title: Therapeutic effect of 1 M tegafur-0.4 M 5-chloro-2, 4-dihydroxypridine-1 M potassium oxonate (S-1) on head and neck squamous carcinoma cells.
abstract: 1 M Tegafur (FT)-0.4 M 5-chloro-2,4-dihydroxypridine (CHDP)-1 M potassium oxonate (Oxo) (S-1), was developed as a new oral antineoplastic agent based on biochemical modulation of fluorouracil (5-FU) by CHDP and Oxo. The antitumor effect of S-1 on human head and neck squamous carcinoma cells was evaluated in xenografts and a metastasis model, in comparison with combined drug of 1 M FT and 4 M uracil (UFT). Mice treatment with S-1 showed a significant higher concentration of 5-FU in the tumor and the serum than UFT treated mice. S-1 showed higher tumor growth inhibition and metastasis inhibition than UFT. The mice in which metastasis was inhibited lived more than twice as long as the control mice. These results suggest that S-1 will have a higher clinical therapeutic effect against advanced squamous cell carcinoma of the head and neck in humans.
authors.affiliation: Department of Otorhinolaryngology, Yokohama City University, School of Medicine, 3-9 Fukuura, Kanazawa-ku, 236-0004, Yokohama, Japan. go_c@med.yokohama-cu.ac.jp
authors.forename: G
authors.initials: G
authors.lastname: Nishimura
authors.forename: S
authors.initials: S
authors.lastname: Yanoma
authors.forename: H
authors.initials: H
authors.lastname: Mizuno
authors.forename: K
authors.initials: K
authors.lastname: Satake
authors.forename: T
authors.initials: T
authors.lastname: Taguchi
authors.forename: Y
authors.initials: Y
authors.lastname: Ikeda
authors.forename: M
authors.initials: M
authors.lastname: Tsukuda
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000627:therapeutic use*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy* / Q000401:mortality / Q000473:pathology; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D005260:Female; D005472:Fluorouracil / Q000097:blood; D006258:Head and Neck Neoplasms / Q000188:drug therapy* / Q000401:mortality / Q000473:pathology; D006801:Humans; D008175:Lung Neoplasms / Q000517:prevention & control / Q000556:secondary; D051379:Mice; D008807:Mice, Inbred BALB C; D008819:Mice, Nude; D016513:Mice, SCID; D009368:Neoplasm Transplantation; D010094:Oxonic Acid / Q000627:therapeutic use*; D011725:Pyridines / Q000627:therapeutic use*; D015996:Survival Rate; D005641:Tegafur / Q000627:therapeutic use*; D014183:Transplantation, Heterologous; D014407:Tumor Cells, Cultured; D014498:Uracil / Q000627:therapeutic use
chemical_list: D000964:Antimetabolites, Antineoplastic; D004338:Drug Combinations; D011725:Pyridines; C079198:S 1 (combination); D005641:Tegafur; D014498:Uracil; D010094:Oxonic Acid; D005472:Fluorouracil