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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 5 of 5. This is the beginning of the thread.
Posted by TriedEveryMedication on November 2, 2015, at 10:25:38
The pipeline for new ADs has been pretty bleak lately. This one seems completely different. Approval in 2016 if it passes phase III trials.
https://en.wikipedia.org/wiki/ALKS-5461
"ALKS-5461 is a combination of buprenorphine, a moderate partial agonist of the mu-opioid receptor (MOR) and antagonist/very weak partial agonist of the Kappa-opioid receptor (KOR), and samidorphan, a selective antagonist of the MOR. The combination of these two drugs results in what is functionally a selective blockade of KORs with minimal or negligible effects on the MOR."
P.s. - Bob - fix your charset on your server so it doesn't mangle Greek letters!
Posted by Lamdage22 on November 3, 2015, at 7:20:50
In reply to Novel AD in phase 3 - K-opioid receptor antagonist, posted by TriedEveryMedication on November 2, 2015, at 10:25:38
Thanks for posting.
Posted by Horse on November 3, 2015, at 11:10:23
In reply to Novel AD in phase 3 - K-opioid receptor antagonist, posted by TriedEveryMedication on November 2, 2015, at 10:25:38
Sounds very promising. It's likely contraindicated for anyone on any sort of opioid maintenance. And would likely weaken any prn as well.
Posted by linkadge on November 5, 2015, at 15:28:10
In reply to Re: Novel AD in phase 3 - K-opioid receptor antagonist, posted by Horse on November 3, 2015, at 11:10:23
Interesting. I'm not sure how this would fare in the long term. I wonder if / how quickly the brain upregulates kappa receptors to compensate?
Linkadge
Posted by SLS on November 13, 2015, at 6:36:40
In reply to Re: Novel AD in phase 3 - K-opioid receptor antagonist, posted by linkadge on November 5, 2015, at 15:28:10
> Interesting. I'm not sure how this would fare in the long term. I wonder if / how quickly the brain upregulates kappa receptors to compensate?
Wouldn't that produce a state that allows for a withdrawal rebound depression should one need to discontinue the drug? Perhaps mu recepter upregulation would compensate for this. It may be way more complicated than this, so I guess experience with the drug will ultimately be the only way to settle the question regarding withdrawal.
- Scott
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