Aromasin~exemestane

**heavyiron** · 01-24-2010, 02:22 PM

Aromasin

(Exemestane)

Aromasin is a steroidal aromatase inactivator used to lower circulating estrogen. It was developed to help fight breast cancer as estrogen plays a role in the growth of cancer cells. Aromasin binds irreversibly to the aromatase enzyme. This suppresses the conversion of androgens into estrogen. Circulating estrogen can be reduced by nearly 85% in women using Aromasin. A common misconception is that aromatase inhibition is similar in men than women. However in trials when males were administered 25mg of Aromasin daily maximal estradiol suppression of 62 ± 14% was observed at 12 hours. Aromasin acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as "suicide inhibition." In other words, Exemestane, by being structurally similar to the target of the enzymes, permanently binds to those enzymes, thereby preventing them from ever completing their task of converting androgens into estrogens. When we compare this mode of action against other AI’s the benefit becomes clear. Arimidex can unbind from the aromatase enzyme when you stop taking it but Aromasin will not therefore there is less chance of estrogen rebound with Aromasin.

Aromasin can be employed during a steroid cycle when aromatizing compounds such as testosterone are administered in order to control estrogen from getting out of control. During the course of a typical steroid cycle estrogen can rise quite high. Estrogen has been measured as much as 7 times higher than normal in men on steroids. This is excessive and can potentially cause water retention, gynecomastia (the formation of female breast tissue) or benign prostatic hyperplasia. Therefore in order to avoid these side effects estrogen must be controlled.

Aromasin not only lowers circulating estrogen and sex hormone binding globulin but it also increases free testosterone by a whopping 117%! Total testosterone increases about 60%. Check out the performance of Aromasin after just 10 days of treatment in males.

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).

Aromasin may be used during a steroid cycle with aromatizing compounds and during PCT to help keep the estrogen to testosterone balance in favor of testosterone. Out of all the medications to control estrogen, Aromasin seems to be the most well balanced. It raises testosterone slightly better than Arimidex and lowers estradiol about 12% better than arimidex in men and is likely to cause less estrogen rebound than Arimidex. Keep in mind that 50mg of Aromasin daily kept estradiol in the normal range for men so if you think using an aromatase inhibitor will crush estrogen too much this science supports the opposite. From the data I have read and my years of experience with this medication 25mg of Aromasin every other day is a good starting point on moderate doses of testosterone. If testosterone doses are raised then 25mg daily may be needed to control estrogen. Since either high and low estrogen can cause side effects such as low libido only labs can determine the appropriate dose of Aromasin.

Written by heavyiron

**MtR** · 01-24-2010, 05:04 PM

Cliffs Notes version for all you window lickers out there......Aromasin is fucking awesome!

**toothache** · 01-25-2010, 03:40 PM

Originally Posted by MtR

Cliffs Notes version for all you window lickers out there......Aromasin is fucking awesome!

hahahaha....agreed 100%

**quark** · 01-25-2010, 05:05 PM

shouldn't that be 0.25mg of arimidex (last paragraph)?

**JerseyDevil** · 01-25-2010, 06:06 PM

Where do you guys suggest buying this? I have used Innovative Research for years for tamoxifin and sildenafil citrate. Good product and prices usually half of the other research chem guys.

However, they seem to be going under, and they never offered Exemestane.

**heavyiron** · 01-25-2010, 06:34 PM

Originally Posted by jchappj

shouldn't that be 0.25mg of arimidex (last paragraph)?

Good eyes, actually it should read Aromasin. Thanks for catching that I edited it.

**tballz** · 01-26-2010, 10:24 AM

Originally Posted by jchappj

shouldn't that be 0.25mg of arimidex (last paragraph)?

Good catch...I do believe it should say that.

**tballz** · 01-26-2010, 10:24 AM

Originally Posted by JerseyDevil

Where do you guys suggest buying this? I have used Innovative Research for years for tamoxifin and sildenafil citrate. Good product and prices usually half of the other research chem guys.

