Found this on another site via google:
Epitiostanol (2?,3?-Epithio-5?-androstan-17?-ol) - A controlled substance.
Havoc has added 17-alpha methyl group.
Epitiostanol is a relatively obscure steroid used for breast cancer that is only available in Japan. Again you might say, ?How does a drug used for breast cancer work for us extreme fitness types?? Well, Epitiostanol was actually developed back in the 1960?s and has an
extremely good anabolic/androgenic ratio. This means that it causes a whole host of positive effects in the body with minimal negative androgenic effects. The reason it was used for breast cancer is that it was shown to exert a potent anti-estrogenic effect which halted the progression of estrogen-stimulated cancers. What wonderful characteristics to have in a steroid! Great muscle growth with small androgenic phenomenon with no estrogenic problems like gyno?sounds like the perfect steroid!
Well, the Japanese company Shionogi thought so too but they wanted a characteristic that epitiostanol lacked?significant oral bioavailability. The smart people at this company went back into the literature and found that 17B steroidal ethers caused a significant increase in oral bioavailability. They used the ether technology and voila, they created Mepitiostane. Fortunately, they didn?t stop there! They decided to
elucidate just how these ethers work. Read below for the story!
The Shionogi research team began their quest by asking the question as to what possible ways could the ether group be increasing bioavailability. They realized that orally administered drugs and nutrients are transferred to the systemic circulation via the portal and/or lymphatic route following passage through the mucosal cell of the intestinal lumen. They also understood that the portal route is considered to be the main route for compounds absorbed from the intestines because blood flow is about 500 times greater than lymph flow in capillaries of the villus.
Thus they first looked at the portal route and asked whether the ether group on the steroid could be preventing the steroid from being metabolized by the liver. They looked at the characteristics of the molecule and decided that this was probably not the right answer.
Although not the primary place of absorption of most compounds, the intestinal lymphatic system is known to play an important role in the absorption of some compounds such as long chain fatty acids, triglycerides and lipid soluble vitamins. A compound absorbed via intestinal lymphatics directly enters the systemic circulation at the level of the subclavian vein which avoids first pass metabolism of the compound through the liver.
With this in mind, our good friends at Shionogi decided to look here for their answers. Hey, all I can say is that these guys were right on the money! Using radioactive labeling of both Epitiostanol and Mepitiostane, they found that Epitiostanol is almost entirely absorbed via the portal route while mepitiostane is almost entirely absorbed via the lymphatic route. Bingo!
One of the most fascinating things that I noticed in their research was that there are literally a multitude of factors that determine the bioavailability of orally consumed steroids. Intestinal absorption usually refers to the process of uptake of a compound from the site of absorption into the systemic circulation. This process includes the penetration through the epithelial cells, metabolism in the epithelial cells and transfer from the epithelial cells into the portal vein or lymphatics. Any or all of these processes can significantly cause inhibition of absorption of the parent compound. I have heard for quite some time from various sources that methandrostenolone (Dianabol) works much better when taken orally than injected. I used to scoff at this but now I might be in a position to believe what I heard. You see, there is quite a bit of research which shows that anabolic steroids undergo significant metabolism in the epithelial cells. Consequently, ingested methandrostenolone, as well as other orally administered steroids, could possibly be significantly converted into other active species with highly different characteristics before it even reaches the liver!
In the magazines and advertisements, we hear all the time that taking so and so amount of prohormone will give you thus and thus blood levels of that particular steroid. They base this simply by saying that a certain predefined percentage makes it through unmetabolized by the liver. They do not consider the facts that a great amount might not get absorbed by the epithelial cells nor do they take into consideration the fact that much might get metabolized into either more or less active species. Basically, the whole situation is quite complex and cannot be simplified with such a sophomoric formula.
I also want to bring up the point again of how important it is to have a proper delivery system to cause increased penetration/absorption in the epithelial cells. I dug up a bunch of research which shows that without any type of delivery system as much as 50% of the ingested steroid can be unabsorbed. You can guess what happens to this unabsorbed steroid! Into the toilet my friend; into the toilet!!!
After Shionogi showed that steroidal ethers are absorbed in the lymphatic system, they did a series of studies which determined exactly what was responsible for lymphatic versus portal partitioning. Please understand that when the steroid is absorbed into the epithelial cell it is PARTITIONED or directed into either the portal vein or the lymphatic system. I already know what you are asking, ?What determines the partitioning??
It is a phenomenon called SUPERLIPOPHILICITY! If you remember correctly fatty acids and triglycerides are almost completely absorbed into the lymph. Superlipophilicity makes the compound associate so strongly with triglycerides and fatty acids that it absorbs in a similar fashion. During absorption, superlipophilic compounds become incorporated into the core lipids of chylomicrons in the intestinal mucosal cells of the intestinal mucosa. These fatty chylomicrons are then transferred almost exclusively into the lymphatic system (including the steroidal ethers).
I had read something about this on another site also. I was wondering what the effects on the lymphatic system would be after, say, a six week cycle?, or maybe even four weeks?!