Can oliceridine (TRV130), an ideal novel µ receptor G protein pathway selective (µ-GPS) modulator, provide analgesia without opioid-related adverse reactions?
- Author:
Hwoe Gyeong OK
1
;
Su Young KIM
;
Su Jung LEE
;
Tae Kyun KIM
;
Billy K HUH
;
Kyung Hoon KIM
Author Information
- Publication Type:Review
- 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
- MeSH: Analgesia; Analgesics, Opioid; Animals; Bias (Epidemiology); Drug-Related Side Effects and Adverse Reactions; GTP-Binding Proteins; Intracellular Signaling Peptides and Proteins; Ligands; Mice; Mice, Knockout; Nausea; Patient Safety; Pharmacokinetics; Receptors, Opioid; Receptors, Opioid, mu; Respiratory Insufficiency; Vomiting
- From:The Korean Journal of Pain 2018;31(2):73-79
- CountryRepublic of Korea
- Language:English
- 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.
