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Aromasin - Exemestane
Chemical Name: Exemestane
Drug Class: Type-I Aromatase Inhibitor
The below article about Aromasin-Exemestane discusses how it works and gives a history of the drug. You can find articles about all of the steroids and other drugs listed on our site, including arimidex, dianabol, testosterone suspension, Letrozole, HGH [Human Growth Hormone] and nolvadex among many others. We are here to help you stay informed and updated on steroids and all other bodybuilding drugs.
Aromasin (Exemestane) is a Type-I aromatase inhibitor, or suicidal aromatase inhibitor. It???s called this because it lowers estrogen production in the body by attaching to the aromatase enzyme, and permanently deactivating it. (1)
Personally, I find this to be a very interesting mechanism of action when compared to type-II aromatase inhibitors, which bind competitively to the aromatase enzyme, and eventually unbind, rendering it active again. In the case of Aromasin, this doesn???t happen, and once it does its job on the enzyme, those particular enzymes will no longer function. Your body will eventually create more of the aromatase enzyme, so this isn???t dangerous, despite the really odd ???suicide??? thing in the first paragraph. As with all aromatase inhibitors, Aromasin was developed to fight breast cancer primarily in post-menopausal women, but we in the athletic community use it to combat estrogenic side effects from aromatizable steroids, or for post cycle therapy.
Estrogen is responsible for many of the effects we???re trying to avoid when we???re on a cycle, including excess water retention and development of gynocomastia (breast tissue development in males. Thus, limiting the conversion of testosterone into estrogen is of use for steroid using athletes, when they???re trying to avoid side effects. In this case, the advantage of using a suicidal aromatase inhibitor is that it really won???t cause much, if any, noticeable ???rebound??? in estrogen when you cease using it.
The hard numbers on Aromasin are reasonably impressive, as it averages an 85% rate of estrogen suppression (2), and this translates to an overall reduction in estradiol levels of about 50%(I believe this is overstated), as well as raising testosterone to a significant degree.(3).
It is also known as a ???steroidal??? aromatase inhibitor. This is really interesting, because it has been known to actually cause side effects (androgenic sides) that include increased aggressiveness and a pretty decent hardening effect. (4) I wouldn???t usually suggest that women should use Aromasin in large doses for any extended period of time, for this reason (possible virilization, or development of male sexual characteristics could occur with its use). It should, therefore, be reserved for use by women to brief periods of time in a possible pre-contest phase or for a form of post cycle therapy after a cycle.
Interestingly (and almost paradoxically) exemestane not only increases testosterone and lowers estrogen, but it also increases levels of insulin-like growth Factor (IGF). (5) I find this to be interesting, because although the rise in testosterone is most likely responsible for the increase in IGF levels, IGF is known to be an aggravating factor in the growth of breast tumors, like the kind found in breast cancer. However, since estrogen is the primary culprit in breast cancer, the large reduction in estrogen levels, even when combined with a rise in IGF, is enough to make Aromasin a very effective breast cancer medication. /div> Aromasin isn???t too harsh on blood lipids (6) (cholesterol), unlike some of the other AIs??? like Letrozole.
Exemestane reaches steady blood plasma levels of after a week of administration and this is also when we see it begin its maximal effect on reducing circulating estrogen levels. It???s also has a ½ life of 27 hours (4), so taking it once per day is going to build up blood plasma levels to a very effective level.
References:
1. A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.Br J Clin Pharmacol. 2005 Mar;59(3):355-64.
2. Eur. J. Cancer. 2000, May;36(8):976-82
3. The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956Copyright © 2003 by The Endocrine Society
4. Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S
5. Anticancer Res. 2003 Jul-Aug;23(4):3485
6. J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.
Aromasin (exemestane)
Exemestane is a steroidal suicide aromatase inhibitor. It isvery similar in structure and action to formestane, although it is significantly more potent in comparison. As a class of drugs, aromatase inhibitors offer an anti estrogenic effect by blocking the enzyme responsible for synthesizing estrogens. Exemestane is approved by the FDA for the treatment of breast cancer in women, specifically in post menopausal patients whose cancer has progressed following therapy with tamoxifen (nolvadex). Male bodybuilders and athletes often use the drug for non approved purposes, namely to counter the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids. This may include gynecomastia, fat buildup, and water retention. Exemestane is one of the most potent aromatase inhibitors presently available. The most commonly cited date reports a lowering of estrogen around 85% on average in clinical studies with women. Exemestane was developed by Pharmacia & Upjohn, which gained FDA approval for sale of the drug in late 1999. They introduced it under the Aromasin brand name in early 2000. Although the drug proved to be effective in doses as low as 2.5mg per day in some patients, the company developed it in a standard and near universally effective dosage of 25mg per tablet. The company has since introduced the drug to many other nations under the same trade name of Aromasin.
