Can oliceridine (TRV130), an ideal novel micro receptor G protein pathway selective (micro-GPS) modulator, provide analgesia without opioid-related adverse reactions?
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Ok HG, Kim SY, Lee SJ, Kim TK, Huh BK, Kim KH
Can oliceridine (TRV130), an ideal novel micro receptor G protein pathway selective (micro-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 2.
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- 29686804 [ View in PubMed]
- 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 micro opioid receptor and non-selectively activates two intracellular signaling pathways: the G protein pathway induce analgesia, while the beta-arrestin pathway is responsible for the opioid-related adverse reactions. An ideal opioid should activate the G protein pathway while deactivating the beta-arrestin pathway. Oliceridine (TRV130) has a novel characteristic mechanism on the action of the micro receptor G protein pathway selective (micro-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 micro 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.
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