Oral fluoropyrimidines in the treatment of colorectal cancer

Eur J Cancer. 1998 Sep;34(10):1509-13. doi: 10.1016/s0959-8049(98)00226-3.

Abstract

5-Fluorouracil (5-FU) has been the mainstay of systemic therapy for colorectal cancer since its initial development 40 years ago. Efforts to improve the therapeutic index of 5-FU have included alteration of schedule and addition of biochemical modulators. An understanding of 5-FU mechanisms of action has resulted in major therapeutic advances in the past 10 years; however, a plateau has been reached in the efficacy of 5-FU, mandating a paradigm shift for those involved in colorectal cancer drug development. One direction vigorously pursued is the development of orally administered fluoropyrimidines that maintain or improve upon the effectiveness of intravenous 5-FU. In this paper the preclinical and clinical development of oral fluoropyrimidines and their modulators is reviewed, including UFT, capecitabine, ethynyluracil and S-1.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Antineoplastic Agents / administration & dosage
  • Antineoplastic Combined Chemotherapy Protocols / administration & dosage
  • Capecitabine
  • Colorectal Neoplasms / drug therapy*
  • Colorectal Neoplasms / enzymology
  • Deoxycytidine / administration & dosage
  • Deoxycytidine / analogs & derivatives
  • Dihydrouracil Dehydrogenase (NADP)
  • Drug Combinations
  • Enzyme Inhibitors / administration & dosage
  • Fluorouracil / administration & dosage*
  • Humans
  • Oxidoreductases / metabolism
  • Pyridines / administration & dosage
  • Tegafur / administration & dosage
  • Uracil / administration & dosage
  • Uracil / analogs & derivatives

Substances

  • Antineoplastic Agents
  • Drug Combinations
  • Enzyme Inhibitors
  • Pyridines
  • UFT(R) drug
  • Deoxycytidine
  • Tegafur
  • eniluracil
  • Uracil
  • Capecitabine
  • Oxidoreductases
  • Dihydrouracil Dehydrogenase (NADP)
  • Fluorouracil
  • gimeracil