Aromasin, as it is most commonly called, is a very potent AI which works by blocking the aromatase enzyme in the body. This drug was originally developed to help fight breast cancer in women by reducing estrogen which some believe to aid in cancer cell growth. While not quite as strong as Letrozole, aromasin is considerably stronger than Anastrozole. Studies done with this substance typically show around an 85% reduction in estrogen levels in the body. This can be very useful to bodybuilders who are using aromatizing compounds such as testosterone. Typically, one will begin the use of aromasin the same day they begin their cycle. It is also important to note that Aromasin has shown to be very effective at increasing testosterone and IGF levels in the body. Because of this, this drug is also very useful during PCT regime when one is trying to restore natural testosterone levels in order to avoid a post cycle "crash". It is important to keep doses of aromasin reasonable, as too much estrogen suppression can result in hindered muscle gains and loss of sex drive. One 25mg tablet a day should be sufficient for effectively keeping estrogen related sides out of the picture, or for effectively raising natural testosterone levels during PCT.
Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose. The active life of the drug is between 24 and 30 hours. This is significant since it is quite shorter than for the non-steroidal inhibitors. A single oral dose of 25 milligrams of exemestane causes a relatively long-lasting reduction in plasma and urinary estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persists for about 4 to 5 days.It has been shown that 25 milligrams of exemestane is basically just as effective as 50 milligrams at suppressing estrogen, raising testosterone levels, and levels of IGF. It is therefore unnecessary to go higher in doses than 25 milligrams per day. Due to the active life of the compound exemestane should be administered roughly once every twenty-four hours. Users often start the drug on the first or second week of steroid use and continue to take it throughout the cycle and for a few weeks afterwards in order to prevent any type of estrogen rebound
Chemical Name: Exemestane
Drug Class: Type-I Aromatase Inhibitor
The below article about Aromasin-Exemestane discusses how it works and gives a history of the drug. You can find articles about all of the steroids and other drugs listed on our site, including arimidex, dianabol, testosterone suspension, Letrozole, HGH [Human Growth Hormone] and nolvadex among many others. We are here to help you stay informed and updated on steroids and all other bodybuilding drugs.
Aromasin (Exemestane) is a Type-I aromatase inhibitor, or suicidal aromatase inhibitor. It???s called this because it lowers estrogen production in the body by attaching to the aromatase enzyme, and permanently deactivating it. (1)
Personally, I find this to be a very interesting mechanism of action when compared to type-II aromatase inhibitors, which bind competitively to the aromatase enzyme, and eventually unbind, rendering it active again. In the case of Aromasin, this doesn???t happen, and once it does its job on the enzyme, those particular enzymes will no longer function. Your body will eventually create more of the aromatase enzyme, so this isn???t dangerous, despite the really odd ???suicide??? thing in the first paragraph. As with all aromatase inhibitors, Aromasin was developed to fight breast cancer primarily in post-menopausal women, but we in the athletic community use it to combat estrogenic side effects from aromatizable steroids, or for post cycle therapy.
Estrogen is responsible for many of the effects we???re trying to avoid when we???re on a cycle, including excess water retention and development of gynocomastia (breast tissue development in males. Thus, limiting the conversion of testosterone into estrogen is of use for steroid using athletes, when they???re trying to avoid side effects. In this case, the advantage of using a suicidal aromatase inhibitor is that it really won???t cause much, if any, noticeable ???rebound??? in estrogen when you cease using it.
The hard numbers on Aromasin are reasonably impressive, as it averages an 85% rate of estrogen suppression (2), and this translates to an overall reduction in estradiol levels of about 50%(I believe this is overstated), as well as raising testosterone to a significant degree.(3).
