Interesting Facts about Aromasin

[DrJMW]

1. It is an irreversible, steroidal aromatase inactivator

2. Structurally related to androstenedione

3. Significantly lowers estrogen and has no detectable effect on adrenal biosynthesis of corticosteroids or aldosterone

4. Aromasin 25mg daily reduced whole body aromitization by 98%

5. Has a slight affinity for the androgen receptor (.28% relative to dihydrotestosterone)

6. The binding affinity of its 17-dihydrometabolite for the androgen receptor is 100-times that of the parent compound.

7. Daily doses had no effect on levels of testosterone, androstenedione, dehydroepiandrosterone, or 17-hydroxyprogesterone.

8. A dose-dependent decrease in sex hormone binding globulin (SHBG) has been observed.

9. Slight, non-dose dependent increases in serum LH and FSH have been observed.

 

[Athernigy]

 

[Triple J]

Kind of sounds like 6-OXO (OTC)

 

[NFG123]

non reversible, eh?

So you are saying it becomes covalently bound to aromatase?

what is the turnover rate of aromatase ... ie, how long would have to wait to regenerate your entire stock of aromatase for normal aromatizing activity ...

NFG

 

[CanadianBro]

non reversible, eh?

what is the turnover rate of aromatase ... ie, how long would have to wait to regenerate your entire stock of aromatase for normal aromatizing activity ...

NFG

The normal metabolic attrition of enzymes in the body would allow the aromatase enzyme to be replaced within 4-5 days.

 

[lawnsaver]

The normal metabolic attrition of enzymes in the body would allow the aromatase enzyme to be replaced within 4-5 days.

Let me simplify...The aromatase enzyme is inactive for up to 5 days. This is how long it usually takes for that specific enzyme to be replaced. This means that to keep estrogen levels down, you still have to take 25mg every 3rd or 4th day depending on your dose of gear.

 

[CanadianBro]

Let me simplify...The aromatase enzyme is inactive for up to 5 days. This is how long it usually takes for that specific enzyme to be replaced. This means that to keep estrogen levels down, you still have to take 25mg every 3rd or 4th day depending on your dose of gear.

Thank you my friend

I sometimes tend to get ahead of myself and allow my educational background to take over.

 

[ryker77]

How does is effect the HDL, LDL and triglicryides?
Thats my main concern.

 

[CanadianBro]

This is another excellent question pertaining to Exemestane.

It appears that Aromasin has very little, if not any, negative effect on Lipid values. I had my bloodwork monitored on a Sustanon only cycle that included 1mg Exemestane every day and the blood lipid levels were unchanged from pre-cycle. As you could imagine, this was quite exciting as I have struggled in the past when consuming other estrogen inhibitors.


I have also posted a study below that provides some valuable information.





SAN FRANCISCO, CA -- May 14, 2001 -- Results from a randomized phase II clinical study in the first-line treatment of advanced breast cancer in postmenopausal women suggest Aromasin® (exemestane tablets) has a higher response rate when compared to tamoxifen. Response rate is a measurement of how effective the treatments are in shrinking the tumor.

Additionally, the study suggests Aromasin has no adverse effect on blood lipid levels, an important consideration for postmenopausal women who, by virtue of their age, are at an increased risk for developing cardiovascular disease. The data was presented today at the American Society for Clinical Oncology (ASCO) annual meeting in San Francisco.

"These findings are very promising. Exemestane demonstrated high activity as an investigational agent in the first-line treatment of breast cancer," explained Caroline Lohrisch, MD, Research Fellow, Investigational Drug Branch for Breast Cancer, European Organization for Research and Treatment of Cancer (EORTC), the organization that conducted the clinical trial. "Given the strength of these findings we have expanded this study into a Phase III trial, which will allow formal comparison of tamoxifen and exemestane."

The study randomized postmenopausal women with advanced breast cancer to either Aromasin (25 mg/day) or tamoxifen (20 mg/day). Of the 122 randomized patients, data are available on 109 for tumor response and 117 for tolerability. The results indicate that patients treated with Aromasin had three times the response rate (complete plus partial responses) in shrinking tumors (44.6 percent vs. 14.3 percent) relative to tamoxifen-treated patients. All responses have been independently reviewed by a third-party.

A sub-study of this trial examined the effect of Aromasin and tamoxifen on triglycerides, HDL and total cholesterol by measuring serum levels of the 122 women (62 Aromasin, 60 tamoxifen) before and during therapy. In general, after 24 weeks, the majority of patients with normal baseline triglyceride or HDL levels experienced no clinically relevant changes in these values. After 24 weeks, women with normal triglyceride levels at baseline (Aromasin 33, tamoxifen 27), experienced a decrease of 20 percent or greater in triglyceride levels in 36 percent and 15 percent patients treated with Aromasin and tamoxifen, respectively.

Dr. Lohrisch continues, "Early results of this sub-study, of a limited number of patients, suggest that exemestane has no negative effect on triglycerides and HDL cholesterol, which is the good cholesterol."

 

[CanadianBro]

Here are some other interesting facts that make Exemestane quite an impressive estrogen inhibitor.

Exemestane possesses notable testosterone stimulating properties. Whatever weak androgenic activity it may have is more than compensated for by its strong ability to lower estrogen levels.

This action, of course, reduces the suppressive signal estrogen sends to your brain (estrogen is a main feedback signal to control the release of testosterone), increasing the testicular output of testosterone. In-vivo human studies show clearly that Exemestane will suppress estrogen concentrations at levels that were not high enough to suppress gonadotropins.

Studies using oral doses as high as 200mg daily have failed to show any notable suppressive effect towards testosterone concentrations. When the drug was given to men, including oral doses as high as 300mg, we have seen measurable increases in serum testosterone concentrations

The benefits of Aromasin continue into post-cycle therapy. The main focus at this time is of course minimizing the post-cycle hypo-androgenic (low androgen) state by trying to restore the natural production of testosterone.

In most cases some type of anti-estrogen is incorporated into an athlete's post-cycle therapy, due to the effect excess estrogen can have on testosterone release.

Now, Exemestane possesses notable testosterone stimulating properties which would typically be a bad idea during post-cycle therapy as androgens are usually suppressive towards testosterone release. However, with Exemestane, its weak androgenic activity is compensated for by its estrogen suppressing action.

So, it can essentially serve as a small bridge to full testosterone recovery