Oliceridine — a unique drug among opioid analgesics

Authors

DOI:

https://doi.org/10.20883/medical.e464

Keywords:

oliceridine, opioids, pain, tolerance

Abstract

Oliceridine is an opioid with a different mechanism of action compared to classical opioid agonists, e.g. morphine, as it does not act through active metabolites and activates the β-arrestin pathway to a small extent, thereby reducing dangerous side effects and broadening the therapeutic window. This is particularly important as, despite the wide availability of drugs from various therapeutic groups, the effectiveness of analgesics in many patients remains low. Oliceridine is a novel and effective analgesic providing rapid analgesia, with a favourable safety and tolerability profile concerning respiratory and gastrointestinal adverse effects compared to morphine, and may provide a new treatment option for patients with moderate to severe postoperative pain where an intravenous opioid is required.

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References

Stein C. Opioid Receptors. Annual Review of Medicine. 2016 Jan 14;67(1):433-451. https://doi.org/10.1146/annurev-med-062613-093100

Sadhasivam S, Chidambaran V. Pharmacogenomics of opioids and perioperative pain management. Pharmacogenomics. 2012 Nov;13(15):1719-1740. https://doi.org/10.2217/pgs.12.152

Bohn LM, Lefkowitz RJ, Gainetdinov RR, Peppel K, Caron MG, Lin F. Enhanced Morphine Analgesia in Mice Lacking β-Arrestin 2. Science. 1999 Dec 24;286(5449):2495-2498. https://doi.org/10.1126/science.286.5449.2495

Corder G, Castro DC, Bruchas MR, Scherrer G. Endogenous and Exogenous Opioids in Pain. Annual Review of Neuroscience. 2018 Jul 8;41(1):453-473. https://doi.org/10.1146/annurev-neuro-080317-061522

Szymiczek M, Kurowska E, Gorczyca W. Rola arestyn w sygnalizacji wewnatrzkomórkowej [Role of arrestins in intracellular signaling]. Postepy Hig Med Dosw. 2005 Jul 8;59:324-33. PMID 16012393

Maguma HT, Dewey WL, Akbarali HI. Differences in the characteristics of tolerance to μ-opioid receptor agonists in the colon from wild type and β-arrestin2 knockout mice. European Journal of Pharmacology. 2012 Jun;685(1-3):133-140. https://doi.org/10.1016/j.ejphar.2012.04.001

Raehal KM, Walker JKL, Bohn LM. Morphine Side Effects in β-Arrestin 2 Knockout Mice. Journal of Pharmacology and Experimental Therapeutics. 2005 May 25;314(3):1195-1201. https://doi.org/10.1124/jpet.105.087254

Cheng J, Cheng T, Li W, Liu G, Zhu W, Tang Y. Computational insights into the G-protein-biased activation and inactivation mechanisms of the μ opioid receptor. Acta Pharmacologica Sinica. 2017 Nov 30;39(1):154-164. https://doi.org/10.1038/aps.2017.158

Raehal K, Bohn L. β-arrestins: regulatory role and therapeutic potential in opioid and cannabinoid receptor-mediated analgesia. Handb Exp Pharmacol. 2014;219:427-43. https://doi.org/10.1007/978-3-642-41199-1_22 PMID 24292843

Bohn L. Selectivity for G protein or arrestin-mediated signaling. In: Neve K, ed. Functional Selectivity of G Protein-Coupled Receptor Ligands. Humana Press; 2009:71-85.

Kenakin T. New Concepts in Drug Discovery: Collateral Efficacy and Permissive Antagonism. Nature Reviews Drug Discovery. 2005 Nov;4(11):919-927. https://doi.org/10.1038/nrd1875

Kenakin T. Biased agonism. F1000 Biology Reports. 2009 Nov 26;1. https://doi.org/10.3410/b1-87

Mailman RB. GPCR functional selectivity has therapeutic impact. Trends in Pharmacological Sciences. 2007 Aug;28(8):390-396. https://doi.org/10.1016/j.tips.2007.06.002

Urban JD, Clarke WP, von Zastrow M, Nichols DE, Kobilka B, Weinstein H, Javitch JA, Roth BL, Christopoulos A, Sexton PM, Miller KJ, Spedding M, Mailman RB. Functional Selectivity and Classical Concepts of Quantitative Pharmacology. Journal of Pharmacology and Experimental Therapeutics. 2006 10.1124/jpet.112.2016166 27;320(1):1-13. https://doi.org/10.1124/jpet.106.104463

DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen X, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD. A G Protein-Biased Ligand at the μ-Opioid Receptor Is Potently Analgesic with Reduced Gastrointestinal and Respiratory Dysfunction Compared with Morphine. Journal of Pharmacology and Experimental Therapeutics. 2013 Jan 8;344(3):708-717. https://doi.org/10.1124/jpet.112.201616

Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang X, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Aug 17;537(7619):185-190. https://doi.org/10.1038/nature19112

