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Metabolic conversion of methotrexate in man
Summary
Methotrexate (MTX) is metabolized into several analogues in the body. The clinical significance of these MTX metabolites, including their role in toxicity and diagnostic assays, requires further investigation.
Area of Science:
- Pharmacology
- Drug Metabolism
- Toxicology
Background:
- Metabolism of methotrexate (MTX) to related analogues is increasingly recognized.
- Key metabolites include 7-hydroxymethotrexate, 2,4-diamino-N10-methylpteroic acid, and MTX poly-gamma-glutamates.
Purpose of the Study:
- To review the established products of methotrexate metabolism in humans.
- To discuss the potential significance of these metabolites in clinical settings.
Main Methods:
- Literature review of established methotrexate metabolites.
- Analysis of the potential roles of these metabolites in MTX-associated adverse effects.
Main Results:
- Identified 7-hydroxymethotrexate, 2,4-diamino-N10-methylpteroic acid, and methotrexate poly-gamma-glutamates as human MTX metabolites.
- Highlighted potential roles in renal failure, chronic toxicity, and radioimmunoassay interference.
Conclusions:
- The clinical significance of MTX metabolites is not fully established.
- These compounds may contribute to MTX-related renal failure and chronic toxicity.
- Metabolites can interfere with radioimmunoassay measurements of MTX concentrations.