# Exemestane-The Underdosed AI



## Jimmyinkedup (Apr 16, 2013)

Ok so let me start off by saying this is quite a departure from what I used to believe re: stane dosage. I have posted it elsewhere and wanted to gather thoughts from here as well.

Its important when we look at AI's and data from studies etc its important that we use data on males. There are several key differences in an ai's effects in men and women. First and foremost is they are more effective in women at reducing estrogen. Second is they have a much longer half life in women than they do in men. Very often people misquote how much an ai will reduce estrogen based on data taken from a study on females. So when you look at studies on ai's,on males you find one thing out very quickly. There are plenty available on anastrozole and letrozole and there is essentially 1 with all inclusive data on exemestane. Luckily that one holds some very solid and applicable data for our purposes.

Key Points of Study:

1- Take Exemestane with dietary fats. They administered it this was in this study, referencing another study which showed an increase in the absorption of exemestane of 40% when taken with fats.

2- Exemestane administered at25mg/day vs 50mg/day offered minimal difference in estrogen levels. While the 50mg/day lowered levels more quickly both dosages ultimately ended up at virtually the same estrogen levels. I suspect the increased androgens of a cycle might alter this slightly and a slight more of a difference would be observed with 50mg/day over 25mg/day it is very obvious that 25mg/day is the optimal therapeutic dose for this drug.

3- Exemestane had either no negative effect or a positive effect on igf and lipids at either dose (25 or 50mg/day). Its interesting in and of itself something that lowers estrogen can have no impact on these things, the fact that there is a positive impact is pretty amazing.

4- Exemestane had a dramatic effect in reducing estrogen, but at both 25mg/day and 50mg/day while estrogen levels were low they were within the clinical range. So it is VERY difficult to "crush"estorgen levels with exemestane. This is huge as anyone that has experienced this with letrozolle or anastrozole will tell you it is no picnic and it is also very unhealthy as well.

5- Exemstane exhibits a half life in males between 8-9hrs. Because of the way ot works this is not indicative of the effective time of the drug. However it is worth paying attention too - something i have previously dismissed.


So based on my personal experience with exemestane, and all the things I read above, all the under dosed stane posts i see across the various forums, and some great discussions here, I had come to the conclusion that we are dosing exemstane too low. We have a compound here with a clear optimal therapeutic dosage of 25mg. It will lower your estrogen levels but not crush them even at a high dose. It has a positive or no effect on the normal areas of concern when lowering estrogen like igf and cholesterol. It has a very short half life.

We have a study here of males not taking testosterone, where they are taking 25-50mg/day and keeping estrogen levels low but within the clinical range. That is our exact goal! As I looked at this more and more it became apparent to me that my thoughts on dosage and administration frequency were in fact incorrect, Not only were they thoughts I subscribed too, but ones that are widely subscribed too. Why would we take less than these males when we have more androgens present? It makes no sense.Well in my opinion the answer is we shouldn't be. I decided I was going to be a guinea pig myself and play with exemestane dosages and get blood work my next cycle. I had become convinced and speculated the optimal protocol for my cycle,which would consist of a test base of 500mgs/week, would be 25mgs of exemestane/day. Broken up into 2 - 12,5 mg doses taken with fats.

Now had I not been browsing the various forums today I wouldn't be posting this. I came across a post of bloodwork from a gentleman, on cycle, 500mgs test/week , taking 25mgs exemestane per day, in 2 -12,5 mg doses with meals and his estrogen levels were safely within reference range!

That pretty much sealed it for me. I seriously think we are taking too little exemestane. I am going to do blood work when I go on cycle but at this point I dont think this is speculation. The study data backs it. The real world data backs it (good and bad), and you have a drug even at high doses that offers nothing in the way of traditional negative effects when lowering estrogen, positively impact some of those effects, and is very difficult to crash estrogen levels when taking.  

I firmly believe that an increase in dosage and frequency of administration combined with taking with dietary fats will improve the effectiveness of exemestane. I really do believe that is the proper dose, taken in the proper way to ensure maximal effectiveness. It has taken some time for me to evolve this opinion and much discussion with some great guys here. Always learning.

Anyway I wanna Hear your guys thoughts on this. Oh and here is the study reference : Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males


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## heavyiron (Apr 16, 2013)

Good post.

I'm currently using 25mg PP's Aromasin every 12 hours.


