Discovery of Anticancer Clinical Candidate, Tosedostat, As an Analgesic Agent

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Tosedostat is an inhibitor of aminopeptidases currently in phase II clinical trials for the treatment of blood-related cancers. In our laboratories, we have discovered that it possesses analgesic properties. Extensive in vivo pharmacological studies for the determination of antinociceptive effects of tosedostat are presented here. These studies have indicated that the observed analgesic effect of tosedostat stems from its action on the peripheral nervous system with minimal contribution from the central nervous system. Additionally, when given in combination with morphine, tosedostat exerts a synergistic analgesic effect resulting in a reduction of effective dosages required to achieve the same analgesic effect. With broad implications in addressing the opioid addiction crisis, these revelations attest to tosedostat being a highly valuable drug candidate with diverse pharmacological functions.

Original languageEnglish (US)
Pages (from-to)4007-4017
Number of pages11
JournalACS Chemical Neuroscience
Issue number9
StatePublished - Sep 18 2019

Bibliographical note

Funding Information:
This research study was supported by the Center for Drug Design research endowment funds at the University of Minnesota, Minneapolis.

Publisher Copyright:
Copyright © 2019 American Chemical Society.


  • analgesia
  • leu-enkephalin
  • met-enkephalin
  • pain
  • peptidase
  • tosedostat


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