Aromatase Inhibitors

Aromatase Inhibitors

The Usual Suspects

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Around 2003 the World Changed

Breast cancer awareness was very strong 15 years ago and most people knew that breast cancer was often treatable by using estrogen blockers. This of course didn’t stop women from getting uterine cancer from the estrogen binding to the endometrium though. That was the big downfall of the main treatment at the time; the SERM tamoxifen (Nolvadex). Tamoxifen seemingly caused one cancer by curing another. But that’s not the truth. By stopping and inhibiting breast growth by binding to the estrogen receptor on the breast there was just that much more estrogen in circulation.

So how did the world change? Aromatase inhibitors (AIs) were developed. Now, instead of just gumming up the receptor like a bandaid we now could stop the body from MAKING estrogen from testosterone.


Aromatase Inhibitors



Here is a graph showing how adding one of the AIs to testosterone stopped conversion of testosterone (A) to estrogen. This is proven in how the combination plates didn’t grow the breast cancer cells like pure estrogen or testosterone did without an AI added.


Aromatase Inhibitors and Bodybuilding

So how does this affect you, a guy? AIs can stop testosterone from converting to estrogen, as I just showed you. This means neither your natural testosterone, anabolic steroids, nor prohormones will be broken down into the ‘anti-test’ estrogen when you’re on an AI.

Why is this important? Estrogen not only counteracts the effects of testosterone, it stops your body from making it!

The main point of a man using an AI post cycle is to stop estrogen from stopping testosterone production. By stopping your body from making estrogen through using an AI, you stop the estrogen from turning off your testosterone production. Now, using the estrogen blocker Tamoxifen, you will give the opposite signal of normal estrogen on the pituitary and turn ON testosterone production (as a secondary effect of LH release)!


So Which Do I Use?

Like the SERMs, AIs are prescription drugs and thus Illegal.

Of the three illegal aromatase inhibitors I think arimidex is the best and here is why:

Arimidex (Anastrozole) and exemestane  (Aromasin) only take 7 days to reach steady state, letrozole (Femara) takes 60!

This is weird because the half lives are 48 hours, 60 hours and 27 hours respectively. So I don’t get how it takes 60 days for letrozole to reach steady state when it should take 4 days with a 27 hour half life.

Arimidex had no negative effect on HDL and thus LDL, nor did it inhibit cortisol. Exemestane and letrozole did. In case you’re new here let me explain. Estrogen is good for some stuff. One of which is it stimulates HDL production, which clears up LDL (the ’bad’ Cholesterol). By stopping all estrogen from forming in the body you’re basically telling your body NOT to make HDL and thus your LDL gets sky high. This is how bodybuilders die. Usually not the liver or kidney, despite what you hear.

SO, if arimidex somehow DOES NOT lower HDL despite that making no sense, then you’ll live longer if you use arimidex than if you use exemestane or letrozole.

Remember how tamoxifen does the opposite of estrogen at the pituitary? It turns on, not off, testosterone production? Well it does the SAME thing as estrogen on the liver; it stimulates HDL production just like estrogen! Yeah Tamoxifen! Way to kick some major ass!

Arimidex offers 90% inhibition of Aromatase, Letro 90%+ and exemestane 60%. That makes exemestane better on cycle for control of estrogen but letro or aromatase better for PCT or competition prep.

Why? Because you want some estrogen when you’re trying to grow since it acts a lot like IGF-1 on muscle cells. Thus exemestane is the better choice, or, you could do what most guys do and use 1 mg arimidex every 3 days instead of every day. This way you get the HDL benefits of Arimidex.


Legal Alternatives


Androsta-3,5-diene-7,17-dione (Androsta) is a metabolite of 7-Keto-DHEA, which is a very potent suicide aromatase inhibitor. Like extemistane, the other suicide inhibitor, it destroys the aromatase enzyme so there is no rebound in estrogen after you stop using it like letrozole or arimidex cause. It is a natural occurring compound, produced by metabolism of the prohormone DHEA, and it’s used in a wide array of supplemental stacks. It is so powerful that even the World Anti-doping Agency(WADA) has it on its banned list of anabolic agents, meaning Olympians will fail a drug test if it shows up in the blood. This does not make it illegal, they have everything on that list from asthma medication to creatine to even CAFFEINE! Rediculous.


7,8 benzoflavone chemical structure

7,8 Benzo

7,8 Benzoflavone is a synthetic flavone derivative, which is a potent aromatase inhibitor. It is known as alpha-naphthoflavone, and it shouldn’t be confused with 5,6 benzo, known as, beta-naphthoflavone, which is an inducer of detoxification enzymes and is not an aromatase inhibitor at all.


Legal SERM + AI Combination Products

There are combination products in the mind and muscle store that are both legal and effective! Form XT combination of Estrogen blockers and Androsta but packaged together for the best results. Arom X has different ERBs but has 7,8 benzo as its AI. I think the best option is to use Form-xt AND Arom X together at half doses post cycle with Rise and Swell.

Rise and Swell is my natural testosterone booster and male sexual enhancer. when coupled with either or both Form XT and Arom X it is a three pronged assault on post cycle therapy!



Arimidex has no downsides and is almost as effective as letro, but, it’s active so much earlier that for the first 60 days arimidex is stronger. Since no PCT is 60 days long…. Arimidex is king. Now keep in mind that this is comparing 2.5 mg of letro a day to 1 mg arimidex. In my PCT article I show the study that proves 2.5 mg letro a WEEK is better than 2.5 mg letro a DAY for purposes of PCT. Likewise normal use of arimidex in bodybuilders is 1 mg arimidex every 2 to 3 days not every day.

If you would rather not break the law, use Form XT and/or Arom X to get as close as legally possible to Arimidex and Tamoxifen, and Rise and Swell to get as close as legally possible to Viagra and HCG.

Nothing in this article or on this site should be considered medical advice or as an endorsement to violate any law of the country in which you reside.  The information given is for fun and entertainment purposes only.  All claims are 100% dependent upon proper diet and exercise.  Please consult a medical practitioner prior to any diet and exercise program.



Buzdar AU, Robertson JF, Eiermann W, Nabholtz JM: An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. Nov 1;95(9):2006-16, 2002
2. Haynes BP, Dowsett M, Miller WR, Dixon JM, Bhatnagar AS: The pharmacology of letrozole. J Steroid Biochem Mol Biol. Oct;87(1):35-45, 2003
3. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
4. Chen S, Masri S, Wang X, Phung S, Yuan YC, Wu X. What do we know about the mechanisms of aromatase inhibitor resistance? J Steroid Biochem Mol Biol. 102(1-5):232-40, 2006
5. Miller, WR; O′Neill, J. The importance of local synthesis of estrogen within the breast. Steroids. 50:537–548, 1987


1. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
2. Riepe FG, Baus I, Wiest S, Krone N, Sippell WG, Partsch CJ: Treatment of pubertal gynecomastia with the specific aromatase inhibitor anastrozole. Horm Res. 62(3):113-8. Epub 2004 Jul 20, 2004


1. Buzdar AU: Pharmacology and pharmacokinetics of the newer generation aromatase inhibitors. Clin Cancer Res. Jan;9(1 Pt 2):468S-72S, 2003
2. Lonning PE: Exemestane: a review of its clinical efficacy and safety. Breast. Jun;10(3):198-208, 2001
3. Mauras N, Lima J, Patel D, Rini A, di Salle E, Kwok A, Lippe B: Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. J Clin Endocrinol Metab. Dec;88(12):5951-6, 2003

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