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Cebranopadol: novel dual opioid/ NOP receptor agonist analgesic
Author(s) -
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.
Publication year - 2017
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1111/jcpt.12461
Subject(s) - nop , nociceptin receptor , analgesic , medicine , chronic pain , opioid , pharmacology , clinical trial , agonist , neuropathic pain , receptor , opioid peptide , physical therapy
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.