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Review of a New Antimetabolic Agent, 1,3-Bis(Tetrahydro-2-Furanyl)-5-Fluoro-2,4-Pyrimidinedione (FD-1)

  • Tetsuo Taguchi
Part of the Recent Results in Cancer Research book series (RECENTCANCER, volume 70)

Summary

FD-1, a new anticancer drug, is a fluorinated pyrimidine derivative that has shown less acute toxicity than 5-FU and FT-207, and higher antitumor activity than FT-207 in Ehrlich carcinoma, S-180, AH-130, Yoshida sarcoma, and Walker 256. A principal feature of FD-1 is that, in comparison with FT-207, in oral administration it can maintain a higher concentration of 5-FU both in plasma and in tumor tissues. FD-1 is considered to be activated into 5-FU by a drug-metabolizing enzyme system in liver microsomes.

In the phase I study of FD-1, the maximum tolerated dose was greater than 20 mg/kg in a single administration. The dose-limiting factor in FD-1 administration is gastrointestinal toxicity that causes side effects such as nausea and vomiting. The recommended dosage for daily oral administration of FD-1 is 6–12 mg/kg/day.

In the phase I study of the sustained released form of FD-1 (FD-1-S), frequency of nausea and vomiting could be definitely reduced by the oral administration of FD-1-S, which showed higher tolerability. FD-1-S can be continuously administered at a dose ranging from 600 mg to 1200 mg/body/day for 4 weeks and can be expected to have higher efficacy. In further studies on the long-term administration of FD-1-S, CNS toxicity has been reported in some cases.

Keywords

Oral Administration Stomach Cancer Daily Oral Administration High Antitumor Activity Ehrlich Carcinoma 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

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    Kawaguchi, Y., Nakamura, Y., Sato, T., Takeda, S., Marunaka, T., Fujii, S.: Studies on the fate of 5-fluoro-1,3-bis(tetrahydro-2-furanyl)-2,4-pyrimidinedione (FD-1), a new antitumor agent. 1. Absorption, distribution, excretion and metabolism of FD-1 administered orally to rats. Yakugaku Zasshi 98, 525 (1978)PubMedGoogle Scholar
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    Unemi, N., Takeda, S., Kitasato, K., Kajihara, M.: Studies on the antitumor activity of 1,3-bis(tetrahydro-2-furanyl)-5-fluoro-2,4-pyrimidinedione (FD-1), a new antitumor agent. 1. Antitumor activity of FP-1 by the oral administration. Chemotherapy 26, 200 (1978)Google Scholar
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    Yasumoto, M., Marunaka, Y., Hashimoto, S., Harima, K., Suzue, T.: Process for producing N 1-(2-tetrahydrofuryl)-5-fluorouracil. Japanese published unexamined patent application 50–50384 (1975)Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1980

Authors and Affiliations

  • Tetsuo Taguchi
    • 1
  1. 1.Department of Oncologic Surgery, Research Institute for Microbial DiseasesOsaka UniversitySuita-shi, Osaka 565Japan

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