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5-Methyltetrahydrohomofolate.

P J O'Dwyer1, B H Wagner, D F Hoth

  • 1Investigational Drug Branch, National Cancer Institute, Philadelphia.

Investigational New Drugs
|January 1, 1987
PubMed
Summary
This summary is machine-generated.

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5-methyltetrahydrohomofolate, an antifolate developed to combat methotrexate resistance, has accumulated preclinical and clinical data. However, newer antifolates show greater promise for the initial therapeutic goals.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Development

Background:

  • 5-methyltetrahydrohomofolate was synthesized in the 1970s.
  • It was designed as an antifolate agent to address methotrexate resistance in cancer therapy.

Purpose of the Study:

  • To review and synthesize existing preclinical and clinical data for 5-methyltetrahydrohomofolate.
  • To evaluate the drug's efficacy and potential in overcoming antifolate resistance.

Main Methods:

  • Comprehensive literature search for preclinical studies.
  • Review of clinical trial data and case reports.
  • Comparative analysis of 5-methyltetrahydrohomofolate with other antifolate agents.

Main Results:

  • Preclinical data demonstrated antifolate activity.

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  • Clinical data showed limited success in overcoming established resistance mechanisms.
  • The drug's profile did not significantly outperform existing therapies.

    • Conclusions:

    • While 5-methyltetrahydrohomofolate was a novel approach, its clinical utility is limited.
    • More recent and better-characterized antifolates present superior therapeutic potential.
    • The initial goals for introducing this drug are better met by contemporary agents.