Yesterday I accessed Novogen's new website after having read the second ASX release yesterday about director resignation, director appointment, I was looking for more info on Dr Andrew Heaton who it seems was the person who developed the drug candidates that MEIP now have, I find it extremely interesting that NRT have bought Triaxial who was started by Dr Andrew Heaton in the first place, it seems to me that MEIP may be about to release some really good news and I reckon NRT/Triaxial are going to leverage off that because what they have is the platform that allowed the drugs that MEIP now have, it seems there are more drugs in that platform, maybe it will be easier for them to trial seeing as how they will be from the same family so to speak!
Here is what I found on the novogen website yesterday, but I cannot access it now?
Novogen’s New Technology Explained
December 5, 2012 By Novogen
Our first post is an attempt to explain a key part of Novogen’s newly-acquired technology. This is the so-called ‘Stealth’ technology……. created specifically to improve the chances of our drugs reaching their cancer target in a fully active state.
First, a bit of terminology that we need to clear up. You might be used to hearing Novogen’s anti-cancer drugs being referred to as isoflavonoids. That is a chemical term. It simply means a particular molecular shape with hydrogen, oxygen and carbon atoms in the appropriate places. All the drugs that Novogen was working on some years ago were all variations of the basic isoflavone molecular scaffold.
The drugs that Novogen is working on now still have an isoflavone heritage, but are so much more complex than the Company was able to produce before that they have become an entirely new family of chemical compounds, only distantly related to isoflavonoids. We refer to these as super benzopyrans.
But the one bit of critical heritage that super benzopyran molecules such as CS-6 have and which is shared by simple isoflavonoid anti-cancer drugs is a particular shape of the head of the molecule that is crucial to binding to the cancer cell target. Where they differ is in the shape of the tail of the molecule, that part of the molecule that delivers the anti-cancer action.
A good analogy is to imagine the molecule as a scorpion….two claws up-front grabbing hold of the prey and a tail then delivering the killer blow. The two ‘claws’ of the isoflavone molecule is how the molecule binds to a particular protein either externally on the cancer cell’s outer membrane or internally on its mitochondrial membrane, with the tail of the molecule then blocking certain functions within the cancer cell leading to its death or malfunction.
The isoflavone ‘claws’ are in fact terminal hydroxyl (OH) groups that are highly chemical reactive. That high reactivity ensures that once they get to a cancer cell they will home in on the target and attach firmly. The problem, however, is that this high chemical reactivity also means that they are prone to binding to a range of substances before they get to the cancer cell. And in this form the isoflavone is inactive…unable to bind to the cancer cell. To use our scorpion analogy again, it would be like putting boxing gloves on the scorpion’s claws, making it impossible for it to grab its prey.
Virtually all isoflavone drug injected into the blood of a patient ends up being bound in this way. The process is called conjugation, with the two main reactive substances being a sugar (glucuronide) or a salt (sulfate). Conjugated isoflavones have no anti-cancer activity and rely on the presence of specific enzymes in the end tissue to cleave off the sugar or the salt in order to release the active isoflavone drug. Normal, healthy tissues are well served with the necessary enzymes to undertake this cleaving; cancer tissues, on the other hand, less so. It’s a lottery….some cancer tissues contain the necessary enzymes, whereas others (probably the majority) don’t, or at best, don’t contain much.
Enter Triaxial’s Stealth technology. We have developed a technology that allows the creation of super benzopyran structures in which the fundamental isoflavone cancer binding site (scorpion claws) is retained, but the tail has been expanded to the point that its anti-cancer potency is considerably enhanced. We have increased the potency of the scorpion’s sting. But in creating the super benzopyran structure, it also emerged that we substantially reduced the susceptibility of the molecule to conjugation. CS-6 is a prime example of this …. a molecule with an exceptionally potent anti-cancer sting in its tail, but two claws that in the laboratory, anyway, are showing a much reduced susceptibility to conjugation.
That’s the promise of this technology. We now proceed to the job of testing this promise in pre-clinical studies.