Phase I pharmacokinetic study of S-1 plus cisplatin in patients with advanced gastric carcinoma

J Clin Oncol. 2005 Oct 1;23(28):6957-65. doi: 10.1200/JCO.2005.01.917. Epub 2005 Sep 6.

Abstract

Purpose: The conversion rate of tegafur (a component of S-1) to fluorouracil (FU) differs in Asians and whites because of polymorphic differences in the CYP2A6 gene. S-1 with cisplatin is considered highly active in Japanese gastric cancer patients. Therefore, we initiated a phase I pharmacokinetic study of this combination in our gastric cancer patients.

Patients and methods: Patients received cisplatin intravenously on day 1 and S-1 orally, twice daily, on days 1 to 21 every 28 days. At level 1, the S-1 dose was 25 mg/m2/dose (50 mg/m2/d), but it was increased by 5 mg/m2/dose for the next level. Cisplatin was administered at 75 mg/m2 (for levels 1 and 2) but was then reduced to 60 mg/m2 (level 1A). At every level, a cohort of three patients, which could be expanded to six patients, was studied. Maximum-tolerated dose (MTD) was determined based on the dose-limiting toxicity (DLT) in the first cycle. Patients with histologic proof of gastric adenocarcinoma and near-normal organ function were studied.

Results: Sixteen patients were enrolled. No DLTs occurred at level 1. However, DLTs occurred at levels 2 and 1A. The area under the curve for FU correlated significantly with DLT (P = .006) and grade 3 to 4 diarrhea (P = .004). Six partial responses were confirmed, including three at the MTD.

Conclusion: At the established MTD of S-1 plus cisplatin, the S-1 dose (50 mg/m2/d for 21 days) is lower in our study than in the Japanese study (80 mg/m2/d for 21 days). A multi-institutional phase II study of this active combination is currently accruing patients.

Publication types

  • Clinical Trial
  • Clinical Trial, Phase I
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenocarcinoma / drug therapy*
  • Adenocarcinoma / pathology
  • Administration, Oral
  • Adult
  • Antineoplastic Combined Chemotherapy Protocols / pharmacokinetics*
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use*
  • Area Under Curve
  • Cisplatin / administration & dosage
  • Drug Combinations
  • Female
  • Humans
  • Infusions, Intravenous
  • Male
  • Maximum Tolerated Dose
  • Middle Aged
  • Oxonic Acid / administration & dosage
  • Oxonic Acid / pharmacokinetics
  • Pyridines / administration & dosage
  • Pyridines / pharmacokinetics
  • Stomach Neoplasms / drug therapy*
  • Stomach Neoplasms / pathology
  • Tegafur / administration & dosage
  • Tegafur / pharmacokinetics
  • Treatment Outcome

Substances

  • Drug Combinations
  • Pyridines
  • S 1 (combination)
  • Tegafur
  • Oxonic Acid
  • Cisplatin