However, they seem to be going under, and they never offered Exemestane.

The sponsor here....CEM Products

**diablomex** · 01-26-2010, 10:29 AM

how do you take that stuff cem has

**MtR** · 01-26-2010, 12:20 PM

Originally Posted by diablomex

how do you take that stuff cem has

1ml = 25mg of Aromasin. It is an oral suspension.

So, you get yourself a dropper, syringe, whatever...and measure out the dosage necessary for your needs. If your needs are 25mg per day or eod then you would use a full 1ml syringe of product or adjust accordingly.

Be forewarned, it tastes like shit so you will need a chaser. I usually drop it under my tounge and hold it for about 20 seconds then swallow.

**tballz** · 01-26-2010, 03:26 PM

CEM gives you a syringe to measure with.

**bigpapabuff** · 01-27-2010, 06:35 PM

cem has very good ai's, i like the aromasin the best, only use letro is you have signs of gyno it is very strong.

**SoreButtCheeks** · 01-30-2010, 05:11 AM

Gonna up my exe dosage to 12.5mg a day for the next week and see if I can notice any changes. I've been using as little as 6.25mg EOD with good results in terms of nipple soreness issues.

S.B.C

Author of the SoreButtCheeks steroid blog.

( Google SoreButtCheeks to find it )

**heavyiron** · 03-08-2010, 07:00 PM

Effects of Tamoxifen and Exemestane on Cognitive Functioning of Postmenopausal Patients With Breast Cancer: Results From the Neuropsychological Side Study of the Tamoxifen and Exemestane Adjuvant Multinational Trial

Christina M. Schilder, Caroline Seynaeve, Louk V. Beex, Willem Boogerd, Sabine C. Linn, Chad M. Gundy, Hilde M. Huizenga, Johan W. Nortier, Cornelis J. van de Velde, Frits S. van Dam, and Sanne B. Schagen*
From the Departments of Psychosocial Research and Epidemiology, Neuro-oncology, and Medical Oncology, Netherlands Cancer Institute; Department of Neurology, Slotervaart Medical Center; Department of Psychology, University of Amsterdam, Amsterdam; Department of Medical Oncology, Erasmus Medical Center-Daniel den Hoed Cancer Center, Rotterdam; Department of Medical Oncology, Radboud University Medical Center, Nijmegen; and the Departments of Medical Oncology and Surgical Oncology, Leiden University Medical Center, the Netherlands.

* To whom correspondence should be addressed. E-mail: s.schagen@nki.nl

Purpose: To evaluate the influence of adjuvant tamoxifen and exemestane on cognitive functioning in postmenopausal patients with breast cancer (BC).

Patients and Methods: Neuropsychological assessments were performed before the start (T1) and after 1 year of adjuvant endocrine treatment (T2) in Dutch postmenopausal patients with BC, who did not receive chemotherapy. Patients participated in the international Tamoxifen and Exemestane Adjuvant Multinational trial, a prospective randomized study investigating tamoxifen versus exemestane as adjuvant therapy for hormone-sensitive BC.

Results: Participants included 80 tamoxifen users (mean age, 68.7 years; range 51 to 84), 99 exemestane users (mean age, 68.3 years; range, 50 to 82), and 120 healthy controls (mean age, 66.2 years; range, 49 to 86). At T2, after adjustment for T1 performance, exemestane users did not perform statistically significantly worse than healthy controls on any cognitive domain. In contrast, tamoxifen users performed statistically significantly worse than healthy controls on verbal memory (P < .01; Cohen's d = .43) and executive functioning (P = .01; Cohen's d = .40), and statistically significantly worse than exemestane users on information processing speed (P = .02; Cohen's d = .36). With respect to visual memory, working memory, verbal fluency, reaction speed, and motor speed, no significant differences between the three groups were found.

