Aromasin (Exemestane) is a steroidal suicide aromatase inhibitor, which means that it lowers estrogen production in the body by blocking the aromatase enzyme, the enzyme responsible for estrogen synthesization. (1)(2)(3)
This stuff was developed to fight breast cancer in post-menopausal women, who need a particularly aggressive therapy, and for whom first line defenses such as SERMS (Tamoxifen) have not worked. This should be our first clue in inferring that this stuff is pretty strong, or at least stronger than some of the other compounds which are used to fight breast cancer.
Aromasin and Side Effects
Aromasin averages an 85% rate of estrogen suppression (4), so its clearly a very effective agent for bodybuilders and other athletes wanting to avoid estrogen related side effects such as gyno, acne, or water-retention brought on by aromatizing steroids. Specifically, Exemestane dose this by selectively inhibiting aromatase activity in a time-dependent and irreversible manner (hence the "suicidal" portion of its name, I guess).(7)
As with most of the compounds in this class, it also causes a reasonable rise in testosterone levels
(6), and as you may have guessed, this rise in testosterone means that Exemestane can also cause androgenic sides(8)(9)(10). As you can see from the chart below, exemestane is very effective at both lowering estrogen (estradiol) and raising testosterone:
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). (13)
So we can see that 25mgs is a very effective dose from that chart, right? As an added benefit, exemestane not only increases testosterone and lowers estrogen, but it also increases IGF le
vels (11).Additionally Worth noting is that Aromasin may possibly be less harsh on blood lipids (14)than some of the other (similar) compounds we use in the world of bodybuilding or athletics (other AIs). It also has, at best no effect on IGF, and at worst could lower (13) it. AIs are very tricky with regards to inconsistencies in IGF levels.
Unfortunately, you need to take Exemestane for a week to reach steady blood plasma levels of it, and exemestane has a life of 27 hours (12.).
The ability of exemestane to lower estrogen levels by the aforementioned 85% makes it a very nice choice for use in any cycle where aromatizing steroids are used. In addition, since its not too harsh at all on blood lipid profiles, its a very good choice for longer cycles. Its ability to raise both testosterone levels also seem to suggest that it would be a very nice addition to a Post-Cycle-Therapy (PCT).
A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation.Br J Clin Pharmacol. 2005 Mar;59(3):355-64.
Exemestane for breast cancer prevention: a feasible strategy?Clin Cancer Res. 2005 Jan 15;11(2 Pt 2):918s-24s.
Endocrinology and hormone therapy in breast cancer: Aromatase inhibitors versus antioestrogens, Anthony Howell1 and Mitch Dowsett2. 1CRUK Department of Medical Oncology, University of Manchester, Christie Hospital, Manchester, UK. 2Academic Department of Biochemistry, Royal Marsden Hospital, London, UK. Breast Cancer Res 2004, 6:269-274 doi:10.1186/bcr945. Published 6 October 2004
Eur. J. Cancer. 2000, May;36(8):976-82
Breast Cancer Res Treat. 1995;36(3):287-97.
J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.
Nippon Yakurigaku Zasshi. 2003 Oct;122(4):345-54.
Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S.
J Clin Endocrinol Metab 2000 Jul;85(7):2370-7
J Steroid Biochem Mol Biol 1997 Nov-Dec;63(4-6):261-7
Anticancer Res. 2003 Jul-Aug;23(4):3485-91
Clin Cancer Res. 2003 Jan;9(1 Pt 2):468S-72S
The Journal of Clinical Endocrinology & Metabolism Vol. 88, No. 12 5951-5956Copyright 2003 by The Endocrine Society
J Clin Endocrinol Metab. 2003 Dec;88(12):5951-6.
This information is about a hormonal therapy used to treat breast cancer called exemestane, which is also
Throughout this information we refer to it by its more commonly used name, Aromasin. It should ideally be
read with our general information about breast cancer or secondary breast cancer .
Aromasin is a type of hormonal therapy used to breast cancer in women who have been through the
menopause (change of life).
Hormonal therapies interfere with the production or action of particular hormones in the body. Hormones are
substances produced naturally in the body. They act as chemical messengers and help to control the activity
of cells and organs.
Many breast cancers rely on the hormone oestrogen to grow. These cancers are known as hormone-sensitive
In women who have had their menopause, the main source of oestrogen is through the conversion of
androgens (sex hormones produced by the adrenal glands) into oestrogens. This is carried out by an enzyme
called aromatase. The conversion process is known as aromatisation, and happens mainly in the fatty tissues
of the body.
Aromasin is a drug that blocks the process of aromatisation, and reduces the amount of oestrogen in the body.
