Aromasin Overview & Features

Overview and History of Aromasin

Aromasin belongs to the category and class of drugs known as Aromatase Inhibitors (AIs).

Aromatase Inhibitors fall under a broader class of drugs known as anti-estrogens.

The other sub-category of drugs in the anti-estrogen classification are Selective Estrogen Receptor Modulators (SERMs), such as Nolvadex and Clomid.

Aromatase Inhibitors and SERMs make up the anti-estrogens.

Aromatase Inhibitors differ significantly from SERMs in their mechanism of action and how they address the issue of Estrogen control.

A significant misunderstanding has persisted for years within the anabolic steroid-using and bodybuilding community, though its explanation has become much clearer in the last 10-15 years.

It is a misconception and a myth that SERMs like Nolvadex and Clomid function to lower Estrogen levels.

This misunderstanding likely arose because SERMs are also referred to as ‘Estrogen blockers,’ leading many to misinterpret ‘blocking Estrogen’ as meaning ‘eliminating Estrogen,’ but this couldn’t be further from the truth.

SERMs only block the activity of Estrogen in certain tissues in the body by occupying the receptor sites in place of Estrogen, so that Estrogen itself cannot exert its effects at that site through receptor site binding, such as its action at receptor sites in breast tissue.

SERMs will also act as Estrogens at receptor sites in other cells in other areas of the body (such as in the liver, in the case of Nolvadex).

This is where the “selective” portion of ‘Selective Estrogen Receptor Modulator’ comes into play.

SERMs do not, however, lower circulating levels of Estrogen in blood plasma.

Aromatase Inhibitors are the compounds that serve this role by eliminating the production of Estrogen through binding to and disabling the aromatase enzyme, which is the enzyme responsible for the conversion (or aromatization) of androgens into Estrogen.

Aromasin is a very powerful and potent steroidal Aromatase Inhibitor of the suicidal type, and the package insert for Aromasin itself states that it is capable of reducing Estrogen levels by 85%, as demonstrated in studies on breast cancer patients.[1]

Suicidal Aromatase Inhibitors like Aromasin (Exemestane) act to permanently inhibit and disable the aromatase enzyme to which it is bound.[2]

This renders that enzyme molecule permanently inactive for good.

The body will eventually manufacture more aromatase enzymes, but the currently bound enzymes are bound indefinitely, eliminating the risk of Estrogen rebound.

This is unseen with the other two major Aromatase Inhibitors (Arimidex and Letrozole), which are non-suicidal Aromatase Inhibitors that are only bound to the aromatase enzyme for a limited time before they are metabolized and the Aromatase Inhibitor unbinds from the aromatase enzyme.

If non-suicidal Aromatase Inhibitors are discontinued too suddenly, the circulating inhibited aromatase enzymes that have not been metabolized out of the body will become free again to begin aromatizing androgens into Estrogen at a rapid rate.

This is not the case with Aromasin.

Exemestane was originally designed by Pharmacia & Upjohn for the purpose of treating female breast cancer patients, specifically post-menopausal patients, as an adjuvant therapy when other first-line breast cancer treatments (such as Nolvadex) have failed.

Shortly after its development, the FDA approved the use of Aromasin (Exemestane) on the prescription drug market in 1999 and began marketing under the brand name Aromasin in the year 2000.

Since its initial release, its use and sales have spread across the globe and it is used in nearly every country in the world.

Due to various patent and marketing/production-related laws, the only officially manufactured and sold Aromasin product is under the Aromasin brand name, and it is very widely available across the globe.

The standard dosage of Aromasin (Exemestane) is 25mg and it is marketed in 25mg tablets, although studies have shown that it is effective at doses as low as 2.5mg daily.

It stands to reason that the characteristics and effects of Aromasin would be helpful to the anabolic steroid using athlete for the purpose of Estrogen control.

Its use among anabolic steroid using athletes is for the control of nearly all Estrogen-related side effects: the manifestation of gynecomastia, water retention and bloating, and rising blood pressure (as a result of water retention increases from Estrogen).

This is in contrast with SERMs such as Nolvadex, which only serves to block gynecomastia.

Like many Aromatase Inhibitors, Aromasin has also demonstrated to increase endogenous Testosterone production levels in men, which will be covered in more detail later on in this profile.

