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Research Article Free access | 10.1172/JCI108308

7-Hydroxymethotrexate as a urinary metabolite in human subjects and rhesus monkeys receiving high dose methotrexate.

S A Jacobs, R G Stoller, B A Chabner, and D G Johns

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Published February 1, 1976 - More info

Published in Volume 57, Issue 2 on February 1, 1976
J Clin Invest. 1976;57(2):534–538. https://doi.org/10.1172/JCI108308.
© 1976 The American Society for Clinical Investigation
Published February 1, 1976 - Version history
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Abstract

Human subjects and rhesus monkeys receiving the antitumor agent methotrexate at the high dose levels recently introduced into clinical use (greater than 50 mg/kg) excrete significant amounts of the metabolite 7-hydroxymethotrexate. The metabolite is not detected in these species after methotrexate therapy at conventional dose levels. The evidence indicates that in primates, the in vivo conversion of methotrexate to 7-hydroxymethotrexate is a dose-dependent phenomenon, with the enzyme system(s) catalyzing the reaction having a low affinity for the drug.

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