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Published on: June 8, 2022
[Pharmacokinetics of S-1]
Koichi Hirata1, Noboru Horikoshi, Kazusaku Tominaga
1Dept of Surgery (Section 1), Sapporo Medical University, Japan.
Gan to Kagaku Ryoho. Cancer & Chemotherapy
|August 11, 2006
Summary
S-1, an oral chemotherapy, combines tegafur, CDHP, and potassium oxonate. Pharmacokinetic studies show its 5-fluorouracil (5-FU) release mimics intravenous infusion, suggesting efficacy with reduced toxicity.
Area of Science:
- Oncology
- Pharmacology
- Drug Development
Context:
- S-1 is an oral fluoropyrimidine antitumor drug.
- It combines tegafur (prodrug of 5-fluorouracil), CDHP (DPD inhibitor), and potassium oxonate (reduces GI toxicity).
- Previous Phase I/II trials informed earlier publications.
Purpose:
- To detail the pharmacokinetics of S-1 components after administration.
- To compare the pharmacokinetic profile of S-1 to intravenous 5-FU.
- To evaluate the potential for effective antitumor activity with minimized adverse effects.
Summary:
- Pharmacokinetic parameters (plasma concentration, Cmax, Tmax, AUC0-14, T1/2) of 5-FU, FT, CDHP, and Oxo were analyzed in 12 cancer patients (gastric, colorectal, breast).
- Single and consecutive administration trials were conducted.
- Results indicated that the 5-FU release from S-1 closely resembled continuous intravenous 5-FU infusion.
Impact:
- The pharmacokinetic data supports S-1's potential for favorable antitumor effects.
- The drug's formulation may offer a reduced toxicity profile compared to traditional 5-FU administration.
- This study contributes to understanding oral chemotherapy efficacy and patient safety.
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