One of the areas of medicine in particular that has seen a lot of progress is the field of breast cancer treatment. Researchers here focus heavily on the reduction of estrogenic activity in the body, as estrogen inhibition can help the disease by starving breast cancer cells that are responsive to this hormone. Their work has spawned several new commercial drug products that are very effective in this regard. Since anti-estrogenic drugs are also widely used by bodybuilders for side-effect mitigation and as hardening/cutting aids, I thought it would be of interest to take a look at a few of the new drugs that have hit the market in recent years. In think you’ll find that the agents discussed here not only hold a great deal of promise, but may even bring us to places that the old-standard anti-estrogens simply could not.
Fareston (toremifene citrate)
Fareston is an estrogen receptor antagonist with mixed agonist/antagonist properties. It’s classified as a “SERM,” which is short for Selective Estrogen-Receptor Modulator. It is specifically a nonsteroidal triphenylethylene derivative, similar in structure and action to both Nolvadex (tamoxifen citrate) and Clomid (clomiphene citrate). Fareston is used for the treatment of breast cancer in postmenopausal women with estrogen-receptor positive or estrogen-receptor unknown (unsure if the cancer is estrogen responsive) tumors. It works by attaching to the estrogen receptor in various tissues, blocking endogenous estrogen from exerting biological activity. This agent in the newest mixed estrogen receptor agonist/antagonist to get our attention in the bodybuilding world, and was approved by the FDA in 1997.
Like Nolvadex, Fareston has an added benefit of being somewhat intrinsically estrogenic in the liver. This allows it to support positive changes in serum cholesterol values, an effect tied to estrogenic activity. It may turn out, however, that Fareston is the measurably better agent of the two in this regard. One study, for example, compared the lipid altering effects of tamoxifen and toremifene in a group of 49 postmenopausal women. Standard oral doses of either tamoxifen (20 milligrams) or toremifene (60 milligrams) were given to the patients for a period of three years.
Both antiestrogens caused a significant reduction in serum total and LDL (bad) cholesterol levels, however the change in HDL/LDL ratio (the more important measure) was much more favorable with the Fareston group. This drug caused an increase in HDL cholesterol levels by 14 percent, whereas tamoxifen use in this case actually decreased HDL values by five percent. In the end, the toremifene group noted much more favorable changes in serum lipid profiles and cardiovascular disease risk. It may turn out to be that Fareston is the antiestrogen of choice for the heart-conscious athlete.
Faslodex (fulvestrant)
Faslodex is one of the newest weapons in the war on estrogen, approved by the FDA in 2002 for the treatment of estrogen receptor positive breast cancer. It’s a highly selective estrogen receptor antagonist (it’s also classified as an estrogen receptor downregulator). This means it does not target the production of estrogen, but like Nolvadex and Clomid, prevents this hormone from being able to exert activity in the body by blocking available receptors. Faslodex seems well equipped to compete with even some of the newer aromatase inhibitors. One study, for example, shows Faslodex to be as effective in Arimidex in treating breast cancer patients who have already failed with first line endocrine treatments. Another shows the drug to prevent tumor cell turnover and growth significantly more effectively than tamoxifen citrate. Studies investigating the physiological response to Faslodex made note that its strong actions allow it to downregulate estrogen receptor concentrations, and progesterone receptor concentrations as well. Clearly, when it comes to anti-estrogens, Faslodex is far more advanced than the “standard-issue” agents we have been using in the bodybuilding world for years.
There are only two real drawbacks to Faslodex. For one, it’s a pure estrogen receptor antagonist, not a mixed agonist/antagonist. This makes is quite different from Nolvadex or Clomid, drugs that actually tend to improve serum cholesterol values because they act as estrogens in certain tissues like the liver. Although I have been unable to find studies looking at cholesterol levels in response to Faslodex, knowing how closely tied estrogen is to the synthesis of HDL cholesterol, I can only assume it will have as strong an influence (negative) here as do aromatase inhibitors.
