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Related Experiment Videos

Fluoropyrimidines: a critical evaluation.

R A Brito1, D Medgyesy, T H Zukowski

  • 1Division of Medicine, The University of Texas M.D. Anderson Cancer Center, Houston, Texas, USA.

Oncology
|August 7, 1999
PubMed
Summary
This summary is machine-generated.

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Capecitabine (Xeloda) offers an oral alternative to intravenous 5-fluorouracil (5-FU) for colorectal cancer treatment. This drug is converted to 5-FU, achieving higher concentrations in tumors and overcoming absorption issues related to dihydropyrimidine dehydrogenase (DPD) levels.

Area of Science:

  • Oncology
  • Pharmacology
  • Gastroenterology

Background:

  • 5-fluorouracil (5-FU) is a cornerstone chemotherapy for colorectal cancer, but its oral administration is limited by variable absorption due to dihydropyrimidine dehydrogenase (DPD) activity.
  • Developing oral fluoropyrimidine analogs that overcome DPD-related absorption variability is crucial for improving colorectal cancer treatment.

Purpose of the Study:

  • To evaluate capecitabine (Xeloda), an oral fluoropyrimidine, as a treatment for colorectal cancer.
  • To assess the efficacy and safety of capecitabine in patients with metastatic breast cancer and colorectal cancer.

Main Methods:

  • Capecitabine is designed as an orally administered prodrug that is selectively activated to 5-FU within tumor tissues.
  • Phase II clinical trials were conducted to assess response rates and time to disease progression in colorectal cancer patients.

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Main Results:

  • Capecitabine demonstrated response rates of 21-24% and a median time to disease progression of 127-230 days in Phase II colorectal cancer trials.
  • The United States Food and Drug Administration (FDA) approved capecitabine for metastatic breast cancer resistant to paclitaxel and contraindicated for anthracyclines.

Conclusions:

  • Capecitabine represents a promising oral chemotherapeutic agent for colorectal cancer, offering a potentially more convenient administration route with targeted tumor activation.
  • Further development of oral fluoropyrimidines, including capecitabine and other agents like S-1, is ongoing for colorectal cancer treatment.