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  1. #1
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    Aromasin~Exemestane

    Aromasin

    (Exemestane)


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    Aromasin is a steroidal aromatase inactivator used to lower circulating estrogen. It was developed to help fight breast cancer as estrogen plays a role in the growth of cancer cells. Aromasin binds irreversibly to the aromatase enzyme. This suppresses the conversion of androgens into estrogen. Circulating estrogen can be reduced by nearly 85% in women using Aromasin. A common misconception is that aromatase inhibition is similar in men than women. However in trials when males were administered 25mg of Aromasin daily, maximal estradiol suppression of 62% +/- 14% was observed at 12 hours. The reason for the difference may be related to the much higher testosterone concentrations in young males than in postmenopausal women and the shorter half-life of exemestane in males. The terminal half-life in males (8.9 h) was considerably shorter than the published value of 27 h in females. This may be a basis for more frequent administration in men (or women administering testosterone) that want maximal E2 supression.

    Aromasin acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogens. When we compare this mode of action against other AI's the benefit becomes clear. Arimidex can unbind from the aromatase enzyme when you stop taking it but Aromasin will not. Therefore, there is less chance of estrogen rebound with Aromasin.

    Aromasin can be employed during a steroid cycle when aromatizing compounds such as testosterone are administered in order to control estrogen from getting out of control. During the course of a typical steroid cycle estrogen can rise quite high. Estrogen has been measured as much as 7 times higher than normal in men using steroids. This is excessive and can potentially cause water retention, gynecomastia (the formation of female breast tissue), negatively effect libido or cause benign prostatic hyperplasia. Therefore in order to avoid these side effects estrogen must be controlled.

    Aromasin not only lowers circulating estrogen and sex hormone binding globulin but it also increases free testosterone by a whopping 117%! Total testosterone increases about 60%. Check out the performance of Aromasin after just 10 days of treatment in males.


    FIG. 1. Estrogen and androgen plasma levels after 10 d of daily exemestane (25 or 50 mg) in healthy young males (mean +/- SD; n = 9?11). To convert to Systeme International units: estradiol, picomoles per liter (x3.671); estrone, picomoles per liter (x3.699); androstenedione, nanomoles per liter (*0.003492); and testosterone, nanomoles per liter (x0.03467).

    Aromasin may be used during a steroid cycle with aromatizing compounds and during PCT to help keep the estrogen to testosterone balance in favor of testosterone. Out of all the medications to control estrogen, Aromasin seems to be the most well balanced. It raises testosterone similar to Arimidex and lowers estradiol about 10% better than arimidex in males and is likely to cause less estrogen rebound than Arimidex. Keep in mind that 50mg of Aromasin daily kept estradiol in the normal range for men so if you think using an aromatase inhibitor will crush estrogen too much this science supports the opposite. Additionally, plasma lipids and IGF-I concentrations in men were unaffected by Aromasin treatment. From the data I have read and my years of experience with this medication, 25mg of Aromasin every other day is a good starting point on moderate doses of testosterone. If testosterone doses are raised then 25mg daily may be needed to control estrogen. Since either high and low estrogen can cause side effects such as low libido only labs can determine the appropriate dose of Aromasin.

    Reference

    Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males

    ~heavyiron
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    Used this myself. It's definitely good to go.


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    Thanks for the read heavy, using aromasin currently during pct alongside clomid.

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    Attention Steroid Users:


    As most of you know, AAS can adversely affect the lipid profile, potentially causing severe flucuations in this important health marker and accutely increasing heart attack risk. Even without AAS, many Americans are already suffering the injurious effects of poor lipid values through diet alone. With 2 risk factors already stacked against us, it would be foollish to use any other substances capable of causing further damage to this aspect of our cardiovascular health. Unfortunately, that is exactly what many steroid users are doing.

