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Comprehensive analysis of endogenous compounds applicable to in vivo evaluation of drugs transporters

Research Project

Project/Area Number 24659071
Research Category

Grant-in-Aid for Challenging Exploratory Research

Allocation TypeSingle-year Grants
Research Field Medical pharmacy
Research InstitutionThe University of Tokyo

Principal Investigator

KUSUHARA Hiroyuki  東京大学, 薬学研究科(研究院), 教授 (00302612)

Project Period (FY) 2012-04-01 – 2014-03-31
Project Status Completed (Fiscal Year 2013)
Budget Amount *help
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2013: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Fiscal Year 2012: ¥1,950,000 (Direct Cost: ¥1,500,000、Indirect Cost: ¥450,000)
Keywords薬物動態 / トランスポーター / 薬物間相互作用 / 個人間変動 / メタボローム / 代謝物 / 内因性基質 / 遺伝子多型
Research Abstract

The purpose of this study is to identify the endogenous probes that are applicable to in vivo evaluation of drug transporter activities in humans. The endogenous probes, the plasma or urinary excretion of which were associated with the transporter activities, were investigated in the biological samples from the healthy subjects who had been enrolled in the drug interaction studies. We could demonstrate that thiamine is a probe renal organic cation transporter (MATE), that 6beta-hydroxycortisol is a probe for renal organic anion transporter (OAT3). Their renal clearances were significantly reduced by the administration of inhibitors, showing their usefulness in the evaluation of drug-drug interactions involving these transporters.

Report

(3 results)
  • 2013 Annual Research Report   Final Research Report ( PDF )
  • 2012 Research-status Report
  • Research Products

    (12 results)

All 2014 2013 2012 Other

All Journal Article (3 results) (of which Peer Reviewed: 3 results,  Open Access: 1 results,  Acknowledgement Compliant: 1 results) Presentation (8 results) (of which Invited: 3 results) Remarks (1 results)

  • [Journal Article] Investigation of endogenous compounds for assessing the drug interactions in the urinary excretion involving multidrug and toxin extrusion proteins2014

    • Author(s)
      Kato K, Mori H, Kito T, Yokochi M, Ito S, Inoue K, Yonezawa A, Katsura T, Kumagai Y, Yuasa H, Moriyama Y, Inui K, Kusuhara H, Sugiyama Y
    • Journal Title

      Pharm Res

      Volume: 31 Pages: 136-147

    • Related Report
      2013 Annual Research Report 2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] 6β-Hydroxycortisol is an endogenous probe for evaluation of drug-drug interactions involving a multispecific renal organic anion transporter, OAT3/SLC22A8, in healthy subjects2014

    • Author(s)
      Imamura Y, Tsuruya Y, Damme K, Heer D, Kumagai Y, Maeda K, Murayama N, Okudaira N, Kurihara A, Izumi T, Sugiyama Y, Kusuhara H
    • Journal Title

      Drug Metab Dispos

      Volume: 42 Pages: 685-694

    • Related Report
      2013 Final Research Report
    • Peer Reviewed
  • [Journal Article] 6β-Hydroxycortisol is an endogenous probe for evaluation of drug-drug interactions involving a multispecific renal organic anion transporter, OAT3/SLC22A8, in healthy subjects.2014

    • Author(s)
      Imamura Y, Tsuruya Y, Damme K, Heer D, Kumagai Y, Maeda K, Murayama N, Okudaira N, Kurihara A, Izumi T, Sugiyama Y, Kusuhara H.
    • Journal Title

      Drug Metab Dispos.

      Volume: 42 Issue: 4 Pages: 685-94

    • DOI

      10.1124/dmd.113.055475

    • Related Report
      2013 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Presentation] Identification of major substrates of efflux transporters in vivo by metabolomics analysis2013

    • Author(s)
      楠原洋之
    • Organizer
      Gordon Research Conference Multi-Drug Efflux Systems
    • Place of Presentation
      Ventura、USA
    • Related Report
      2013 Final Research Report
  • [Presentation] 薬物トランスポーターの発現・機能変動に伴い血漿中濃度・尿中排泄が変動する代謝物の探索2013

    • Author(s)
      楠原洋之
    • Organizer
      第86回日本生化学会
    • Place of Presentation
      横浜
    • Related Report
      2013 Final Research Report
  • [Presentation] 薬物トランスポーターの発現・機能変動に伴い血漿中濃度・尿中排泄が変動する代謝物の探索2013

    • Author(s)
      楠原洋之
    • Organizer
      第86回日本生化学会
    • Place of Presentation
      横浜
    • Related Report
      2013 Annual Research Report
    • Invited
  • [Presentation] Identification of major substrates of efflux transporters in vivo by metabolomic analysis2013

    • Author(s)
      楠原 洋之
    • Organizer
      Gordon Research Conference Multi-Drug Efflux Systems
    • Place of Presentation
      Ventura, USA
    • Related Report
      2012 Research-status Report
    • Invited
  • [Presentation] Recent Developments in Drug-Transporter Research2012

    • Author(s)
      楠原洋之
    • Organizer
      2012 AAPS Annual Meeting and Exposition
    • Place of Presentation
      Chicago、USA
    • Related Report
      2013 Final Research Report
  • [Presentation] Metabolomic analysis of urine specimens after treatment with pyrimethamine, a potent inhibitor of multidrug and toxin extrusion (MATE)2012

    • Author(s)
      加藤幸司, ほか
    • Organizer
      27^<th> JSSX Annual Meeting
    • Place of Presentation
      東京
    • Related Report
      2013 Final Research Report
  • [Presentation] Metabolomic analysis of urine specimens after treatment with pyrimethamine, a potent inhibitor of multidrug and toxin extrusion (MATE)2012

    • Author(s)
      加藤 幸司
    • Organizer
      27th JSSX Annual Meeting
    • Place of Presentation
      東京
    • Related Report
      2012 Research-status Report
  • [Presentation] Recent Developments in Drug-Transporter Research2012

    • Author(s)
      楠原 洋之
    • Organizer
      2012 AAPS Annual Meeting and Exposition
    • Place of Presentation
      Chicago, USA
    • Related Report
      2012 Research-status Report
    • Invited
  • [Remarks]

    • URL

      http://www.f.u-tokyo.ac.jp/~molpk/

    • Related Report
      2013 Final Research Report

URL: 

Published: 2013-05-31   Modified: 2019-07-29  

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