Antitumor activity and low intestinal toxicity of S-1, a new formulation of oral tegafur, in experimental tumor models in rats

Cancer Chemotherapy and Pharmacology

Volumn 39, Issue 3, 1996, Pages 205-211

  Takechi, Teiji ^a   Nakano, Koushi ^a   Uchida, Junji ^a   Mita, Akira ^a   Toko, Kisako ^a   Takeda, Setsuo ^a   Unemi, Norio ^a   Shirasaka, Tetsuhiko ^a  

^a TAIHO PHARMACEUTICAL CO LTD   (Japan)

Author keywords

Biochemical modulation; Intestinal toxicity; Metabolism; Rat; S 1

Indexed keywords

FLUOROPYRIMIDINE; FLUOROURACIL; OXONIC ACID; TEGAFUR; THYMIDYLATE SYNTHASE; UFT;

ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; CONTROLLED STUDY; DIARRHEA; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG METABOLISM; DRUG TUMOR LEVEL; ENZYME INHIBITION; GASTROINTESTINAL TOXICITY; LUNG CARCINOMA; MALE; NONHUMAN; OCCULT BLOOD; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RAT; RNA ANALYSIS; YOSHIDA SARCOMA;

EID: 0031060433     PISSN: 03445704     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002800050561     Document Type: Article

References (39)

