-Methopterin

“…Clinical and haematological remissions were obtained in 50% of these patients, and in two cases were maintained for 16 and 23 months. The reported incidence of remissions in cases treated by other authors varies from 9% (Meyer et al, 1949) to 45% (Pierce and Alt, 1948). Dacie et al (1950), in a study of 13 cases treated with aminopterin, found that remissions were induced in nine.…”

“…Several of these compounds are available, all of which, though structurally related to folic acid, are biologically antagonistic (Smith et al, 1948). Meyer (1948) treated five cases of acute leukaemia with the folic acid antagonists pteroylaspartic acid and methylpteroic acid, and obtained temporary clinical and haematological remissions in four; and Farber and his colleagues (19.48) reported significant remissions in 10 out of 16 children treated with 4-aminopteroylglutamic acid (" aminopterin ").…”