Improving Fluorouracil Chemotherapy with Novel Orally Administered Fluoropyrimidines

作者: Robert B. Diasio

DOI: 10.2165/00003495-199958003-00016

关键词:

摘要: During the 40 years since initial synthesis of fluorouracil, there have been many attempts to improve fluoropyrimidine chemotherapy. These included utilisation different schedules fluorouracil administration, modulation metabolism with other drugs increase its therapeutic benefit, and prodrugs that are potentially more effective less toxic. Of particular interest at present is clinical evaluation several new can be orally administered. include capecitabine, tegafur/uracil (UFT®), eniluracil (GW-776C85; 5-ethynyluracil), S-1, emitefur (BOF-A2). The pharmacological principles influenced development these initially presented. This followed by a review our current knowledge pharmacology each agents, focusing on antitumour activity toxicity from studies conducted in US. Studies tegafur/uracil, early indicate least similar protracted infusion but additional quality-of-life economic benefits.

参考文章(31)
Robert B. Diasio, Glen D. Heggie, Jean-Pierre Sommadossi, David S. Cross, William J. Huster, Clinical Pharmacokinetics of 5-Fluorouracil and Its Metabolites in Plasma, Urine, and Bile Cancer Research. ,vol. 47, pp. 2203- 2206 ,(1987)
Sungman Cha, M. H. El Kouni, F. N. M. Naguib, Enzymes of Uracil Catabolism in Normal and Neoplastic Human Tissues Cancer Research. ,vol. 45, pp. 5405- 5412 ,(1985)
Steven A. Rosenberg, Vincent T. DeVita, Samuel Hellman, Cancer : Principles and Practice of Oncology ,(1982)
Z.H. Lu, R Zhang, R.B. Diasio, Purification and characterization of dihydropyrimidine dehydrogenase from human liver Journal of Biological Chemistry. ,vol. 267, pp. 17102- 17109 ,(1992) , 10.1016/S0021-9258(18)41899-6
Norio Unemi, Teiji Takechi, Setsuo Takeda, Hitoshi Saito, Akio Fujioka, Masakazu Fukushima, Hiroyasu Satake, Tetsuhiko Shirasaka, Kiyomi Oyama, Hiroyuki Okabe, Junji Uchida, Koushi Nakano, 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 Cancer Research. ,vol. 56, pp. 2602- 2606 ,(1996)
M Mackean, A Planting, C Twelves, J Schellens, D Allman, B Osterwalder, B Reigner, T Griffin, S Kaye, J Verweij, Phase I and pharmacologic study of intermittent twice-daily oral therapy with capecitabine in patients with advanced and/or metastatic cancer. Journal of Clinical Oncology. ,vol. 16, pp. 2977- 2985 ,(1998) , 10.1200/JCO.1998.16.9.2977