As less oestrogen reaches the cancer cells they grow more slowly or stop growing altogether. Drugs that work
in this way are known as aromatase inhibitors. Other aromatase inhibitors include anastrozole (Arimidex®)
and letrozole (Femara®) .
How it is taken
Aromasin is a tablet which is taken once a day, preferably after a meal and at the same time each day. It
doesn't matter whether this is in the morning or evening.
When it is given
Your doctor will take a number of different factors into account when planning your treatment.
Aromasin is used to treat post-menopausal women with hormone-sensitive breast cancer.
Early breast cancer
Aromasin may be used to treat women with early breast cancer (cancer that has not spread) after they have
completed two or three years of tamoxifen treatment.
Macmillan and Cancerbackup merged in
2008. Together we provide free, high quality
information for people affected by cancer through
our publications, website and phone service. .
Advanced breast cancer
Aromasin is used to treat women who have advanced or secondary breast cancer (cancer that has spread to
other parts of the body). It is also used to treat women whose breast cancer has come back after initial
Length of treatment
Your doctors will discuss the length of treatment they feel is appropriate for you. The length of your treatment
will depend on your individual situation. Aromasin may be given over a number of years, or for as long as it is
controlling the cancer. It may also be given after 2-3 years of treatment with tamoxifen.
Possible side effects
Each person's reaction to any medicine is different. Most people have very few side effects with Aromasin,
while others may experience more. The side effects described in this information will not affect everyone and
may be different if you are having more than one drug.
We have outlined the most common side effects but haven't included those that are rare and therefore unlikely
to affect you. If you notice any effects that are not listed in this section, discuss them with your doctor or nurse.
You may have some of the following side effects, to varying degrees:
Hot flushes and increased sweatingThese are usually mild and may wear off after a period of time. Some
people find it helps to cut down on tea, coffee, nicotine and alcohol. Research suggests that hormones called
progestogens, or some antidepressants, may help to control this side effect. Your doctor or nurse can discuss
this with you.
Some people find complementary therapies, such as acupuncture, helpful. Your GP may be able to give you
details about getting these on the NHS.
You can read more about treatments for menopausal symptoms like hot flushes in our information about
breast cancer and menopausal symptoms.
Feeling sick (nausea)Let your doctor know if this occurs, as it can usually be effectively treated. Feeling sick
can often be relieved by taking your tablet with food or at night.
Feeling tired (fatigue) Some people find they are more tired when taking Aromasin. Getting plenty of rest can
HeadachesIf you have frequent headaches your doctor can prescribe medicines to help.
Difficulty sleepingSome women find they have trouble getting to sleep while taking Aromasin. Having a
warm bath or a hot milky drink before bed can help, as can using relaxation techniques, tapes or CDs.
Abdominal pain and diarrhoeaRarely, Aromasin can cause diarrhoea . This can usually be controlled with
medicine, but let your doctor know if it is severe. It is important to drink plenty of fluids if you have diarrhoea.
Joint pains/muscular stiffnessSome women have pain and stiffness in their joints while taking Aromasin.
Let your doctor know of these effects are a problem. You may find it helpful to take mild painkillers.
Risk of osteoporosisWomen who have, or are at risk of, osteoporosis (weakened bones) should have their
bone strength assessed before and during treatment with Aromasin. Some women may need to take bonestrengthening
drugs to help prevent osteoporosis from developing.
Hair thinningSome women notice that some of their hair falls out while they are taking Aromasin. This is
usually mild and the hair regrows at the end of treatment.
Always let your doctor or nurse know about any side effects you have. There are usually ways in which they
can be controlled or improved.
آروماسین به لحاظ عملکرد شبیه لتروزول است اما به لحاظ ساختار شیمیایی برتری دارد.
داروهای گروه درمانی سرطان سینه متنوع ان ولی تقریبا سه دسته ان
یک : تخلیه کننده رسپتور(گیرنده ) استروژن مثل تاموکسیفن - سیکلوفنیل و ....
دو " مهارکننده آروماتاز مثل لتروزول-آروماسین-آناسترازول و ...
سه : آندروژن های ضداستروژن مثل دانازول-پروویرون و ....
عوارض جانبی: این دارو بر روی خانمهایی که دارای سرطان سینه بوده اند مورد آزنایش قرار گرفته و این عوارض مشاهده شده است: عصبانیت و تعرق زیاد، دل آشوب، خستگی، سردرد، دشواری در خوابیدن (بیخوابی)، اسهال و دردهای شکمی، در زانو و کوفتگی عضلات، تحلیل استخوانها، ضعف مو
آروماسین شرکت اسوه ایرانه که 30 تا 25 میلی گرمیش=60 هزار تومان
خارجیش (وارداتی): 60 تا 25 میلی گرم 320 هزار تومان
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%, 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.
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