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## ErikGearhead (Apr 16, 2013)

I had tried aromasin previously and had bad luck with it.  I think it may have been dosage related, as I followed the recommended 12.5mg ED protocol.
I'm happy to see a study like this--I think i'll give it another try at 25.


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## purchaseprotein (Apr 16, 2013)

I've always tested at 25 mg per day until the joint pain on my test subject became unbearable. then I'd pull it back to 12.5mg.  We're currently back to an upswing of 25mg per day. 
Good read jimmy!


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## HARD AT IT (Apr 16, 2013)

Really interesting. I have never used stane before. I go with liquidex or ari


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## DaBeast25 (Apr 16, 2013)

On 800mg of Test per week 10mg of Aromasin 3x/day had my estro at 46.1


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## AllAboutPeptides (Apr 16, 2013)

Well worth the read. Thank you


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## HFO3 (Apr 16, 2013)

great thread, thanks for posting!


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## purchaseprotein (Apr 17, 2013)

My thought are moving to bi daily administration. makes sense with an 8 hour half life



heavyiron said:


> Good post.
> 
> I'm currently using 25mg PP's Aromasin every 12 hours.


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## BIGBEN2011 (Apr 17, 2013)

but  that would make exemstane a lot lot higher priced ai than any other .i am just asking why would people pay 3 or 4 times as much as they would for one of the other ai?


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## Jimmyinkedup (Apr 17, 2013)

purchasepeptides said:


> My thought are moving to bi daily administration. makes sense with an 8 hour half life



Well the way stane works the half life isnt exactly indicative of the time of activity. It takes time for the body to produce new aromatase- so its effective time is much longer than the half life indicates. That being said the thing that really jumps out is that it is VERY difficult to crush estrogen with stane - even  at 50mg/day with no exogenous test e was low - but still in reference. Combine this with stanes lack of negative effects on igf and lipids i would error on the side of too much over too little. At any rate its prob a combo of all the factors-including half life.. Its a shame the study wasnt a long term one - we could ascertain more definitively. Either way I think its time to start to change the mindset when it comes to proper dosing of this ai. Surely do away with eod and probably in most cases take more than previously thought. Thanks to everyone for the participation!


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## Jimmyinkedup (Apr 17, 2013)

BIGBEN2011 said:


> but  that would make exemstane a lot lot higher priced ai than any other .i am just asking why would people pay 3 or 4 times as much as they would for one of the other ai?



Great question. Of all the ai's stane has the least in the way of negative impact on igf and lipids. Also it will not result in any "rebound"of estrogen after cessation of use since it renders the aromatase it binds to permanently inactive. Where as when letro and dex wear off the aromatase they were bound to becomes active again. It also seems to be forgiving in the area of crushing estrogen levels , which if anyone has done in the past they will tell you it sucks. The study shows even at 50mg/day with no exogenous test - the e levels were low but still in reference range.


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## crackrbaby (Apr 17, 2013)

I was running 750 test and 25mg. Exemestane 1 time daily. My estro sat at 17.7 with this dose. I later changed to 12.5 am and 12.5 pm dosing and I started getting extreme joint pains and felt like shit (estro crash) which I then took a week off the exemestane.  Once i continued with my 1 time daily dose, everything returned to normal. This leads me to believe that twice a day exemestane dosing is more effective at lowering estro than a single dose. Unfortunately I did not have bloods done when I felt like I crashed my estro, so I cannot say 100%. Just my experience


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## BIGBEN2011 (Apr 17, 2013)

ok that gave me my answer. so what i do is i take exemstane 15mg a day but i allso take one huge pump of formeron a day with it seems to work for me.but i may try taking 12.5mg twice a day am and pm and keep the pump of formeron.


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## Jimmyinkedup (Apr 17, 2013)

BIGBEN2011 said:


> ok that gave me my answer. so what i do is i take exemstane 15mg a day but i allso take one huge pump of formeron a day with it seems to work for me.but i may try taking 12.5mg twice a day am and pm and keep the pump of formeron.



Please keep us updated if you do this.


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## longworthb (Apr 17, 2013)

I'd pay more for the simple fact it's a better ai overall IMO. There's no rebound and its not harsh at all bro


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## BIGBEN2011 (Apr 17, 2013)

Jimmyinkedup said:


> Please keep us updated if you do this.


sure will


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## XYZ (Apr 17, 2013)

Good post.  Thanks for sharing.


