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Ok HG, Kim SY, Lee SJ, et al. Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?. Korean J Pain. 2018;31(2):73-79doi: 10.3344/kjp.2018.31.2.73.
Ok, H. G., Kim, S. Y., Lee, S. J., Kim, T. K., Huh, B. K., & Kim, K. H. (2018). Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?. The Korean journal of pain, 31(2), 73-79. https://doi.org/10.3344/kjp.2018.31.2.73
Ok, Hwoe Gyeong, et al. "Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?." The Korean journal of pain vol. 31,2 (2018): 73-79. doi: https://doi.org/10.3344/kjp.2018.31.2.73
Ok HG, Kim SY, Lee SJ, Kim TK, Huh BK, Kim KH. Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?. Korean J Pain. 2018 Apr;31(2):73-79. doi: 10.3344/kjp.2018.31.2.73. Epub 2018 Apr 02. PMID: 29686804; PMCID: PMC5904350.
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Korean J Pain. 2018 Apr;31(2):73-79. doi: 10.3344/kjp.2018.31.2.73. Epub 2018 Apr 02.

Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?.

The Korean journal of pain

Hwoe Gyeong Ok, Su Young Kim, Su Jung Lee, Tae Kyun Kim, Billy K Huh, Kyung Hoon Kim

Affiliations

  1. Department of Anesthesia and Pain Medicine, School of Medicine, Pusan National University, Yangsan, Korea.
  2. Department of Pain Medicine, The University of Texas M.D. Anderson Cancer Center, Houston, TX, USA.

PMID: 29686804 PMCID: PMC5904350 DOI: 10.3344/kjp.2018.31.2.73

Abstract

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, while the β-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the β-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the µ receptor G protein pathway selective (µ-GPS) modulation. Even though adverse reactions (ADRs) are significantly attenuated, while the analgesic effect is augmented, the some residual ADRs persist. Consequently, a G protein biased µ opioid ligand, oliceridine, improves the therapeutic index owing to increased analgesia with decreased adverse events. This review article provides a brief history, mechanism of action, pharmacokinetics, pharmacodynamics, and ADRs of oliceridine.

Keywords: Adverse drug reactions; Beta-arrestin 2; G protein-coupled receptors; Intracellular signaling peptides and proteins; Knockout mice; Ligands; Mu opioid receptor; Oliceridine; Opioid analgesics; Patient safety

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