Gastroenterologia Japonica

, Volume 17, Issue 4, pp 295–300 | Cite as

Studies on the designing of chemotherapy for gastric cancer in man, based on the tumor tissue concentration of anticancer agents

  • Shoji Suga
  • Kiyoji Kimura
  • Yasuhisa Yokoyama
  • Kichiro Isobe
  • Yuichi Yoshida
  • Toru Takada
  • Akihiko Sato
  • Toshimasa Kuwabara
  • Hiroaki Iwase
Original Articles


5-fluorouracil analogs investigated in this study include a combination of uracil and Ftorafur (UFT), Ethyl (±)-t-butoxy-5 -fluoro-hexahydro-2,4-dioxopyrimidine r-5-carboxylate (TAC-278), and 5′-deoxy-5-fluorouridine (5′-DFUR). In a total of 45 patients with gastric cancer, tumor tissue level of 5-fluorouracil (5-FU) was determined at 2, 4, 6, 8, and 12 hours following the oral administration of drug, using a resected stomach specimen as material. As a result, it was demonstrated that oral administration of 200 mg/m2 of UFT maintained above 0.05jΜg/g (minimum inhibitory concentration: MIC) of 5-FU in tumor tissues over 12 hours in 11 of 13 patients. On the contrary, 133 mg/m2 of TAC-278, and 200mg/m2 or 300mg/m2 of 5′-DFUR (which is activated by thymidine phosphorylase in man) did not produce an effective 5-FU concentration in tumor tissues. Serum 5-FU level was high in order of TAC-278, UFT, and 5′-DFUR. Clinical response rates obtained with UFT (200mg/m2 twice a day), or TAC-278 (133–200mg/m2, 3 times daily) were 27.5% (49 of 178 cases), and 8.3% (3 of 36 cases, by Koyama et al.), respectively. Fisher’s direct probability test revealed that there was a significant difference (p<0.05) between them in the response rate. It was considered that the measurement of concentration of anticancer drugs in tumor tissues might provide us useful information for the designing of chemotherapy of gastric cancer.

Key Words

UFT TAC-278 5′-DFUR tumor tissue level of 5-FU 


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Copyright information

© The Japanese Society of Gastroenterology 1982

Authors and Affiliations

  • Shoji Suga
    • 1
  • Kiyoji Kimura
    • 1
  • Yasuhisa Yokoyama
    • 2
  • Kichiro Isobe
    • 1
  • Yuichi Yoshida
    • 1
  • Toru Takada
    • 1
  • Akihiko Sato
    • 1
  • Toshimasa Kuwabara
    • 1
  • Hiroaki Iwase
    • 1
  1. 1.National Nagoya HospitalNagoyaJapan
  2. 2.Yokoyama Gastrointestinal HospitalNagoyaJapan

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