Two dosages of oral fluoropyrimidine S-1 of 35 and 40 mg/m2 bid: Comparison of the pharmacokinetic profiles in Korean patients with advanced gastric cancer

Hei Cheul Jeung, Sun Young Rha, Sang Joon Shin, Joong Bae Ahn, Sung Hoon Noh, Jae Kyung Roh, Hyun Cheol Chung

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Abstract

Objective: In this study, we compared the pharmacokinetic profiles of 5-fluorouracil (5-FU), tegafur, 5-chloro-2,4-dihydroxypyridine (CDHP) and potassium oxonate (Oxo) after administration of S-1 at 35 or 40 mg/m. 2 bid for 28 consecutive days, in Cycles 1 and 3, in patients with advanced gastric cancer. Methods: Three patients were enrolled for each dosage. S-1 dosage was assigned based on body surface area (BSA), which is different from the Japanese dosing system. The median daily dose per BSA was 76 mg/m. 2, ranging from 70 to 88 mg/m. 2. Results: Plasma levels of 5-FU, tegafur, CDHP and Oxo at 4 h post-dose reached steady-state on day 8. The estimated steady-state level was dependent on S-1 dosage. There were no intercyclic differences of pre-dose and 4 h post-dose levels between Cycles 1 and 3, implying no cumulative effect of S-1 was shown probably due to 2-week drug-resting period. Pharmacokinetic profiles on day 28 were similar to previous Japanese report. Cmax and AUC0-48 h values of each S-1 component increased depending on S-1 dosage. Pharmacokinetic parameters were not correlated with tumor response or toxicity. Conclusions: We suggest that these pharmacokinetic profiles of Asian population could provide a basis for schedule optimization and for additional studies on interaction with other antitumor drugs.

Original languageEnglish
Article numberhyp124
Pages (from-to)29-35
Number of pages7
JournalJapanese Journal of Clinical Oncology
Volume40
Issue number1
DOIs
Publication statusPublished - 2009 Oct 31

All Science Journal Classification (ASJC) codes

  • Oncology
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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