In:
Current Topics in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 20, No. 31 ( 2020-12-03), p. 2822-2829
Abstract:
Opioid agonists elicit their analgesic action mainly via μ opioid receptors; however, their use
is limited because of adverse events including constipation and respiratory depression. It has been shown that analgesic action is transduced by the G protein-mediated pathway whereas adverse events
are by the β-arrestin-mediated pathway through μ opioid receptor signaling. The first new-generation opioid TRV130, which preferentially activates G protein- but not β-arrestin-mediated signal, was constructed
and developed to reduce adverse events. TRV130 and other G protein-biased compounds tend to elicit desirable analgesic action with less adverse effects. In clinical trials, the intravenous TRV130
(oliceridine) was evaluated in Phase I, II and III clinical studies. Here we review the discovery and synthesis of TRV130, its main action as a novel analgesic having less adverse events, its up-to-date status in
clinical trials, and additional concerns about TRV130 as demonstrated in the literature.
Type of Medium:
Online Resource
ISSN:
1568-0266
DOI:
10.2174/1568026620999201027224229
Language:
English
Publisher:
Bentham Science Publishers Ltd.
Publication Date:
2020
SSG:
15,3
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