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

Rohit Singh, Wei Xie, Jessica Williams, Robert Vince, Swati S More

Research output: Contribution to journalArticle

Abstract

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
Volume10
Issue number9
DOIs
StatePublished - Sep 18 2019

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Analgesics
Neurology
Pharmacology
Phase II Clinical Trials
Aminopeptidases
Second Primary Neoplasms
Peripheral Nervous System
Morphine
Opioid Analgesics
Blood
Central Nervous System
tosedostat
Pharmaceutical Preparations

Keywords

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

PubMed: MeSH publication types

  • Journal Article

Cite this

Discovery of Anticancer Clinical Candidate, Tosedostat, As an Analgesic Agent. / Singh, Rohit; Xie, Wei; Williams, Jessica; Vince, Robert; More, Swati S.

In: ACS Chemical Neuroscience, Vol. 10, No. 9, 18.09.2019, p. 4007-4017.

Research output: Contribution to journalArticle

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