It is also known as a ???steroidal??? aromatase inhibitor. This is really interesting, because it has been known to actually cause side effects (androgenic sides) that include increased aggressiveness and a pretty decent hardening effect. (4) I wouldn???t usually suggest that women should use Aromasin in large doses for any extended period of time, for this reason (possible virilization, or development of male sexual characteristics could occur with its use). It should, therefore, be reserved for use by women to brief periods of time in a possible pre-contest phase or for a form of post cycle therapy after a cycle.
Interestingly (and almost paradoxically) exemestane not only increases testosterone and lowers estrogen, but it also increases levels of insulin-like growth Factor (IGF). (5) I find this to be interesting, because although the rise in testosterone is most likely responsible for the increase in IGF levels, IGF is known to be an aggravating factor in the growth of breast tumors, like the kind found in breast cancer. However, since estrogen is the primary culprit in breast cancer, the large reduction in estrogen levels, even when combined with a rise in IGF, is enough to make Aromasin a very effective breast cancer medication. /div> Aromasin isn???t too harsh on blood lipids (6) (cholesterol), unlike some of the other AIs??? like Letrozole.
Exemestane reaches steady blood plasma levels of after a week of administration and this is also when we see it begin its maximal effect on reducing circulating estrogen levels. It???s also has a ½ life of 27 hours (4), so taking it once per day is going to build up blood plasma levels to a very effective level.
References:
1. A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.Br J Clin Pharmacol. 2005 Mar;59(3):355-64.
2. Eur. J. Cancer. 2000, May;36(8):976-82
3. The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956Copyright © 2003 by The Endocrine Society
4. Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S
5. Anticancer Res. 2003 Jul-Aug;23(4):3485
6. J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.
Aromasin (exemestane)
Exemestane is a steroidal suicide aromatase inhibitor. It isvery similar in structure and action to formestane, although it is significantly more potent in comparison. As a class of drugs, aromatase inhibitors offer an anti estrogenic effect by blocking the enzyme responsible for synthesizing estrogens. Exemestane is approved by the FDA for the treatment of breast cancer in women, specifically in post menopausal patients whose cancer has progressed following therapy with tamoxifen (nolvadex). Male bodybuilders and athletes often use the drug for non approved purposes, namely to counter the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids. This may include gynecomastia, fat buildup, and water retention. Exemestane is one of the most potent aromatase inhibitors presently available. The most commonly cited date reports a lowering of estrogen around 85% on average in clinical studies with women. Exemestane was developed by Pharmacia & Upjohn, which gained FDA approval for sale of the drug in late 1999. They introduced it under the Aromasin brand name in early 2000. Although the drug proved to be effective in doses as low as 2.5mg per day in some patients, the company developed it in a standard and near universally effective dosage of 25mg per tablet. The company has since introduced the drug to many other nations under the same trade name of Aromasin.
Aromasin, as it is most commonly called, is a very potent AI which works by blocking the aromatase enzyme in the body. This drug was originally developed to help fight breast cancer in women by reducing estrogen which some believe to aid in cancer cell growth. While not quite as strong as Letrozole, aromasin is considerably stronger than Anastrozole. Studies done with this substance typically show around an 85% reduction in estrogen levels in the body. This can be very useful to bodybuilders who are using aromatizing compounds such as testosterone. Typically, one will begin the use of aromasin the same day they begin their cycle. It is also important to note that Aromasin has shown to be very effective at increasing testosterone and IGF levels in the body. Because of this, this drug is also very useful during PCT regime when one is trying to restore natural testosterone levels in order to avoid a post cycle "crash". It is important to keep doses of aromasin reasonable, as too much estrogen suppression can result in hindered muscle gains and loss of sex drive. One 25mg tablet a day should be sufficient for effectively keeping estrogen related sides out of the picture, or for effectively raising natural testosterone levels during PCT.
Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose. The active life of the drug is between 24 and 30 hours. This is significant since it is quite shorter than for the non-steroidal inhibitors. A single oral dose of 25 milligrams of exemestane causes a relatively long-lasting reduction in plasma and urinary estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persists for about 4 to 5 days.It has been shown that 25 milligrams of exemestane is basically just as effective as 50 milligrams at suppressing estrogen, raising testosterone levels, and levels of IGF. It is therefore unnecessary to go higher in doses than 25 milligrams per day. Due to the active life of the compound exemestane should be administered roughly once every twenty-four hours. Users often start the drug on the first or second week of steroid use and continue to take it throughout the cycle and for a few weeks afterwards in order to prevent any type of estrogen rebound
