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Development of a novel form of an oral 5-fluorouracil derivative (S-1) directed to the potentiation of the tumor selective cytotoxicity of 5-fluorouracil by two biochemical modulators.
We have focused our attention on the development of a novel form of a tegafur-based [FT; a prodrug of 5-fluorouracil (5-FU)] antitumor agent. We have used two biochemical and pharmacological… Expand
Inhibitory effects of pyrimidine, barbituric acid and pyridine derivatives on 5-fluorouracil degradation in rat liver extracts.
- K. Tatsumi, M. Fukushima, T. Shirasaka, S. Fujii
- Biology, Medicine
- Japanese journal of cancer research : Gann
- 1 July 1987
The inhibitory effects of about 30 compounds, mainly pyrimidine and pyridine derivatives, on 5-fluorouracil degradation catalyzed by dihydrouracil dehydrogenase (DHU dehydrogenase) were investigated.… Expand
Antitumor activity of 1 M tegafur-0.4 M 5-chloro-2,4-dihydroxypyridine-1 M potassium oxonate (S-1) against human colon carcinoma orthotopically implanted into nude rats.
The purpose of this study was to establish a nude rat orthotopic (organ-specific) human colorectal cancer model as an in vivo secondary screen for general evaluation of new anticancer agents against… Expand
Pharmacokinetic study of S-1, a novel oral fluorouracil antitumor drug.
- K. Hirata, N. Horikoshi, +9 authors T. Shirasaka
- Clinical cancer research : an official journal of…
- 1 August 1999
S-1 is a novel oral fluorouracil antitumor drug that combines three pharmacological agents: tegafur (FT), which is a prodrug of 5-fluorouracil (5-FU); 5-chloro-2,4-dihydroxypyridine (CDHP), which… Expand
Inhibition by oxonic acid of gastrointestinal toxicity of 5-fluorouracil without loss of its antitumor activity in rats.
The possibility of decreasing the gastrointestinal (GI) toxic effects of 5-fluorouracil (5-FU) on the digestive tract such as its injury of cells and induction of diarrhea, without reducing its… Expand
Antitumor activity and low intestinal toxicity of S-1, a new formulation of oral tegafur, in experimental tumor models in rats
- T. Takechi, K. Nakano, +5 authors T. Shirasaka
- Chemistry, Medicine
- Cancer Chemotherapy and Pharmacology
- 2 December 1996
Abstract S-1, a new oral antitumor agent, is composed of 1-(2-tetrahydrofuryl)-5-fluorouracil (Tegafur, FT), 5-chloro-2,4-dihydroxypyridine (CDHP) and potassium oxonate (Oxo) in a molar ratio of 1 :… Expand
Effect of uracil and its derivatives on antitumor activity of 5-fluorouracil and 1-(2-tetrahydrofuryl)-5-fluorouracil.
Uracil prevented the growth inhibition of Staphylococcus aureus 209P by 5fluorouracil (5-FU). However, uracil did not reverse the growth inhibition by 5-FU in mammalian FM3A/B and HeLa cells even at… Expand
Activities of various enzymes of pyrimidine nucleotide and DNA syntheses in normal and neoplastic human tissues.
The activities of the key enzymes of pyrimidine nucleotide and DNA syntheses in 43 human tumors and 28 normal human tissues were investigated. The activities of cytidine triphosphate synthetase,… Expand
Preclinical antitumor efficacy of S-1: a new oral formulation of 5-fluorouracil on human tumor xenografts.
- M. Fukushima, H. Satake, +9 authors T. Shirasaka
- International journal of oncology
- 1 October 1998
S-1 is a new oral formulation of 5-fluorouracil (5-FU) consisted of 1M tegafur, 0.4M 5-chloro-2,4-dihydroxypyridine that inhibits a degradation of 5-FU, and 1M potassium oxonate that regulates the… Expand
Development History and Concept of an Oral Anticancer Agent S-1 (TS-1®): Its Clinical Usefulness and Future Vistas
- T. Shirasaka
- Japanese journal of clinical oncology
- 12 November 2008
Dushinsky et al. left a great gift to human beings with the discovery of 5-fluorouracil (5-FU). Approximately 50 years have elapsed from that discovery to the development of S-1 (TS-1®). The concept… Expand