Conclusion: After 1 year of adjuvant therapy, tamoxifen use is associated with statistically significant lower functioning in verbal memory and executive functioning, whereas exemestane use is not associated with statistically significant lower cognitive functioning in postmenopausal patients with BC. Our results accentuate the need to include assessments of cognitive effects of adjuvant endocrine treatment in long-term safety studies.

**theCaptn'** · 03-08-2010, 07:13 PM

Heavy, so Im guessing a std 12.5mg ED and 25mg EOD dosages are inter-changable?

**heavyiron** · 03-08-2010, 07:37 PM

Originally Posted by CaptRichArund

Heavy, so Im guessing a std 12.5mg ED and 25mg EOD dosages are inter-changable?

Probably close enough.

**heavyiron** · 03-08-2010, 07:46 PM

Aromasin is an AI that has been studied in men. This is significant because circulating estradiol is reduced in differing percentages between genders.

Pharmacokinetics and Dose Finding of a Potent Aromatase Inhibitor, Aromasin (Exemestane), in Young Males

Nelly Mauras, John Lima, Deval Patel, Annie Rini, Enrico di Salle, Ambrose Kwok and Barbara Lippe
Nemours Children’s Clinic and Research Programs (N.M., J.L., A.R.), Jacksonville, Florida 32207; and University of Florida Health Sciences Center (D.P.) and Amersham Pharmacia Biotech (E.d.S., A.K., B.L.), Peapack, New Jersey 07977

Address all correspondence and requests for reprints to: Nelly Mauras, M.D., Nemours Children’s Clinic, 807 Children’s Way, Jacksonville, Florida 32207. E-mail: nmauras@nemours.org.

Abstract

Suppression of estrogen, via estrogen receptor or aromatase blockade, is being investigated in the treatment of different conditions. Exemestane (Aromasin) is a potent and selective irreversible aromatase inhibitor. To characterize its suppression of estrogen and its pharmacokinetic (PK) properties in males, healthy eugonadal subjects (14–26 yr of age) were recruited. In a cross-over study, 12 were randomly assigned to 25 and 50 mg exemestane daily, orally, for 10 d with a 14-d washout period. Blood was withdrawn before and 24 h after the last dose of each treatment period. A PK study was performed (n = 10) using a 25-mg dose. Exemestane suppressed plasma estradiol comparably with either dose [25 mg, 38% (P 0.002); 50 mg, 32% (P 0.008)], with a reciprocal increase in testosterone concentrations (60% and 56%; P 0.003 for both). Plasma lipids and IGF-I concentrations were unaffected by treatment. The PK properties of the 25-mg dose showed the highest exemestane concentrations 1 h after administration, indicating rapid absorption. The terminal half-life was 8.9 h. Maximal estradiol suppression of 62 ± 14% was observed at 12 h. The drug was well tolerated. In conclusion, exemestane is a potent aromatase inhibitor in men and an alternative to the choice of available inhibitors. Long-term efficacy and safety will need further study.

full study;
http://jcem.endojournals.org/cgi/con...ull/88/12/5951

**ersin.konuk** · 03-09-2010, 09:20 AM

I taking 20 mg of nolva a day and i want to switch over to aromasin, can u do that? and if so what is the procedure?

**heavyiron** · 03-09-2010, 10:24 AM

Originally Posted by ersin.konuk

I taking 20 mg of nolva a day and i want to switch over to aromasin, can u do that? and if so what is the procedure?

Start the aromasin and keep using the nolva alongside it for 7 days and then drop the nolva.

**ersin.konuk** · 03-09-2010, 11:29 AM

Thanks heavy,

**DANISH VIKING** · 03-21-2010, 08:00 PM

Thanks for these Solid Rock Hard Info's, and for the Good work put into this-
for providing the Knowledge to Us ALL
"GREAT JOB" Heavy!!!
DV.

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Nolva makes you dumb, Aromasin does not

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