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Methotrexate polyglutamates

Zhilin Yang1,2, Jiayi Mo1,2, Wenshu Li1,2

  • 1Department of Pharmacy, Beijing Tiantan Hospital, Capital Medical University, Beijing, P. R. China.

Expert Review of Clinical Pharmacology
|October 11, 2024
PubMed
Abstract

Insights

Methotrexate polyglutamates (MTXPGs) are key to methotrexate (MTX) drug activity. Understanding MTXPGs may personalize treatment and reduce adverse reactions.

Area of Science:

  • Pharmacology
  • Drug Metabolism
  • Clinical Pharmacy

Background:

  • Methotrexate polyglutamates (MTXPGs) are intracellular metabolites of methotrexate (MTX).
  • MTXPGs significantly influence MTX efficacy and toxicity.
  • The precise role of MTXPGs requires further elucidation for clinical application.

Purpose of the Study:

  • To provide a comprehensive review of MTXPGs.
  • To explore MTXPG pharmacokinetics, analytical methods, and determinants of exposure.
  • To examine the correlation between MTXPGs and MTX efficacy and toxicity.

Main Methods:

  • Comprehensive literature search of PubMed and Web of Science databases.
  • Inclusion of reviews, clinical trials, and real-world analyses.
  • Manual searches and citation reviews were also conducted.

Main Results:

  • MTXPGs are implicated in MTX efficacy and toxicity.
  • A relationship exists between MTXPG levels and therapeutic outcomes.
  • MTXPGs have potential for personalized MTX treatment strategies.

Conclusions:

  • MTXPGs warrant greater clinical attention.
  • Further research is needed to validate and refine the correlation between MTXPGs and MTX response.
  • Other MTX metabolites may also possess clinical significance.
Keywords:
Analytical methodsefficacymethotrexate polyglutamatespharmacokineticstoxicity

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