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Cebranopadol: A Novel First-in-Class Potent Analgesic Acting via NOP and Opioid Receptors

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The Nociceptin/Orphanin FQ Peptide Receptor

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 254))

Abstract

Cebranopadol is a novel first-in-class analgesic with highly potent agonistic activity at nociceptin/orphanin FQ peptide (NOP) and opioid receptors. It is highly potent and efficacious across a broad range of preclinical pain models. Its side effect profile is better compared to typical opioids. Mechanistic studies have shown that cebranopadol’s activity at NOP receptors contributes to its anti-hyperalgesic effects while ameliorating some of its opioid-type side effects, including respiratory depression and abuse potential. Phase II of clinical development has been completed, demonstrating efficacy and good tolerability in acute and chronic pain conditions.

This article focusses on reviewing data on the preclinical in vitro and in vivo pharmacology, safety, and tolerability, as well as clinical trials with cebranopadol.

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Acknowledgments

Thanks are given to Stefanie Frosch and Marielle Eerdekens for careful revision of the manuscript.

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  1. Grünenthal GmbH, Global Innovation, Aachen, Germany

    Thomas M. Tzschentke, Klaus Linz, Thomas Koch & Thomas Christoph

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  1. Thomas M. Tzschentke
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  2. Klaus Linz
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Correspondence to Thomas M. Tzschentke .

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  1. Department of Physiology and Pharmacology, Wake Forest University, School of Medicine, Winston-Salem, NC, USA

    Mei-Chuan Ko

  2. Department of Medical Sciences, Section of Pharmacology, University of Ferrara, Ferrara, Italy

    Girolamo Caló

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Tzschentke, T.M., Linz, K., Koch, T., Christoph, T. (2019). Cebranopadol: A Novel First-in-Class Potent Analgesic Acting via NOP and Opioid Receptors. In: Ko, MC., Caló, G. (eds) The Nociceptin/Orphanin FQ Peptide Receptor. Handbook of Experimental Pharmacology, vol 254. Springer, Cham. https://doi.org/10.1007/164_2019_206

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