The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of prodrugs in humans

• Project/Area Number: 23790604
• Research Category: Grant-in-Aid for Young Scientists (B)
• Allocation Type: Multi-year Fund
• Research Field: Applied pharmacology
• Research Institution: Osaka University (2012); Oita University (2011)
• Principal Investigator: SUZAKI Yuki 大阪大学, 医学部附属病院, 特任講師(常勤) (50527645)
• Project Period (FY): 2011 – 2012
• Project Status: Completed (Fiscal Year 2012)
• Budget Amount: ¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000); Fiscal Year 2012: ¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000); Fiscal Year 2011: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
• Keywords: 薬物代謝酵素 / CES1 / プロドラッグ / 遺伝子多型 / カルボキシルエステラーゼ / 個人差 / オセルタミビル / タミフル

Research Abstract

This study was designed to examine whether the pharmacokinetics of prodrug is affected by carboxylesterase (CES) 1A genetic polymorphisms. The individual differences in the metabolism of oseltamivir are not explained by the CES1A genetic polymorphisms. However, one subject, out of a total number of 30, was an outlier with about a10-fold higherAUC for oseltamivir. Further studies are required to reveal the cause of the individual differences in CES1 metabolism.

Research Products

• [Journal Article] The effect of carboxylesterase 1 (CES1) polymorphisms on the pharmacokinetics of oseltamivir in humans. (2013)
  • Author(s): Suzaki Yuki
  • Journal Title: Eur J Clin Pharmacol. Volume: 69(1) Issue: 1 Pages: 21-30
  • DOI: 10.1007/s00228-012-1315-5
  • Peer Reviewed
• [Journal Article] Gly143Glu polymorphism of the human carboxylesterase1 gene in an Asian population. (2013)
  • Author(s): Suzaki Yuki
  • Journal Title: Eur J Clin Pharmacol. Volume: 69(3) Issue: 3 Pages: 735-736
  • DOI: 10.1007/s00228-012-1352-0
  • Peer Reviewed
• [Presentation] オセルタミビル(タミフル[〇!R])の薬物動態に及ぼすCES1A遺伝子多型の影響 (2011)
  • Author(s): 須崎友紀、森本卓哉、伊藤田暎子、高田誠、今井浩光、大山哲司、濱崎一、廣田和仁、上村尚人、稲野彰洋、立石正登、大橋京一
  • Organizer: 第32回 日本臨床薬理学会年会
  • Place of Presentation: 浜松
  • Year and Date: 2011-12-01
• [Presentation] オセルタミビル（タミフル）の薬物動態に及ぼすCES1A遺伝子多型の影響
  • Author(s): 須崎友紀、森本卓哉、伊藤田暎子、高田誠、今井浩光、大山哲司、濱崎一、廣田和仁、上村尚人、稲野彰洋、立石正登、大橋京一
  • Organizer: 第32回日本臨床薬理学会年会
  • Place of Presentation: 浜松