The other major problem is price. A single five milliliter injection runs over $900 at the pharmacy. I guess when you make a medicine that people are only going to need once per month, you aren’t going to make millions on it if you sell it for $50. Mind you, I have no knowledge of how costly this drug is to manufacture, but if I had to guess I would think the price has much more to do with how much the company thinks they should get from a patient on a monthly basis. Since it’s expensive, of course, there is little chance this drug will catch on with the bodybuilding public.
Aromasin (exemestane)
Aromasin is a steroidal suicide aromatase inhibitor, extremely similar in structure and action to formestane. It works to lower estrogen production in the body by blocking the aromatase enzyme, which is responsible for synthesizing estrogens. The FDA approved Aromasin in late 1999 for the treatment of advanced breast cancer, specifically in post-menopausal women whose disease has progressed following therapy with a first line agent such as tamoxifen. It’s given only to post-menopausal women because before menopause most of a woman’s estrogen comes directly from the ovaries, not aromatization (aromatase is the principle source of estrogen after menopause). Aromasin is being advertised as the only “aromatase inactivator” available, which ignores the fact that formestane is sold as an over-the-counter nutritional supplement in the U.S. right now. Although both these agents essentially do the same thing in the body, Aromasin does the job far more effectively.
Aromasin may be the most effective aromatase inhibitor available to date, in fact. While Arimidex boasts of estrogen suppression around 78 percent in its packaging insert, Aromasin reports it can lower estrogen as much as 85 percent on average. Feedback from bodybuilders tends to support the preference for Aromasin over other aromatase inhibitors, so this may very well be the case. Regardless of which one is the true “king,” all of the newer aromatase inhibitors— Arimidex, Femara, Aromasin— should be looked at as extremely effective for reducing estrogen synthesis in the body. A possible 10 percent difference in inhibition between the weakest and the strongest of the three is really not going to amount to all that much during your next cycle. If you are looking at one of these agents to prevent gynecomastia and help you lose fat and water on your next cycle, they are all going to do a good job for you. If you absolutely need the best agent, my money would be on this one.
Black Market Update
Weratestone 250. This particular product contains testosterone enanthate, in a concentration of 250mg/ml. Weratestone is made by the French pharmaceuticals manufacturer Weimer Pharma, however it is not available for sale on the domestic prescription drug market in France. Instead, it is exported to French-speaking countries in Africa, such as Algeria, Zimbabwe and Mozambique. This steroid very rarely circulates in the United States, however it’s found from time to time in Western Europe. Testosterone enanthate is, of course, one of the most abundantly manufactured steroids worldwide. It’s also one of the most frequently counterfeited, and indeed many of the more popular brands in Europe, such as Testoviron, Primoteston and Testosteron Depot, are copied with alarming frequency. Although glass ampules such as the one Weratestone 250 comes in are by no means difficult to duplicate, the less than popular nature of this particular brand has kept it pretty low on the counterfeiters’ radar. So long as your source is otherwise reliable, you can probably trust this item when located.
Shown also this month is a counterfeit vial of nandrolone decanoate that’s supposed to originate in Russia. It is listed to contain the steroid in a concentration of 200mg/ml, and holds a nicely sized 10ml volume of oil. Farmadon, who is labeled to have made the drug, was a real company operating in the steroid business at one time. It has been closed for a couple of years, however, and definitely did not make this product. When it did make anabolic steroids, it packaged them in very odd, tall and thin glass ampules, not 10ml multi-dosed (American-style) vials like this. It appears that an underground manufacturer, who is believed to be in Russia, has simply taken up the abandoned name and started producing a number of different products including this Deca, nandrolone phenylpropionate, testosterone enanthate, testosterone propionate, and a Sustanon clone. The contents of these products have not yet been verified, but judging by the positive feedback, they probably do contain some amount of real steroid. –WL
source:musculardevelopment.com
