Development of a novel trapping reagent, GSHEE-d<sub>5</sub>, for reactive metabolites

DOI
  • Yamaoka Toshikazu
    DMPK Research Laboratory, Watarase Research Center, Kyorin Pharmaceutical Co., Ltd.

Bibliographic Information

Other Title
  • 新規反応性代謝物トラッピング試薬GSHEE-d<sub>5</sub>の開発

Abstract

<p>Reactive metabolites (RMs) are thought to be one of the causes of idiosyncratic drug toxicity (IDT). During the lead optimization stage of drug discovery, glutathione trapping assay is performed to eliminate chemical entities that produce RMs from drug candidates. However, the assay often produces false-positive and false-negative results. Although various glutathione analogs have been developed, the detection capability is still insufficient. A novel trapping reagent, GSHEE-d5, which was invented to overcome the disadvantages of existing reagents, was capable of detecting RMs with high sensitivity and selectivity. Thus, this reagent can provide reliable clues for medicinal chemists to address RM-related problems. GSHEE-d5 is expected to be useful in the development of safe drugs with a lower potential of IDT.</p>

Journal

  • MEDCHEM NEWS

    MEDCHEM NEWS 27 (2), 100-104, 2017-05-01

    The Pharmaceutical Society of Japan

Keywords

Details 詳細情報について

  • CRID
    1390564238107931520
  • NII Article ID
    130007685152
  • DOI
    10.14894/medchem.27.2_100
  • ISSN
    24328626
    24328618
  • Text Lang
    ja
  • Data Source
    • JaLC
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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