Opioid Tolerance-Abating Treatment
A precision medicine approach blocking formation of analgesic tolerance and reversing analgesic tolerance from chronic opioid administration.
Opiates are commonly prescribed in the US for surgical and other severe pain; and many people also obtain opioids illegally. Opioids work well for acute pain; but for those with chronic pain requiring long-term treatment, this pain management strategy has been a disaster. People accommodate to opiates quickly, and in an attempt to obtain pain relief, self-treat by increasing the dose. This is a slippery slope to addiction and, for some, to death. In 2014, nearly 19,000 people died in the US from opioid overdose; by 2019, that number had more than tripled, and it just keeps going up.
SUNY Downstate Medical Center researchers have identified a scaffolding domain-competing peptide as well as an endogenous, non-receptor tyrosine kinase (c-Src) inhibitor (PP2) that is able to do two things: 1. block the development of morphine analgesic tolerance, and 2. reverse the tolerance once it has developed. These blocking and reversing effects both last for days and they remain fully effective even after a number of repeated treatments.
Since tolerance does not develop when the scaffolding domain-competing peptide is administered, it can be repeatedly administered for chronic pain management without the worry about addiction or overdose. The idea that a single biochemical perturbation may be a cellular adaptation mediating analgesic tolerance by altering the formation of multiple signaling complexes is a novel departure from conventional thinking.
This innovative technology is quite different from other pain relief therapies; and its ability to mitigate multiple opioid analgesic tolerance mechanisms concomitantly is a more effective -- and much safer -- pain relieving strategy than anything currently available.
Further Details:
- Subcellular Localization of μ-Opioid Receptor Gs Signaling J Pharmacol Exp Ther. 2010.
- Chronic opioid treatment augments caveolin-1 scaffolding: relevance to stimulatory μ-opioid receptor adenylyl cyclase signaling J Neurochem. 2016.
There is no other similar or effective strategy for mitigating opioid tolerance and treating pain while blocking the development of, and reversing already present opioid tolerance.
For chronic pain patients on longer-term opioids and for anyone who has been treated for opioid overdose but is continuing to take opioids.
PCT/US20/67679 METHODS FOR PREVENTING AND REVERSING OPIOID ANALGESIC TOLERANCE IN SUBJECTS WITH CHRONIC PAIN, Filed 12/31/20
Available for collaboration or licensing to move technology into clinical trials and beyond.
Development partner, Licensing
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