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Related Experiment Videos

[5'-DFUR (doxifluridine)].

T Taguchi

    Gan to Kagaku Ryoho. Cancer & Chemotherapy
    |July 1, 1987
    PubMed
    Summary
    This summary is machine-generated.

    5'-DFUR demonstrates potent antitumor activity, particularly in breast cancer, by selectively converting to 5-FU within tumor tissues. This targeted activation results in high efficacy with manageable side effects, making it a promising chemotherapy agent.

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    Area of Science:

    • Pharmacology
    • Oncology
    • Biochemistry

    Context:

    • 5 '-DFUR is a prodrug converted to 5-fluorouracil (5-FU) by pyrimidine nucleoside phosphorylase.
    • Pyrimidine nucleoside phosphorylase activity is elevated in tumor tissues compared to normal tissues.
    • This differential enzyme activity leads to selective drug accumulation and activation within tumors.

    Purpose:

    • To evaluate the antitumor activity and safety profile of 5 '-DFUR.
    • To assess the tumor-selective toxicity mechanism of 5 '-DFUR.
    • To explore the clinical efficacy of 5 '-DFUR in various cancers, including breast, gastric, and colorectal.

    Summary:

    • 5 '-DFUR exhibits significant antitumor effects in preclinical models with reduced toxicity and immunosuppression.
    • Clinical studies show efficacy in gastric, colorectal, and particularly breast cancer, with complete responses observed.

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  • The drug is activated preferentially in tumor cells, leading to high intratumoral 5-FU concentrations and tumor-selective toxicity.
  • Adverse events, primarily manageable diarrhea, were mild, with minimal bone marrow and CNS toxicity.

    • Impact:

    • 5 '-DFUR represents a promising therapeutic agent with a favorable efficacy and safety profile for cancer treatment.
    • Its tumor-selective activation mechanism offers a potential advantage over conventional chemotherapies.
    • 5 '-DFUR shows potential as a combination therapy agent and for surgical adjuvant chemotherapy, especially in breast cancer.