Effect of gastrectomy on the pharmacokinetics of S-1, an oral fluoropyrimidine, in resectable gastric cancer patients

Cancer Chemother Pharmacol. 2007 Oct;60(5):693-701. doi: 10.1007/s00280-007-0415-x. Epub 2007 Feb 15.

Abstract

Purpose: The effect of gastrectomy on pharmacokinetics after S-1 administration was investigated.

Patients and methods: A dose of 40 mg/m(2) of S-1 was administered orally twice daily for 7 days (80 mg/m(2)/day) preoperatively in ten patients with resectable gastric cancer, and the same dose of S-1 was administered for 28 consecutive days after gastrectomy. Plasma concentrations of tegafur, gimeracil, and oteracil potassium, all the components of S-1, and 5-FU were measured on pre- and postoperative days. Concentrations of 5-FU in tumor and normal tissues were also determined.

Results: At day 4 from the initial preoperative administration of S-1, the AUC of 5-FU was 1,055 +/- 304 ng h/ml. At day 18, day 28, and day 42 after gastrectomy, it was 1,012 +/- 331, 1,070 +/- 403, and 946 +/- 226 ng h/ml, respectively. No significant differences for plasma 5-FU were observed between pre- and postoperative days. In the resected tumor tissues, concentrations of 5-FU were 242 +/- 83 ng/g around 4.5 h and 91.7 +/- 37.0 ng/g around 20 h after the final administration, respectively.

Conclusion: Gastrectomy does not affect on pharmacokinetics of 5-FU derived from S-1 regardless of partial or total gastrectomy, indicating that S-1 can be a useful drug in postoperative adjuvant chemotherapy for gastric cancer.

Publication types

  • Clinical Trial

MeSH terms

  • Administration, Oral
  • Aged
  • Antimetabolites, Antineoplastic / pharmacokinetics*
  • Chemotherapy, Adjuvant
  • Drug Combinations
  • Female
  • Fluorouracil / pharmacokinetics
  • Gastrectomy*
  • Humans
  • Male
  • Middle Aged
  • Oxonic Acid / pharmacokinetics*
  • Pyridines / pharmacokinetics
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / metabolism
  • Stomach Neoplasms / surgery*
  • Tegafur / pharmacokinetics*

Substances

  • Antimetabolites, Antineoplastic
  • Drug Combinations
  • Pyridines
  • S 1 (combination)
  • Tegafur
  • Oxonic Acid
  • Fluorouracil
  • gimeracil