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ATX-1209 (metabolite of naltrexone): ~100-fold less potent antagonist than naltrexone in blocking opioid analgesia
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Repeat opioid analgesic dosing leads to a sustained ligand free signaling active state (MOR-u**) driving opioid dependence
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ATX-1209 potently binds MOR-u** gradually reversing the receptor back to the resting state, reversing dependence
Potential Clinical Utility
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Non-addictive pain therapy combined with an opioid agonist
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Treatment for Opioid Use Disorder
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Prevention and treatment for Neonatal Opioid Withdrawal Syndrome (NOWS)
Mechanism of Action
Pre-clinical studies have shown that ATX-1209 potently reverses the opioid dependent state by lowering elevated ligand-free signaling of the
µ opioid receptor (MOR), a driver of opioid dependence.