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

  • Thomas M. TzschentkeEmail author
  • Klaus Linz
  • Thomas Koch
  • Thomas Christoph
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 254)


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.


Cancer pain Chronic low back pain Diabetic peripheral neuropathy Nociceptin/orphanin FQ Postoperative pain Respiratory depression 



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


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© Springer Nature Switzerland AG 2019

Authors and Affiliations

  • Thomas M. Tzschentke
    • 1
    Email author
  • Klaus Linz
    • 1
  • Thomas Koch
    • 1
  • Thomas Christoph
    • 1
  1. 1.Grünenthal GmbH, Global InnovationAachenGermany

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