Investigational New Drugs

, Volume 18, Issue 4, pp 383–390 | Cite as

Clinical Development of Eniluracil/Fluorouracil: an Oral Treatment for Patients with Solid Tumors

  • Jeremey Levin
  • John Hohneker


Eniluracil (776C85, GW776) inactivatesdihydropyrimidine dehydrogenase (DPD), the principal enzyme of5-fluorouracil (5-FU) catabolism. Inactivation of DPD eliminatesa potential mechanism for tumor 5-FU resistance and permitsachievement of reliable and predictable pharmacokincticsfollowing oral 5-FU administration. Eniluracil/5-FU hasdemonstrated efficacy as monotherapy in patients with a varietyof solid tumors when given on a 5 or 28-day dosing schedule. Theprimary and dose-limiting toxicity is myelosuppresion with the5-day schedule and diarrhea with the 28-day schedule. Thefrequency of hand-foot syndrome is minimal with either schedule.Phase III pivotal registration-directed studies witheniluracil/5-FU given by the 28-day schedule are ongoing orplanned for the near future in patients with advanced colorectal,breast and pancreatic cancer.

dehydrogenase dihydropyrimidine oral therapy eniluracil 5-fluorouracil 776C85 


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Copyright information

© Kluwer Academic Publishers 2000

Authors and Affiliations

  • Jeremey Levin
    • 1
  • John Hohneker
    • 1
  1. 1.Glaxo Wellcome, Inc.USA

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