Journal article
Preclinical development of eniluracil: Enhancing the therapeutic index and dosing convenience of 5-fluorouracil
Investigational new drugs, Vol.18(4), pp.365-371
11/01/2000
DOI: 10.1023/A:1006401432488
PMID: 11081572
Abstract
Eniluracil (5-ethynyluracil, GW 776, 776C85) is being developed as a novel modulator of 5-fluorouracil (5-FU) for the treatment of cancer. Eniluracil is an effective mechanism-based inactivator of dihydropyrimidine dehydrogenase (DPD), the first enzyme in the catabolic pathway of 5-FU. By temporarily eliminating this prevalent enzyme, eniluracil provides predictable dosing of 5-FU and enables oral administration of 5-FU to replace intravenous bolus and continuously infused dosing. New DPD is synthesized with a half-life of 2.6 days. It also eliminates the formation of problematic 5-FU catabolites. Most importantly, in laboratory animals, eniluracil increases the therapeutic index and absolute efficacy of 5-FU. Accompanying reports in this journal indicate that eniluracil has promising clinical potential.
Details
- Title: Subtitle
- Preclinical development of eniluracil: Enhancing the therapeutic index and dosing convenience of 5-fluorouracil
- Creators
- Melanie Paff - Research Triangle Park FoundationDavid P Baccanari - Glaxo Wellcome, Inc, USAStephen T Davis - Glaxo Wellcome, Inc, USAShousong Cao - Roswell Park Cancer InstituteRobert L Tansik - Roswell Park Cancer InstituteYoucef M Rustum - Hematology, Oncology, and Blood & Marrow TransplantationThomas Spector - Research Triangle Park Foundation
- Resource Type
- Journal article
- Publication Details
- Investigational new drugs, Vol.18(4), pp.365-371
- Publisher
- Springer Nature B.V
- DOI
- 10.1023/A:1006401432488
- PMID
- 11081572
- ISSN
- 0167-6997
- eISSN
- 1573-0646
- Language
- English
- Date published
- 11/01/2000
- Academic Unit
- Hematology, Oncology, and Blood & Marrow Transplantation; Internal Medicine
- Record Identifier
- 9984359683702771
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