Ckblgr
New Member
All,
I love how aromasin (exemestane) makes me feel, much more than arimidex (anastrazole). Anastrazole feels harsh and slightly poisonous, where exemestane feels smooth and mild. I have been using it on and off for years as a stand-alone, to both increase testosterone, lower SHBG and control E2. It lowers my anxiety, mental chatter, emotionality, and simply makes me feel more "manly". It increases my sexual confidence and erectile function. The problem is, it has been VERY tricky to dose properly and dial in -- it is very easy to overshoot, and end up with low E2 that takes weeks to recover. (I have repeated bloodwork that shows it takes me 10 days to recover 4 points of E2 after taking exemestane. As background, my baseline E2 hovers only slightly above the normal range: low 30s pg/ml, Quest sensitive test.)
So in order to figure out the right dosing protocol, I have been scouring the research over the past week, and want to share my key findings. I hope this will be a starting point for further discussion and self-experimentation on the forum.
1)There is only one study performed on men with exemestane (1), so that's all we have to work with. All subjects were young (20s) and healthy. Unfortunately, the study only tested daily doses of 25 and 50mg over 7 days. So it makes it difficult to figure out what an ideal long term dosing protocol would be.
2)According to this study, the half-life of the drug in these men was 8.9 hours -- compared to about 24 hours for women. (This means that it should be dosed every day in order to achieve stable blood levels).
3)When you compare the effect of 25mg in men, to the effect of 25mg in women in other studies (2, 3), E2 is suppressed only 58% in men as it is in women. (This means men would need a higher doses for the same result). To add credence to this claim, this number is remarkably consistent with how anastrazole performs in men vs. women in another study (57% suppression at the same dose) (4).
4)But the question is, how does exemestane behave in men over longer time periods? At lower doses? We have to draw some inferences. Look at this graph. This is the expected estrone sulfate (E1S) suppression in women at various daily exemestane doses. (E1S was used as a proxy for all estrogens, which rise and fall in proportion with E2) (5)
5) Assuming that men actually do clear exemestane faster, and that each dose actually is less effective in men vs. women, we can assume that this graph would be the same shape for men, just each line would be shifted upwards.
6)So if we assume that each dose in men really does only achieve 58% the E2 suppression as it would in women, this means that daily exemestane dosing at 0.5mg would suppress E2 by about 23%. 1mg/day would suppress by about 30%. And 2.5mg/day by about 46%. (These studies were done on young men and post-menopausal women, who have similar E2 levels. For levels far above the range, as might occur with steroid use or major obesity, these predictions would not apply.)
Conclusions:
1)25mg or even 5mg is way too much for most men.
2)Whether you are on TRT or not, you will get the best and most stable results if you dose daily.
3)0.5mg-2.5mg/day is perfect for most men. Better to start at a low dose.
4)DO NOT OVERSHOOT. Depending on your genetics, it can take weeks to recover your aromatase levels, especially if you are low for a long time. But if you do, don't panic, it will come back.
I still greatly prefer exemestane to anastrazole, it simply feels better, and it puts free testosterone near or above the top of the range as a standalone. With these dosing guidelines, I am much more confident how to dose without overshooting. Over the next weeks, I will be taking 1mg/day and getting regular blood tests, and will share my results.
-Chris
References:
(1) Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. - PubMed - NCBI
(2) The minimal effective exemestane dose for endocrine activity in advanced breast cancer. - PubMed - NCBI
(3) Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
(4) An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. - PubMed - NCBI
(5) A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation
I love how aromasin (exemestane) makes me feel, much more than arimidex (anastrazole). Anastrazole feels harsh and slightly poisonous, where exemestane feels smooth and mild. I have been using it on and off for years as a stand-alone, to both increase testosterone, lower SHBG and control E2. It lowers my anxiety, mental chatter, emotionality, and simply makes me feel more "manly". It increases my sexual confidence and erectile function. The problem is, it has been VERY tricky to dose properly and dial in -- it is very easy to overshoot, and end up with low E2 that takes weeks to recover. (I have repeated bloodwork that shows it takes me 10 days to recover 4 points of E2 after taking exemestane. As background, my baseline E2 hovers only slightly above the normal range: low 30s pg/ml, Quest sensitive test.)
So in order to figure out the right dosing protocol, I have been scouring the research over the past week, and want to share my key findings. I hope this will be a starting point for further discussion and self-experimentation on the forum.
1)There is only one study performed on men with exemestane (1), so that's all we have to work with. All subjects were young (20s) and healthy. Unfortunately, the study only tested daily doses of 25 and 50mg over 7 days. So it makes it difficult to figure out what an ideal long term dosing protocol would be.
2)According to this study, the half-life of the drug in these men was 8.9 hours -- compared to about 24 hours for women. (This means that it should be dosed every day in order to achieve stable blood levels).
3)When you compare the effect of 25mg in men, to the effect of 25mg in women in other studies (2, 3), E2 is suppressed only 58% in men as it is in women. (This means men would need a higher doses for the same result). To add credence to this claim, this number is remarkably consistent with how anastrazole performs in men vs. women in another study (57% suppression at the same dose) (4).
4)But the question is, how does exemestane behave in men over longer time periods? At lower doses? We have to draw some inferences. Look at this graph. This is the expected estrone sulfate (E1S) suppression in women at various daily exemestane doses. (E1S was used as a proxy for all estrogens, which rise and fall in proportion with E2) (5)
5) Assuming that men actually do clear exemestane faster, and that each dose actually is less effective in men vs. women, we can assume that this graph would be the same shape for men, just each line would be shifted upwards.
6)So if we assume that each dose in men really does only achieve 58% the E2 suppression as it would in women, this means that daily exemestane dosing at 0.5mg would suppress E2 by about 23%. 1mg/day would suppress by about 30%. And 2.5mg/day by about 46%. (These studies were done on young men and post-menopausal women, who have similar E2 levels. For levels far above the range, as might occur with steroid use or major obesity, these predictions would not apply.)
Conclusions:
1)25mg or even 5mg is way too much for most men.
2)Whether you are on TRT or not, you will get the best and most stable results if you dose daily.
3)0.5mg-2.5mg/day is perfect for most men. Better to start at a low dose.
4)DO NOT OVERSHOOT. Depending on your genetics, it can take weeks to recover your aromatase levels, especially if you are low for a long time. But if you do, don't panic, it will come back.
I still greatly prefer exemestane to anastrazole, it simply feels better, and it puts free testosterone near or above the top of the range as a standalone. With these dosing guidelines, I am much more confident how to dose without overshooting. Over the next weeks, I will be taking 1mg/day and getting regular blood tests, and will share my results.
-Chris
References:
(1) Pharmacokinetics and dose finding of a potent aromatase inhibitor, aromasin (exemestane), in young males. - PubMed - NCBI
(2) The minimal effective exemestane dose for endocrine activity in advanced breast cancer. - PubMed - NCBI
(3) Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor.
(4) An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. - PubMed - NCBI
(5) A predictive model for exemestane pharmacokinetics/pharmacodynamics incorporating the effect of food and formulation
