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

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

Handb Exp Pharmacol

Grünenthal GmbH, Global Innovation, Aachen, Germany.

Published: July 2019

AI Article Synopsis

Article 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.

Download full-text PDF

Source
http://dx.doi.org/10.1007/164_2019_206DOI Listing

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