Formasin(????) Formastane(Bill L.)/4-hydroxyandrostenedione or 6OXO(Patrick Arnold)/3,6,17-androstenetrione
Formasin
<P id=details1>Prototype Nutrition introduces a powerful anti-estrogen to the market in their product Formasin™, which contains the suicide aromatase inhibitor formestane (4-hydroxyandrostenedione). Formestane has been shown to be far more potent than any existing anti-estrogen supplement (5-alpha-androstanedione, chrysin, etc). Formasin™ contains the only active ingredient proven by numerous placebo-controlled human medical studies, which is effective enough to battle breast cancer via perscription in numerous foriegn countries.
<B>Suicide Inhibitor </B>
Formasin works by attaching to the active binding site of the aromatase enzyme, and hence, preventing the receptor from converting other androgens to estrogen. With the aromatase enzyme binding site occupied, the receptor becomes inactive. Because of this, formestane will dramatically suppress estrogen concentrations if it is present in a high enough concetration in the blood. Unlike existing inhibitors, Formasin™ binds permanently with the aromatase enzyme, rendering it useless until the body actually replaces it. Therefore, formestene is called a suicide or irreversible aromatase inhibitor; it also is both highly selective in its action on estrogen and has a long-lasting in effect.
Formestane has successfully treated breast cancer patients in many countries including Germany, England, Switzerland, Australia, Spain, New Zealand, and Italy. After tamoxifen, an estrogen receptor antagonist, has failed to elicit a positive response, formestane has been shown to be an effective option that produces a response statistically similar to tamoxifen. Now, atheletes who would like to hinder the actions of estrogen can use a substance so powerful that it is often obtained through a prescription.
<B>Dosage and Effects </B>
Peak levels of 4-hydroxyandrostenedione are detected in the blood at approximently an hour and a haf after oral administration, and the substance ellicits a half-life of approximately 3 hours. Because it is an irreversible inhibitor, the estrogen-suppressing activity outlives the actual presence in the bloodstream. It has been shown that maximum estrogen suppression is achieved with an oral dose of only 250mg a day. An increase in this dose does not cause any significant rise in inhibition.
<B>Estrogen Maintenance In Men </B>
Estrogen increases muscle glucose utilization, supports HDL cholesterol, and even increases androgen receptor concentrations. In contrast to past beliefs, estrogen serves many useful purposes in men and is particularly important in rapid muscle mass gain. Hence, those bulking would not immediately need estrogen maintenance compounds until post-cycle. Aside from the numerous benefits of estrogen, there still remains a long list of negative effects. Firstly, estrogen increases water retention and fat buildup, which can hide muscle definition. Estrogen can also promote the development of female breast tissue (gynecomastia) in men. When dieting and cutting are goals, or when there is a potential for gynecomastia development, it is often beneficial to maximize the ratio between androgens and estrogens.
<B>Anabolic Stimulation </B>
Formestane has been shown to be lesser prohormone to the anabolic steroid 4-hydroxytestosterone; aside from aromatase inhibitition, 4-hydroxyandrostenedione also has notable testosterone stimulating properties. Although this conversion rate is low, it is greatly amplified by its ability to inhibit estrogen. By doing so, the testosterone-suppressive signal estrogen sends to your brain is greatly reduced, thus increasing testicular output of testosterone. It has been demostrated by in-vivo human studies that 4-hydroxyandrostenedione will suppress estrogen levels to such a point that they were not high enough to suppress gonadotropins [1]. An amount of only 250mg to 500mg of formestane injected every 2 weeks, or oral doses as high as 1000mg daily, have not shown any significant testosterone suppressive effect [2]. When given to men in oral doses as high as 500mg, there has been a great increases in serum testosterone concentrations [3 4 5].
<B>Post-Cycle Estrogen Maintenence </B>
Formasin™ can offer a very unique additional benefit, when used during the recovery window after a cycle of androgens. At this time, one must minimizw post-cycle hypoandrogenic state by restoring the natural production of testosterone. Often, some type of anti-estrogen is used to accomplished the stated task. Since Formasin™ is also converts to 4-hydroxytestosterone, it allows for continued supplementation of androgens during this window, while also suppressing estrogen. Normally, androgens are usually suppressive towards testosterone production. However, with Formasin, its weak androgenic activity is compensated for by its estrogen suppression. Hence, it can basically serve as a small bridge to full testosterone recovery. Other aromatase-inhibitors cannot offer this anabolic stimulation.
