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XenaLives

10/27/18 11:24 AM

#170005 RE: Amatuer17 #170004

Anavex has current process patents for 2-73. IP protection is sufficient.

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bas2020

10/27/18 11:37 AM

#170007 RE: Amatuer17 #170004

Anavex has a manufacturing patent on A2-73.

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OFP

10/27/18 1:05 PM

#170017 RE: Amatuer17 #170004

Can company do a simple test in few healthy patients to see the concentration level for DZP and DZP naive patients. That will settle the matter.

If by concentration you mean blood concentration I would not expect it to be dramatically* affected by the binding affinity differences. However your primary point remains. If 2-73 and DZP bind to the same site (and all signs point to a single orthosteric site for both) then they will compete for access and DZP will win when they go head to head (as per the nature of dramatically different binding affinities). With the caveat that DZP may not occupy 100% of receptors at therapeutic doses so limited access might be possible. The result is that 2-73 has limited or no access to the S1R when DZP is present. This should be a very elementary question for AVXL and is one they should have answered long ago...There are two possibilities:
1. AVXL is so incompetent that they didn't already answer this incredibly basic and central question.
2. They have the answer but they are not sharing it (in which case the results are undoubtedly bad).

I think it's #2. Someone needs to ask if they have this data in a public setting when Missling can't do some BS dodge of the question.


*I guess it's theoretically possible to alter the free vs. protein bound levels and therefore potentially affect metabolism rates. Expect this is somewhere between a non-effect and a trivial one though.
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Steady_T

10/27/18 2:40 PM

#170031 RE: Amatuer17 #170004

Does better binding means better concentration?



Binding and concentration are different things.

Concentration is the level of the drug in the blood stream at the time the blood is drawn.

Binding is the number of Sigma 1 sites that the molecule docks in given as a percentage of sites as I interpret the data.