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Aromasin

Complete info about Aromasin

Aromasin (Exemestane) is a steroidal suicide aromatize inhibitor, which means that it lowers estrogen production in the body by blocking the aromatize enzyme, the enzyme responsible for estrogen synthesization (1)(2)(3).

Aromasin 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 (Selective Estrogen Receptor Modulators, like 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 averages an 85% rate of estrogen suppression (4), so it's 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 aromatize 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:

Experts say 25mgs is a very effective dose. As an added benefit, exemestane not only increases testosterone and lowers estrogen but it also increases IGF levels (11). Additionally worthy note is that Aromasin may possibly be less harsh on blood lipids (14) than some of the other (similar) compounds we use (other AIs) in the world of bodybuilding or athletics. It also has, at best, no effect on IGF, and, at worst, lowers (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, and exemestane has a half 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 it's not too harsh at all on blood lipid profiles, it's 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).
Also, as previously mentioned, exemestane is the only currently available aromatize inhibitor that can be run concurrently (and effectively) with Nolvadex (which usually lowers blood plasma levels of AIs), making it perfect for PCT.

References

  • 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: Aromatize inhibitors versus antioestrogens, Anthony Howell1 and Mitch Dowsett2 1 CRUK 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