1. Anderson NR, Lokich JJ (1991) Prolonged venous infusion of fluorouracil in colorectal cancer: pharmacologic rational, clinical experience and future directions. In: Abad A (ed) Medical treatment of colorectal cancer. Gaficas Mounterreina, Madrid, p 144
2. Arima S, Ohsato K, Hisaguchi T, Shimura H (1994) Multicentre randomized study of adjuvant chemotherapy with mitomycin C and tegafur or tegafur-uracil in gastric cancer. Eur J Surg 160:227
3. Barbounis VP, Kalofonos HP, Munro AJ, McKenzie CG, Sackier JM, Epenetos AA (1989) Treatment of colorectal cancer and other malignancies with continuous infusion of 5-fluorouracil. Anticancer Res 9:33
4. Caballero GA, Ausman RK, Quebbeman EJ (1985) Long-term, ambulator continuous iv infusion of 5-FU for the treatment of advanced adenocarcinoma. Cancer Treat Rep 69:13
5. Chou TC, Talalay P (1984) Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 22:27
6. Duschinsky R, Pleven E, Heidelberger C (1957) The synthesis of 5-fluoropyrimidines. J. Am Chem Soc 79:4559
7. Fujii S, Ikenaka K, Fukushima M, Shirasaka T (1978) Effect of uracil and its derivatives on antitumor activity of 5-fluorouracil and 1-(2-tetrahydrofuryl)-5-fluorouracil. Jpn J Cancer Res 69:763
8. Fujii S, Kitano S, Ikenaka K, Shirasaka T (1979) Effect of coadministration of uracil or cytosine on the antitumor activity of clinical doses of 1-(2-tetrahydrofuryl)-5-fluorouracil and level of 5-fluorouracil in rodents. Jpn J Cancer Res 70:209
9. Fujii S, Fukushima M, Shimamoto Y, Shirasaka T (1989) Pharmacokinetic modulation of plasma 5-fluorouracil concentrations to potentiate the antitumor activity of continuous venous infusion of 5-fluorouracil. Jpn J Cancer Res 80:509
10. Hansen R, Quebbeman E, Beatty P, Ritch P, Anderson T, Jenkins D, Frick J, Ausman R (1987) Continuous 5-fluorouracil infusion in refractory carcinoma of the breast. Breast Cancer Res Treat 10:145
11. Heidelberger C (1975) Fluorinated pyrimidines and their nucleosides. In: Sartorelli AC, Johns D (eds) Antineoplastic and immunosuppressive agents. Handbook of experimental pharmacology. Springer, New York, p 193
12. Heidelberger C, Danenberg PV, Moran RG (1989) Fluorinated pyrimidines and their nucleosides. Adv Enzymol Relat Areas Mol Biol 54:57
13. Huan S, Pazdur R, Singhakowinta A, Samal B, Vaitkevicius VR (1989) Low-dose continuous infusion 5-fluorouracil, evaluation in advanced breast carcinoma. Cancer 63:419
14. Ikenaka K, Shirasaka T, Kitano S, Fujii S (1979) Effect of uracil on metabolism of 5-fluorouracil in vitro. Jpn J Cancer Res 70:353
15. Kawaguchi Y, Nagayama S, Masuda H, Yasuda A (1980) Studies on the metabolism of 1-(2-tetrahydrofuryl)-5-fluorouracil and uracil coadministered orally to tumor-bearing rats. Jpn J Cancer Res 71:889
16. Kimura K, Suga S, Shimaji T, Kitamura M, Kubo K, Suzuoki Y, Isobe K (1980) Clinical basis of chemotherapy for gastric cancer with uracil and 1-(2′-tetrahydrofuryl)-5-fluorouracil. Gastroenterogia Japonica 15:324
17. Kubota Y, Hosaka M, Fukushima S, Kondo I (1993) Prophylactic oral UFT therapy of superficial bladder cancer. Cancer 71:1842
18. Lokich JJ, Ahlgren JD, Gullo JJ, Phillips JA, Fryer JG (1989) A prospective randomized comparison of continuous infusion fluorouracil with a conventional bolus schedule in metastatic colorectal carcinoma: a mid-Atlantic oncology program study. J Clin Oncol 7:425
19. MacDonald JS (1989) Cancer of the stomach. In: Devita VT Jr. et al. (eds) Cancer, principles and practice of oncology, JB Lippincott, Philadelphia, p 765
20. Maehara Y, Watanabe A, Kakeji Y, Baba H, Kohnoe S, Sugimachi K (1990) Postgastrectomy prescription of mitomycin C and UFT for patients with stage IV gastric carcinoma. Am J Surg 160:242
21. Marunaka T, Umeno Y, Yoshida K, Nagamachi M, Minami Y, Fujii S (1980) High-pressure liquid chromatographic determination of Ftorafur [1-(tetrahydro-2-furanyl)-5-fluorouracil] and GLC-mass spectrometric determination of 5-fluorouracil and uracil in biological materials after oral administration of uracil plus Ftorafur. J Pharm Sci 69:1296
22. Mitomi T, Tsuchiya S, Hiki Y, Noto T, Ogawa N (1993) A randomized controlled study on adjuvant chemotherapy with UFT in curatively resected colorectal cancer. Proc Am Soc Clin Oncol 12:690
23. Morikawa K, Walker SM, Nakajima M, Pathak S, Jessup JM, Fidler IJ (1988) Influence of organ environment on the growth, selection, and metastasis of human colon carcinoma cells in nude mice. Cancer Res 48:6863
24. Mynihan T, Hansen R, Anderson T, Quebbeman E, Beatty P, Ausman R, Ritch P, Chitamber C, Vukelich M (1988) Continuous 5-fluorouracil infusion in advanced gastric carcinoma. Am J Clin Oncol 11:461
25. Ninomiya Y, Miwa M, Eda H, Sahara H, Fujimoto K, Ishida M, Umeda I, Yokose K, Ishitsuka H (1990) Comparative antitumor activity and intestinal toxicity of 5′-deoxy-5-fluorouridine and its prodrug trimethoxybenzoyl-5′-deoxy-5-fluorouridine. Jpn J Cancer Res 81:188
26. Pinedo HH, Peters GFJ (1988) Fluorouracil: biochemistry and pharmacology. J Clin Oncol 6:1653
27. Poon MA (1989) Biochemical modulation of fluorouracil: evidence of significant improvement of survival and quality of life in patient with advanced colorectal cancer. J Clin Oncol 7:1407
28. Quebbeman E, Ausman R, Hansen R, Becker T, Caballero G, Ritch P, Jenkins D, Blake D, Tangen L, Schulte W (1985) Long-term ambulatory treatment of metastatic colorectal adenocarcinoma by continuous intravenous infusion of 5-fluorouracil. J Surg Oncol 30:60
29. Schneider WC (1946) Phosphorus compounds in animal tissues III. A comparison of methods for the estimation of nucleic acids. J Biol Chem 221:164
30. Shirasaka T, Shimamoto Y, Fukushima M (1993) Inhibition by oxonic acid of gastrointestinal toxicity of 5-fluorouracil without loss of its antitumor activity in rats. Cancer Res 53:4004
31. Spears CP, Shahinian AH, Moran RG, Heidelberger C, Corbett T (1982) In vivo kinetics of thymidylate synthetase inhibition in 5-fluorouracil-sensitive and -resistant murine colon adenocarcinomas. Cancer Res 42:450
32. Tatsumi K, Fukushima M, Shirasaka T, Fujii S (1987) Inhibitory effects of pyrimidine, barbituric acid and pyridine derivatives on 5-fluorouracil degradation in rat liver extract. Jpn J Cancer Res 78:748
33. Toide H, Akiyoshi H, Minato Y, Okuda H, Fujii S (1977) Comparative studies on the metabolism of 2-(tetrahydrofuryl)-5-fluorouracil and 5-fluorouracil. Jpn J Cancer Res 68:533
34. Uchida J, Umeno Y, Takeda S (1992) Significance of measuring 5-fluorouracil incorporated intio RNA of tumor tissue as a parameter for the antitumor activity of 5-fluorouracil and its derivatives (in Japanese with English summary). Jpn J Cancer Chemother 19:677
35. Uchida J, Takechi T, Nakano K, Takeda S, Fukushima M, Unemi N, Shirasaka T (1995) Preclinical studies of S-1, a new oral tegafur plus two modulators. Proc Am Assoc Cancer Res 36:2423
36. Wada H, Hitomi S, Teramatsu T (1994) Postoperative non-small cell lung cancer: a prospective randomized trial of cisplatin (P)-vindesine (VDS)-UFT vs. UFT alone vs. control. Proc Am Soc Clin Oncol 13:1084
37. Wade JL, Herbst S, Greenburg A (1986) Prolonged venous infusion (PVI) of 5-fluorouracil (5-FU) for metastatic colon cancer (MCC). Proc Am Soc Clin Oncol Annu Meet 5:341
38. Wadler S (1989) Fluorouracil and recombinant alpha-2a interferon: an active regimen against advanced colorectal carcinoma J Clin Oncol 7:1769
39. Wills J (1986) An EORTC Gastrointestinal Group evaluation of the combination of sequential methotrexate and 5-fluorouracil, combined with adriamycin in advanced measurable gastric cancer. J Clin Oncol 4:1799