The G Protein Signal-Biased Compound TRV130; Structures, Its Site of Action and Clinical Studies
Current Topics in Medicinal Chemistry, 2020Opioid 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 ...
Kanako Miyano +2 more
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First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers
Journal of Clinical Pharmacology, 2014Abstract TRV130 is a G protein‐biased ligand at the µ‐opioid receptor. In preclinical studies it was potently analgesic while causing less respiratory depression and gastrointestinal dysfunction than morphine, suggesting unique benefits in acute pain management.
David G Soergel +2 more
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The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats [PDF]
Drug and Alcohol Dependence, 2018 Mu-opioid agonists (e.g., oxycodone) are highly effective therapeutics for pain. However, they also produce reinforcing effects that increase their likelihood of abuse. Recent strategies in drug development have focused on opioids with biased receptor-signaling profiles that favor activation of specific intracellular pathways over others with the aim ...
Bruce E Blough, Kevin B Freeman
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Effects of acute and repeated treatment with the biased mu opioid receptor agonist TRV130 (oliceridine) on measures of antinociception, gastrointestinal function, and abuse liability in rodents [PDF]
Journal of Psychopharmacology, 2017 Rationale: TRV130 (oliceridine; N-[(3-methoxythiophen-2-yl)methyl]-2-[(9 R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethanamine) is a novel mu opioid receptor (MOR) agonist that preferentially activates G-protein versus β-arrestin signaling pathways coupled to MORs.
Ahmad Altarifi +2 more
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The G‐protein‐biased agents PZM21 and TRV130 are partial agonists of μ‐opioid receptor‐mediated signalling to ion channels [PDF]
British Journal of Pharmacology, 2019 Background and Purpose Opioids remain the most efficient medications against severe pain; they act on receptors that couple to heterotrimeric G‐proteins in the G αi/o family.
Yevgen Yudin, Tibor Rohacs
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Mo1578 - The Effect of a G-Protein Biased Ligand, TRV130, on Opioid-Induced Constipation
Gastroenterology, 2018Hamid I Akbarali
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Efficacy of conventional opioids can be limited by adverse events (AEs). TRV130 is a structurally novel biased ligand of the μ-opioid receptor that activates G protein signaling with little β-arrestin recruitment. In this phase 2, randomized, placebo- and active-controlled study, we investigated the efficacy and tolerability of TRV130 in acute pain ...
Eugene R Viscusi +2 more
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Korean Journal of Pain, 2018 All drugs have both favorable therapeutic and untoward adverse effects. Conventional opioid analgesics possess both analgesia and adverse reactions, such as nausea, vomiting, and respiratory depression. The opioid ligand binds to µ opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia,
Tae Kyun Kim
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Conventional opioids provide powerful analgesia but also produce efficacy-limiting adverse effects, limiting their clinical utility (CU). TRV130 is being evaluated to determine whether CU can be expanded by way of increased efficacy, decreased adverse effects, or some combination thereof.This phase 2 study of TRV130 blends traditional objectives with ...
Franck Skobieranda
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First Human Dosing Experience with TRV130, a Biased Ligand at the Mu Opioid Receptor (P02.013)
Neurology, 2013David Soergel +5 more
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