<B>Supplement Facts</B>
90 Capsules per Container
Amount per Serving
4-hydroxyandrostenedione 50mg
<B>Directions: </B>
Take 1-5 capsules per day, depending on the level of effect desired. Do not exceed 12 weeks of continuous use. Not recommended for women, especially if pregnant or nursing. Consult your doctor before using if you have or at risk for high blood pressure, heart disease, diabetes or are taking any medications. This product is not intended to treat, cure, prevent or diagnose any disease.
<B>References: </B>
[1] Aromatase inhibitors and hormone-dependent cancers. Brodie AM, Banks PK, Inkster SE, Dowsett M, Coombes RC. J Steroid Biochem Mol Biol 1990 Nov 20;37(3):327-33
[2] Dose-related endocrine effects and pharmacokinetics of oral and intramuscular 4-hydroxyandrostenedione in postmenopausal breast cancer patients. Dowsett M, Cunningham DC et al. Cancer Res 1989 Mar 1;49(5):1306-12
[3] Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men. Dowsett M, Lloyd P. Cancer Chemother Pharmacol 1990;27(1):67-71
[4] Pharmacokinetics of 4-hydroxyandrostenedione in man after intramuscular injection of different formulations and the effect of this drug on plasma aromatizable androgens and 17beta-estradiol concentrations. Danza G, Muratori M, Guarna A, Occhiato EG, Sadri R, Serio M. J Steroid Biochem Mol Biol 1993 Sep;46(3):373-9
[5] Aromatase inhibition: 4-hydroxyandrostenedione (4-OHA, CGP 32349) in advanced prostatic cancer. Davies JH, Dowsett M, Jacobs S, Coombes RC, Hedley A, Shearer RJ. Br J Cancer 1992 Jul;66(1):139-42
Formasin
<P id=details1>Prototype Nutrition introduces a powerful anti-estrogen to the market in their product Formasin™, which contains the suicide aromatase inhibitor formestane (4-hydroxyandrostenedione). Formestane has been shown to be far more potent than any existing anti-estrogen supplement (5-alpha-androstanedione, chrysin, etc). Formasin™ contains the only active ingredient proven by numerous placebo-controlled human medical studies, which is effective enough to battle breast cancer via perscription in numerous foriegn countries.
<B>Suicide Inhibitor </B>
Formasin works by attaching to the active binding site of the aromatase enzyme, and hence, preventing the receptor from converting other androgens to estrogen. With the aromatase enzyme binding site occupied, the receptor becomes inactive. Because of this, formestane will dramatically suppress estrogen concentrations if it is present in a high enough concetration in the blood. Unlike existing inhibitors, Formasin™ binds permanently with the aromatase enzyme, rendering it useless until the body actually replaces it. Therefore, formestene is called a suicide or irreversible aromatase inhibitor; it also is both highly selective in its action on estrogen and has a long-lasting in effect.
Formestane has successfully treated breast cancer patients in many countries including Germany, England, Switzerland, Australia, Spain, New Zealand, and Italy. After tamoxifen, an estrogen receptor antagonist, has failed to elicit a positive response, formestane has been shown to be an effective option that produces a response statistically similar to tamoxifen. Now, atheletes who would like to hinder the actions of estrogen can use a substance so powerful that it is often obtained through a prescription.
<B>Dosage and Effects </B>
Peak levels of 4-hydroxyandrostenedione are detected in the blood at approximently an hour and a haf after oral administration, and the substance ellicits a half-life of approximately 3 hours. Because it is an irreversible inhibitor, the estrogen-suppressing activity outlives the actual presence in the bloodstream. It has been shown that maximum estrogen suppression is achieved with an oral dose of only 250mg a day. An increase in this dose does not cause any significant rise in inhibition.