Many anabolic steroid users and bodybuilders consider Aromasin to be far more effective and much more useful than Arimidex (due to its suicidal inhibition), though Arimidex is far more popular in the anabolic steroid using community today.

This is due to the fact that Arimidex was developed and released prior to Aromasin, and bodybuilders and athletes had caught on to it much quicker.

Aromasin (Exemestane) was, to a degree, overlooked and missed by many.

Things are changing today, as many are beginning to notice the superiority and advantages of Aromasin over Arimidex (which will be detailed throughout this profile).

Advantages that are not seen with other Aromatase Inhibitors include: its suicidal inhibition, its promotion of increases in IGF-1 (Insulin-like Growth Factor 1), its lack of incompatibility with other compounds (which is seen with other AIs), and its less negative impact on cholesterol profiles (which is seen with other AIs).

Aromasin Properties and Actions

Aromasin is a steroidal suicidal Aromatase Inhibitor.

This means that it possesses the characteristic four-ring cycloalkane carbon structure that all steroidal molecules have in common.

The fact that Exemestane is a steroidal Aromatase Inhibitor is a primary reason for why it is a suicidal Aromatase Inhibitor that permanently binds to the aromatase enzyme.

The aromatase enzyme is highly attracted to the steroidal structure of androgens (Testosterone), and the chemical structure of Aromasin serves to ‘trick’ the aromatase enzyme into binding with it, only to be inhibited/disabled.

Because the binding strength is so strong, this inhibition on the part of the Aromasin to the aromatase enzyme that it binds to is permanent.

A similar steroidal Aromatase Inhibitor, Formestane, exhibits the exact same property (though it is much weaker and less potent in comparison to Aromasin).

This is why there is absolutely no risk of Estrogen rebound upon sudden cessation of Aromasin administration.

The other two major Aromatase Inhibitors (Arimidex and Letrozole) are non-steroidal AIs and are therefore associated with the risk of Estrogen rebound following their discontinuation.

This is because they are not structurally similar to the aromatase enzyme’s target hormones, unlike Aromasin.

Aromasin is very effective at reducing Estrogen, with 25mg daily having previously demonstrated its effectiveness at reducing circulating serum Estrogen levels in the body by 85%.

As with other secondary breast cancer treatments, Aromasin is very effective at lowering Estrogen levels by inhibiting the aromatase enzyme, which is why, like Arimidex, it is only administered to post-menopausal women or in cases where other first-line breast cancer treatments have failed.

This is because post-menopausal women experience very different shifts in hormone levels and endocrine function compared to pre-menopausal women.

Arimidex and Letrozole are both classified as non-steroidal and non-suicidal Aromatase Inhibitors that compete with the substrate for binding to the active site of the enzyme.

This is very different from Aromasin (Exemestane), which is a mechanism-based steroidal and suicidal Aromatase Inhibitor that mimics the substrate and is converted by the enzyme to a reactive intermediate, which then inactivates the aromatase enzyme.[3]

To explain this in layman’s terms, this means that Aromasin’s chemical structure is similar to the traditional ‘target’ that aromatase binds to (e.g. Testosterone), and that it essentially ‘tricks’ the aromatase enzyme into binding with it, only to be inhibited/disabled.

Because the binding strength is so strong, this inhibition on the part of the Aromasin to the aromatase enzyme that it binds to is permanent.

Arimidex and Letro, being non-suicidal AIs, compete with the enzyme’s traditional ‘targets’ instead of being guaranteed a permanent spot (this is an advantage that Aromasin holds over the other two).

Athletes, bodybuilders, and anabolic steroid using individuals will favor Aromasin as an Aromatase Inhibitor for its usefulness in reducing, mitigating, and preventing Estrogenic side effects.

These side effects are the result of aromatizable androgens (such as Testosterone) converting (or aromatizing) into Estrogen, which results in Estrogen levels in the body rising far above normal physiological levels.

Aromasin (Exemestane) is very beneficial and highly favored among anabolic steroid users because it eliminates the rising Estrogen level issue at its root cause.