Nafziger AN, Arscott KA, Cochrane K, Skobieranda F, Burt DA, Fossler MJ. The Influence of Renal or Hepatic Impairment on the Pharmacokinetics, Safety, and Tolerability of Oliceridine. Clinical Pharmacology in Drug Development. 2019 Nov 7;9(5):639-650. https://doi.org/10.1002/cpdd.750

Viscusi ER, Webster L, Kuss M, Daniels S, Bolognese JA, Zuckerman S, Soergel DG, Subach RA, Cook E, Skobieranda F. A randomized, phase 2 study investigating TRV130, a biased ligand of the μ-opioid receptor, for the intravenous treatment of acute pain. PAIN. 2016 Jan;157(1):264-272. https://doi.org/10.1097/j.pain.0000000000000363

Liang D, Li W, Nwaneshiudu C, Irvine K, Clark JD. Pharmacological Characters of Oliceridine, a μ-Opioid Receptor G-Protein–Biased Ligand in Mice. Anesthesia & Analgesia. 2019 Nov;129(5):1414-1421. https://doi.org/10.1213/ane.0000000000003662

Altarifi AA, David B, Muchhala KH, Blough BE, Akbarali H, Negus SS. 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. Journal of Psychopharmacology. 2017 Feb;31(6):730-739. https://doi.org/10.1177/0269881116689257

Austin Zamarripa C, Edwards SR, Qureshi HN, Yi JN, Blough BE, Freeman KB. The G-protein biased mu-opioid agonist, TRV130, produces reinforcing and antinociceptive effects that are comparable to oxycodone in rats. Drug and Alcohol Dependence. 2018 Nov;192:158-162. https://doi.org/10.1016/j.drugalcdep.2018.08.002

Gan T, Wase L. Oliceridine, a G protein-selective ligand at the mu-opioid receptor, for the management of moderate to severe acute pain. Drugs of Today. 2020;56(4):269. https://doi.org/10.1358/dot.2020.56.4.3107707

Gan T, Wase L. Oliceridine, a G protein-selective ligand at the mu-opioid receptor, for the management of moderate to severe acute pain. Drugs of Today. 2020;56(4):269. https://doi.org/10.1358/dot.2020.56.4.3107707

Viscusi ER, Skobieranda F, Soergel DG, Cook E, Burt DA, Singla N.

APOLLO-1: a randomized placebo and active-controlled phase III study investigating oliceridine (TRV130), a G protein-biased ligand at the µ-opioid receptor, for management of moderate-to-severe acute pain following bunionectomy

. Journal of Pain Research. 2019 Mar;Volume 12:927-943. https://doi.org/10.2147/jpr.s171013

Pedersen MF, Wróbel TM, Märcher-Rørsted E, Pedersen DS, Møller TC, Gabriele F, Pedersen H, Matosiuk D, Foster SR, Bouvier M, Bräuner-Osborne H. Biased agonism of clinically approved μ-opioid receptor agonists and TRV130 is not controlled by binding and signaling kinetics. Neuropharmacology. 2020 Apr;166:107718. https://doi.org/10.1016/j.neuropharm.2019.107718

Singla N, Skobieranda F, Soergel D, Salamea M, Burt D, Demitrack M, Viscusi E. APOLLO-2: A Randomized, Placebo and Active-Controlled Phase III Study Investigating Oliceridine (TRV130), a G Protein-Biased Ligand at the μ-Opioid Receptor, for Management of Moderate to Severe Acute Pain Following Abdominoplasty. Pain Pract. 2019 Sep;19(7):715-31. https://doi.org/10.1111/papr.12801 PMID 31162798

Fossler MJ, Sadler BM, Farrell C, Burt DA, Pitsiu M, Skobieranda F, Soergel DG. Oliceridine (TRV130), a Novel G Protein-Biased Ligand at the μ-Opioid Receptor, Demonstrates a Predictable Relationship Between Plasma Concentrations and Pain Relief. I: Development of a Pharmacokinetic/Pharmacodynamic Model. The Journal of Clinical Pharmacology. 2018 Feb 7;58(6):750-761. https://doi.org/10.1002/jcph.1076

Soergel DG, Ann Subach R, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW. First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers. The Journal of Clinical Pharmacology. 2014 Jan 28;54(3):351-357. https://doi.org/10.1002/jcph.207

Negus SS, Freeman KB. Abuse Potential of Biased Mu Opioid Receptor Agonists. Trends in Pharmacological Sciences. 2018 Nov;39(11):916-919. https://doi.org/10.1016/j.tips.2018.08.007

Trevena Announces FDA Approval of OLINVYK™ (Oliceridine) Injection.

William E, James C. Oliceridine Injection. Internal Medicine Alert. 2020 Sep;42(17).

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Published

2020-09-29

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How to Cite

1.
Gibuła-Tarłowska E, Burat M, Kędzierska E. Oliceridine — a unique drug among opioid analgesics. JMS [Internet]. 2020 Sep. 29 [cited 2024 Nov. 5];89(3):e464. Available from: https://jms.ump.edu.pl/index.php/JMS/article/view/464
Received 2020-09-07
Accepted 2020-09-24
Published 2020-09-29