<B>Estrogen Maintenance In Men </B>
Estrogen increases muscle glucose utilization, supports HDL cholesterol, and even increases androgen receptor concentrations. In contrast to past beliefs, estrogen serves many useful purposes in men and is particularly important in rapid muscle mass gain. Hence, those bulking would not immediately need estrogen maintenance compounds until post-cycle. Aside from the numerous benefits of estrogen, there still remains a long list of negative effects. Firstly, estrogen increases water retention and fat buildup, which can hide muscle definition. Estrogen can also promote the development of female breast tissue (gynecomastia) in men. When dieting and cutting are goals, or when there is a potential for gynecomastia development, it is often beneficial to maximize the ratio between androgens and estrogens.
<B>Anabolic Stimulation </B>
Formestane has been shown to be lesser prohormone to the anabolic steroid 4-hydroxytestosterone; aside from aromatase inhibitition, 4-hydroxyandrostenedione also has notable testosterone stimulating properties. Although this conversion rate is low, it is greatly amplified by its ability to inhibit estrogen. By doing so, the testosterone-suppressive signal estrogen sends to your brain is greatly reduced, thus increasing testicular output of testosterone. It has been demostrated by in-vivo human studies that 4-hydroxyandrostenedione will suppress estrogen levels to such a point that they were not high enough to suppress gonadotropins [1]. An amount of only 250mg to 500mg of formestane injected every 2 weeks, or oral doses as high as 1000mg daily, have not shown any significant testosterone suppressive effect [2]. When given to men in oral doses as high as 500mg, there has been a great increases in serum testosterone concentrations [3 4 5].
<B>Post-Cycle Estrogen Maintenence </B>
Formasin™ can offer a very unique additional benefit, when used during the recovery window after a cycle of androgens. At this time, one must minimizw post-cycle hypoandrogenic state by restoring the natural production of testosterone. Often, some type of anti-estrogen is used to accomplished the stated task. Since Formasin™ is also converts to 4-hydroxytestosterone, it allows for continued supplementation of androgens during this window, while also suppressing estrogen. Normally, androgens are usually suppressive towards testosterone production. However, with Formasin, its weak androgenic activity is compensated for by its estrogen suppression. Hence, it can basically serve as a small bridge to full testosterone recovery. Other aromatase-inhibitors cannot offer this anabolic stimulation.
<B>Supplement Facts</B>
90 Capsules per Container
Amount per Serving
4-hydroxyandrostenedione 50mg
<B>Directions: </B>
Take 1-5 capsules per day, depending on the level of effect desired. Do not exceed 12 weeks of continuous use. Not recommended for women, especially if pregnant or nursing. Consult your doctor before using if you have or at risk for high blood pressure, heart disease, diabetes or are taking any medications. This product is not intended to treat, cure, prevent or diagnose any disease.
<B>References: </B>
[1] Aromatase inhibitors and hormone-dependent cancers. Brodie AM, Banks PK, Inkster SE, Dowsett M, Coombes RC. J Steroid Biochem Mol Biol 1990 Nov 20;37(3):327-33
[2] Dose-related endocrine effects and pharmacokinetics of oral and intramuscular 4-hydroxyandrostenedione in postmenopausal breast cancer patients. Dowsett M, Cunningham DC et al. Cancer Res 1989 Mar 1;49(5):1306-12
[3] Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men. Dowsett M, Lloyd P. Cancer Chemother Pharmacol 1990;27(1):67-71
[4] Pharmacokinetics of 4-hydroxyandrostenedione in man after intramuscular injection of different formulations and the effect of this drug on plasma aromatizable androgens and 17beta-estradiol concentrations. Danza G, Muratori M, Guarna A, Occhiato EG, Sadri R, Serio M. J Steroid Biochem Mol Biol 1993 Sep;46(3):373-9
[5] Aromatase inhibition: 4-hydroxyandrostenedione (4-OHA, CGP 32349) in advanced prostatic cancer. Davies JH, Dowsett M, Jacobs S, Coombes RC, Hedley A, Shearer RJ. Br J Cancer 1992 Jul;66(1):139-42