By binding to and inhibiting/disabling the aromatase enzyme, supra-physiological levels of aromatizable androgens (such as Testosterone, Dianabol, Boldenone, etc.) cannot convert into Estrogen, thus eliminating the risk of Estrogen-related side effects.

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Aromasin Side Effects

Aromasin is known to be relatively well-tolerated by most users.

However, it is not without its potential side effects, and there are a few side effects of concern.

These are generally the result of Estrogen levels decreasing too much or too quickly, or Estrogen being suppressed for too long.

It is also important to understand that the use of Aromasin (or any Aromatase Inhibitor) will present a larger side effect profile in women than in men.

The first Aromasin side effects an individual will experience are joint and/or bone pain.

This is due to the fact that Estrogen plays an important and significant role in maintaining proper mineralization and bone density within bone tissue.

Although this is characteristic of all Aromatase Inhibitors, Aromasin has actually been shown in studies to strengthen bone tissue to some degree, whereas AIs like Arimidex (Anastrozole) or Letrozole (Femara) have been shown to severely reduce it.

Lethargy and fatigue are frequently reported side effects of Aromasin and all other AIs.

Estrogen plays a key role in the central nervous system (CNS), and any compound that drives Estrogen levels too low can induce routine chronic fatigue.

Restoration of Estrogen levels to normal physiological levels will alleviate this side effect.

Negative cholesterol changes are another significant risk with the use of any AI, and Aromasin is no exception.

Because Estrogen plays an important role in the maintenance and management of proper cholesterol health, its severe reduction can have a negative impact on LDL and HDL values.

However, studies have demonstrated that Aromasin has less of a negative impact than other Aromatase Inhibitors.

The risk is still present, however, and regular checkups and blood work should be performed.

The only Aromasin side effects that could be considered unique to Aromasin are the potential for androgenic side effects.

This may be due to the fact that Aromasin is itself an androgenic steroid in its structural nature.

Androgenic side effects can and do include: increased oily skin (and acne as a result), increased facial and body hair growth, and the triggering of Male Pattern Baldness (MPB) if the genetic trait for it exists.

A noticeable increase in aggression and drive can also be experienced with Aromasin use, though not to the degree of powerful androgens such as Masteron (Drostanolone).

Aromasin Dosing and Administration

Medically, Aromasin is used as a secondary treatment for post-menopausal breast cancer patients when first-line treatments have failed.

In this case, a 25mg per day dosage of Aromasin is recommended for cancer treatment.

Prescription guidelines also recommend that it be taken following a meal.

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Aromasin On-Cycle for Gynecomastia and Estrogen Control

For the treatment of gynecomastia and for ongoing Estrogen control during a cycle of anabolic steroids, the average dose is 12.5 – 25mg per day.

Some users have even opted for a protocol of 12.5mg every other day, but this is highly dependent on the type and dosage of aromatizable steroids being used.

Others opt to keep Aromasin on hand but not use it unless an Estrogen-related side effect or issue begins to present itself.

In this case, an individual might opt to take a full 25mg until the side effect subsides, and then reduce the dosage to 12.5mg per day or every other day, or even less.

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Aromasin for Post Cycle Therapy (PCT)

Studies have demonstrated that Aromasin can increase endogenous natural Testosterone levels in men by 60%, which is quite significant, especially in only 10 days.

The most ideal Aromasin dosage for this purpose is 25mg per day for no longer than a 2-week period.

Nolvadex is typically run alongside Aromasin for a period of 4 weeks at a dose of 20 – 40mg.

Aromasin possesses a half-life of approximately 27 hours.

It can be administered at any time of day, though both studies and prescription guidelines indicate that consuming it with food may result in better absorption into the body.

It is also important to understand that it takes 7 days for the body to reach peak plasma levels of the compound.

It is also very important to understand that with a compound such as Aromasin that reduces Estrogen levels, the concept and idea here should be to control Estrogen levels and not eliminate them.

The elimination of Estrogen levels can result in very terrible consequences, especially in the long run.

Estrogen should only be controlled to proper levels when necessary, and the administration of an Aromatase Inhibitor (such as Aromasin) should either be ceased, discontinued, or have its dose greatly reduced.

Severely reducing Estrogen levels will not only increase side effects, but it will also negatively impact muscle gains in the long run.

Exemestane (AKA Aromasin)