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Product description*
Molecular Nutrition, the company that introduced the first steroidal aromatase inhibitor to the sports supplement market just a year ago, has teamed up with Syntrax Innovations to bring the war on estrogen to a close, once and for all. Formastat™ contains the suicide aromatase inhibitor formestane (4-hydroxyandrostenedione), a clinically proven anti-estrogen exceedingly more potent than any supplement to come before it. 6-oxo-androstenedione, chrysin, indole-3-carbinol, calcium d-glucarate, trihydroxystilbene, not even our old Viratase (5-alpha-androstanedione) can come close. All of them combined in one capsule still wouldn't even have a shot. Formastat™ is such a revolutionary advance in the area of estrogen suppression because it contains the only agent backed by not one but numerous placebo-controlled human medical studies, and so effective it is actually a prescription breast cancer drug in other countries.
Suicide Aromatase Inhibitor
Formastat is in many regards similar to a competitive steroidal aromatase inhibitor like Viratase. Both are steroidal compounds that work by attaching to the active binding site of the aromatase enzyme, preventing it from interacting with other steroids (such as testosterone) that are capable of being converted to estrogen. With the enzyme binding site occupied, it is for all intents and purposes inactive. If the inhibitor is present in a high enough level it will dramatically suppress estrogen concentrations in the blood. The difference between a competitive inhibitor like Viratase, and Formastat, is that the former will detach after some time, rendering the enzyme active again. Formastat on the other hand binds permanently with the aromatase enzyme, making it useless until the body actually replaces it through the normal metabolic attrition of enzymes. This type of compound is called a suicide or irreversible aromatase inhibitor, and has the benefit of being both highly selective in its action on estrogen and long-lasting in effect.
Because of its potent estrogen-suppressing action, 4-hydroxyandrostenedione has been successfully used on breast cancer patients in many other countries including England, Germany, Switzerland, Spain, Australia, New Zealand, Italy and Malaysia It has been shown to be an effective option as a second line of defense after tamoxifen, an estrogen receptor antagonist, has failed to elicit a positive response with patients, and to produce an overall response statistically similar to tamoxifen when administered as the first-line therapy . Those of us in the bodybuilding world looking to mitigate the physiological effects of estrogen for other purposes have likewise been confronted for the first time with a legal supplement that has all the actions and potency of a pharmaceutical agent, which would normally be obtained only with a doctor's prescription! .
Dose and Pharmacokinetics
After oral administration peak levels of 4-hydroxyandrostenedione are reached in the blood at approximately 1.5 hours , and the drug is cleared from the body with a half-life of approximately 3 hours . Due to its nature as an irreversible inhibitor, its estrogen-suppressing activity outlives it actual active lifespan in the bloodstream. Studies have demonstrated that maximum estrogen suppression is achieved with an oral dose of only 250mg per day . Doubling this dose to 500mg, or even quadrupling it to 1000mg, was shown to have no effect on aromatase inhibition or estrogen levels appreciably different from the 250mg dose.
The Need for Estrogen Maintenance
Estrogen has both positive and negative effects that you should be aware of. On the positive it supports "good" high density cholesterol, increases muscle glucose utilization for tissue growth and repair, and even increases androgen receptor concentrations in various tissues. It is now understood that estrogen serves many useful purposes in men, particularly if we are looking for rapid muscle mass gain. If bulk is the goal it is therefore usually advised to hold off on estrogen maintenance compounds until there is a clear need for them. This brings us to the negative side of estrogen, namely that it can work to hide muscle definition by increasing water retention and fat buildup. It can also promote gynecomastia (the development of female breast tissue) in men if levels get too high. Since androgens and estrogens playing opposing roles on the disposition of body fat and the growth of mammary tissues, maximizing the ratio between these two hormones is often an important objective, particularly at times when dieting and cutting are key goals or gynecomastia is a worry because strongly aromatized hormones such as testosterone are being supplemented.
Manufacturer
Molecular Nutrition
Packaged Weight: .6 Lbs.
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