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The oral fluorinated pyrimidines.

J S de Bono¹, C J Twelves

¹Cancer Research Campaign Department of Medical Oncology, Beatson Oncology Centre, Western Infirmary, Glasgow, UK. jdebono@saci.org

Investigational New Drugs

|April 9, 2001

Summary

New oral fluoropyrimidines offer improved cancer treatment options. These agents overcome the limitations of intravenous 5-fluorouracil (5FU) by enhancing oral bioavailability and patient convenience.

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Area of Science:

Oncology
Pharmacology
Drug Development

Background:

5-fluorouracil (5FU) has been a cornerstone in cancer chemotherapy.
Intravenous 5FU administration, while effective, presents challenges like cost, inconvenience, and complications.
Improved understanding of 5FU's pharmacology has driven advancements in fluoropyrimidine therapy.

Purpose of the Study:

To discuss the development and characteristics of novel oral fluoropyrimidine agents.
To highlight strategies overcoming the limitations of traditional 5FU administration.
To present oral fluoropyrimidines as a more convenient and potentially effective alternative.

Main Methods:

Review of two primary strategies for oral fluoropyrimidine development.
Strategy 1: Prodrugs like capecitabine, absorbed intact and converted to 5FU.
Strategy 2: Co-administration of 5FU with dihydropyrimidine dehydrogenase (DPD) inhibitors (e.g., UFT, S1).

Main Results:

Oral fluoropyrimidines have successfully addressed the bioavailability and administration issues of 5FU.
Prodrugs and 5FU/DPD inhibitor combinations offer viable oral therapeutic options.
These new agents represent significant advances in fluoropyrimidine therapy.

Conclusions:

Oral fluoropyrimidines provide a more patient-friendly and pharmaco-economical approach to cancer treatment.
The development of these agents has overcome previous barriers to oral 5FU administration.
These innovations offer improved therapeutic options for various common tumors.

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