    While useful for lowering estrogen into a normal range, older anti-estrogenic drugs, such as A-dex and Letro, are notorious for disturbing the lipids--often quite significantly. However, we do not have to choose between elevated estrogen and altered lipids. With Aromasin, we can control our estrogen levels without the fear of adversely affecting our lipids. This is a huge benefit for steroid users and one you should not take lightly. With Aromasin costing roughly the same as other AI's, deciding which to choose should be a no-brainer.

    I have been using Aromasin exclusivley for a few years now and not only do my estrogen levels remain within the normal range, but I am no longer struggling to control my cholesterol. Aromasin assuredly played a significant role in this. The next time you need to pick up an AI, consider Aromasin. Superior Hardcore Peptides carries this AI, but unlike most other peptide companies, you can be 100% sure that you are getting what you pay for when you purchase from Hardcore. Just like with IML products, all of Hardcore's products are also 3rd party lab tested for purity & potency, assuring the highest quality product available....and none of the Chinese stuff, guys...these products are made right here in the U.S.
    Last edited by Mike Arnold; 04-26-2014 at 09:41 PM.
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    I have been going back and forth between adex and aromasin over the years not really sure which one I like better . But hearing that aromasin doesn't kill your lipids nails it for me . Wish I hadn't just bought a whole bottle of adex last week , lol. Also I had read in the past that aromasin actually raised IGF-1 levels but you are saying it doesn't affect them either way ?

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    Quote Originally Posted by l69lou View Post
    I have been going back and forth between adex and aromasin over the years not really sure which one I like better . But hearing that aromasin doesn't kill your lipids nails it for me . Wish I hadn't just bought a whole bottle of adex last week , lol. Also I had read in the past that aromasin actually raised IGF-1 levels but you are saying it doesn't affect them either way ?
    Not only does it not mess up your lipids like A-dex, but neither does it cause estrogen rebound. Since A-dex does not permanently deactivate estrogen, as soon as you stop taking it the estrogen that is currenty bound to A-dex will be released back into free circulation as soon as its active life expires.
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  8. #8
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    Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males

    Nelly Mauras, John Lima, Deval Patel, Annie Rini, Enrico di Salle, Ambrose Kwok, andBarbara Lippe
    DOI: http://dx.doi.org/10.1210/jc.2003-031279
    Received: July 23, 2003
    Accepted: September 10, 2003
    Published Online: July 02, 2013

    Abstract

    Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P ≤ 0.002); 50 mg, 32% (P ≤ 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P ≤ 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 + or - 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.








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    Great read

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    Good stuff!

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    For someone who's e2 was 51 on 120mg a week of trt cyp and started forming gyno, do you think aromasin would be strong enough to keep my e2 under 40 on 500mgs a week. I know its impossible to say but clearly I'm extremely gyno sensative and wondering if I should start my first cycle with a stronger AI knowing that at only 52 on a 15-42 scale I form Gyno and get itchy nips

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    I've kept E2 below 40 on 500mgs of test a week with Aromasin. This was proven via blood work. Now I'm probably not as sensitive as you are but that could be offset with a higher dose.

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    Cool thanks. Also if someone were to take 37.5mg a day(1.5 pills) would you reccomend half a pill 3x a day or a full pill, then 8 hours later a half pill. Curious if the higher dose at once is needed to keep e2 lower or a smaller dose more frequently will do the same

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    Quote Originally Posted by Machmood View Post
    Cool thanks. Also if someone were to take 37.5mg a day(1.5 pills) would you reccomend half a pill 3x a day or a full pill, then 8 hours later a half pill. Curious if the higher dose at once is needed to keep e2 lower or a smaller dose more frequently will do the same
    Dosing Aromasin 2X daily will maintain more even clood levels of the drug, as Aromasin has a relatively short actve life compared to something like A-dex or letro. Still, many take it only once daily and do fine.
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    I heard that Aromasin is Estrogen killer, without rebound effect. It take few days to ( 3-4 days ) to back with main Estrogen level so people can keep estro on Aromasin even with e3d/e4d dosage.

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    placed an order !

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