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Cebranopadol is a first-in-class, orally available small molecule analgesic of the benzenoid class. It acts as a dual agonist at the nociceptin/orphanin FQ peptide (NOP) receptor and classical opioid receptors, including mu (MOP), delta (DOP), and kappa (KOP) opioid receptors. Cebranopadol is unique in its mechanism, providing both NOP and opioid receptor agonism within a single molecule. This mixed activity offers potential advantages for treating moderate-to-severe acute and chronic pain, with clinical trials demonstrating efficacy in conditions such as chronic low back pain, cancer pain, osteoarthritis pain, diabetic neuropathy, neoplasms-related pain, and post-surgical pain. The drug has shown favorable safety profiles in phase 3 studies for acute pain and is also being investigated for opioid use disorder. Originally discovered by Grünenthal in Germany and further developed by Tris Pharma in the United States (with previous involvement from Park Therapeutics and Depomed), cebranopadol is currently under late-stage clinical development with plans for regulatory submission[1][3][4][6][7].
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