Nafamostat mesilate is an extremely potent inhibitor of human tryptase

Shuji Mori, Yoshinori Itoh, Ryoko Shinohata, Toshiaki Sendo, Ryozo Oishi, Masahiro Nishibiro

Research output: Contribution to journalArticlepeer-review

92 Citations (Scopus)


Previously, nafamostat mesilate was found to be a potent inhibitor of human tryptase. In present study, we performed a kinetic study to determine its Ki value for tryptase and compared it with that of gabexate mesilate. Nafamostat mesilate inhibited human tryptase in a competitive manner. The apparent Ki value was estimated to be 95.3 pM, which was 1,000 times lower than that of gabexate mesilate (95.1 nM). These results strongly indicated that nafamostat mesilate is an extremely potent inhibitor of tryptase and suggested that some of its beneficial effects in the treatment of clinical status may be due to tryptase inhibition.

Original languageEnglish
Pages (from-to)420-423
Number of pages4
JournalJournal of Pharmacological Sciences
Issue number4
Publication statusPublished - Aug 1 2003


  • Inhibition
  • Nafamostat mesilate
  • Tryptase

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology


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