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## hypno (Apr 22, 2013)

Killer post! Thank you!


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## moodyman1 (Apr 22, 2013)

I've seen and read the study the OP posted. It certainly makes for an interesting discussion. But I would proceed with caution. 

Information from the maker of Exemestane seems to conflict with the study posted above.

(Take note of the amount of estrogen supression)

*Effect on Estrogens

Multiple doses of exemestane ranging from 0.5 to 600 mg/day were administered to postmenopausal women with advanced breast cancer. Plasma estrogen (estradiol, estrone, and estrone sulfate) suppression was seen starting at a 5-mg daily dose of exemestane, with a maximum suppression of at least 85% to 95% achieved at a 25-mg dose. Exemestane 25 mg daily reduced whole body aromatization (as measured by injecting radiolabeled androstenedione) by 98% in postmenopausal women with breast cancer. After a single dose of exemestane 25 mg, the maximal suppression of circulating estrogens occurred 2 to 3 days after dosing and persisted for 4 to 5 days. *

Now here is the kicker...

*
Gender

The pharmacokinetics of exemestane following administration of a single, 25-mg tablet to fasted healthy males (mean age 32 years) were similar to the pharmacokinetics of exemestane in fasted healthy postmenopausal women (mean age 55 years).*


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## Jimmyinkedup (Apr 22, 2013)

moodyman1 said:


> I've seen and read the study the OP posted. It certainly makes for an interesting discussion. But I would proceed with caution.
> 
> Information from the maker of Exemestane seems to conflict with the study posted above.
> 
> ...



The only reason I laugh (and it is not at youat all) is because I myself have posted the very same thing - yet upjohn/pharmaxia backs (or doesnt back) this statement with no avail data on the clinicals in men - just that statement and when you try to find any data...it mysteriously doesnt exist. Hmmmn...


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## moodyman1 (Apr 22, 2013)

Yeah..u definately have a point. I can't find the actual Upjohn study either. I certainly wouldn't put it past them to drop in the male statement based on an assumption. Especially considering the drug is targeted towards woman. The seperate study done on males by independent researchers is certainly compelling.


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## Jimmyinkedup (Apr 30, 2013)

Another log with bloodwork that strongly supports the contention of the orginal post in this thread: http://www.ironmagazineforums.com/anabolic-zone/180916-friends-lab-results-high-testosterone.html


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## Mkpaint (Apr 30, 2013)

I've got labs posted on asf where my test was 2925 and e2 -41.6 on 12.5mg xtane 2 times a day.


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## Luxx (Aug 19, 2014)

@jimmy thank you so much for posting this. Great info!


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## Machmood (Aug 19, 2014)

Im on a trt dose of 200mg a week. Total test 1066, free 33. I take 12.5mg a day and my E2 is 16.  Guys taking 4x my dose are taking 12.5 EOD, seems crazy. I aromatize very easily , but still that low of a dose seems ineffective. When I blast with 500mg I'll be taking 25mg am, 12.5 8 hours later.


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## Rayjay1 (Aug 19, 2014)

Machmood said:


> Im on a trt dose of 200mg a week. Total test 1066, free 33. I take 12.5mg a day and my E2 is 16.  Guys taking 4x my dose are taking 12.5 EOD, seems crazy. I aromatize very easily , but still that low of a dose seems ineffective. When I blast with 500mg I'll be taking 25mg am, 12.5 8 hours later.



This is similar to how I use exemestane.  I have always needed 25+ on cycle.  EOD or E3D dosing people say they use has never made any sense to me


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## jadean (Aug 19, 2014)

Awesome read


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## Mike Arnold (Aug 21, 2014)

I've been telling guys for years that 10-12.5 mg is too low, yet I continue to see guys using 12.5 mg while running huge dosages of aromatizable AAS.  I have never recommended less than 25 mg for the reasons the OP stated above.  This study actually came out a few years back (I believe Heavy posted it over at MD) and was quite revealing.


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## Machmood (Aug 21, 2014)

I think people only associate sensative nips with high esteogen.  Some guys E2 can be 200 and they don't get sensative nips so think everything is fine.  In this case they think that 12.5 is doing a good job, yet E2 is out of controll. For me I get sensative nips tne second my e2 is out of range, so I know when my e2 is high


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