Cebranopadol: novel dual opioid/NOP receptor agonist analgesic. (24th October 2016)

• Record Type: Journal Article
• Authors: Raffa, R. B.; Burdge, G.; Gambrah, J.; Kinecki, H. E.; Lin, F.; Lu, B.; Nguyen, J. T.; Phan, V.; Ruan, A.; Sesay, M. A.; Watkins, T. N.
• Is Part Of: Journal of clinical pharmacy and therapeutics. Volume 42:Number 1(2017)
• Page Start: 8
• Page End: 17
• Publication Date: 2016-10-24
• Subjects: analgesic -- cebranopadol -- chronic pain -- nociceptin/orphanin FQ -- opioid; Clinical pharmacology -- Periodicals; Chemotherapy -- Periodicals; 615
• DOI: 10.1111/jcpt.12461
• Languages: English
• ISSNs: 0269-4727

Abstract

Summary: What is known and objective: Chronic pain presents a difficult clinical challenge because of the limited efficacy, the limiting adverse‐effect profile or the abuse potential of current analgesic options. Cebranopadol is a novel new agent in clinical trials that combines dual agonist action at opioid and nociceptin/orphanin FQ peptide (NOP) receptors. It is the first truly unique, centrally acting analgesic in several years. We here review the basic and clinical pharmacology of cebranopadol. Methods: Published literature and Internet sources were searched to identify information related to the basic science (pharmacology and medicinal chemistry) and development (clinical trial) information on the mechanism of dual opioid and NOP receptor pharmacologic action in general, and for cebranopadol in particular. The identified sources were reviewed and the information synthesized. Results: The preclinical testing of cebranopadol has characterized it as a dual opioid and NOP receptor agonist that displays antinociceptive and antihyperalgesic action in a variety of acute and chronic pain models in animals. Unlike most current traditional opioids, it is generally more potent against neuropathic than nociceptive pain. Several phase 2 clinical trials have been completed. What is new and conclusion: Despite the medical need, a truly novel centrally acting analgesic has not been developed in many years. Cebranopadol represents a truly novel mechanistic approach. Its actual place in pain pharmacotherapy awaits the results of phase 3 clinical trials. Abstract : Chronic pain presents a difficult challenge because of the limited efficacy, adverse effect profile, or abuse potential of current analgesic options. Cebranopadol is a new agent that combines dual agonist action at opioid and nociceptin/orphanin FQ peptide (NOP) receptors and, as such, represents the first truly unique centrally acting analgesic in several years. We review the basic pharmacology and available clinical trial information on cebranopadol.