Mr. Brodkin And His Post On Twitter About $AVXL. Part One.

Do not trade this blog as 4 billion years of evolution is against me and possibly even God laughs at it, He has a great sense of humor!

There will be number of posts on this lengthy twitter post by Jesse Brodkin, who claims to be a scientist and enterpreneur.

let’s see the first assertion made by Mr. Brodkin.

Mr. Brodkin claimes that Anavex2-73 is being dosed 30 to 100 fold too low to engage SIGMAR1 or M-1 receptors. So let’s run the numbers. Link to Mr. Brokin’s tweet https://twitter.com/jesse_brodkin/status/1550477966123171840?s=20&t=MdTQ5Aes7PJyFbCFHRQQAQ

Accordingly to Wikipedia IC50 is measure of amount of compound to achieve ~50% inhibition . Link https://en.wikipedia.org/wiki/IC50.

IC50=860 nanoMole for SIGMAR1.

So Mr. Brodkin claimes that the amount of Anvex2-73 in the blood is just too low to bind to SIGMAR1 sufficiently to have ~50% occupancy at SIGMAR1. Let’s see his numbers.

There are 317 grams per Mole. The blood concentration of 6 nanograms per milliliter gives 18.9274 nanoMoles per liter. All is fine but an adult has about 5 liters of blood. Accordingly there should be 30 micrograms of Anavex2-73 in an adult patient or about 95 nanomoles at the point of measurement. Now, we go to the crux of the matter, the concentration in the blood under constant dosing is not the occupation of the SIGMAR1 or M-1. Why, because the concentration is dependent on the rate the drug is being digested (entering stomach juices) and absorbed in small intestine, then the rate it occupies the SIGMAR1 , and most of all how long it stays there. The fact that blood concentration can be 1/10 of IC50 at any given moment means nothing as occupancy is dependent on its dynamics, not concentration in blood on any given moment. IC50 measures overall quantity not concentration in blood. These are two diferent things. Also IC50 measures not occupancy but reaction to some unspecified occupancy.
Anavex ran number of tests on murine model with riadiography to document the almost full occupancy of SIGMAR1 by Blarcamesine. It is all in presentations given by the company. I will not hunt for these slides as my time is limited this morning.
Mr. Brodkin exhibits, at least for a scientists, basic misunderstanding of measured quatities and their relationships. This is basic science. There is a note approprieting the information to somebody else refered to by @black6cap. That is even more damning. Picking up info from somebody and not checking it for inconsistencies. Also IC50 measures not occupancy but reaction to some unspecified occupancy.

Soon to be continued.

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