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  #1  
Old 04-10-2004, 01:33 PM
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Aromasin

??????

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.
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Old 06-17-2004, 02:22 AM
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Good stuff bass, thanks!

Doing a little research on this, thinking about running it... Sumbled across this. For anyone who wants to read the full profile at the FDA website, here's the link...

http://www.fda.gov/cder/foi/label/1999/20753lbl.pdf
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Old 06-21-2004, 03:50 AM
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I was thinking about adding some for my cycle to help cut up and keep bloat down!
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Old 05-07-2013, 04:33 PM
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Aromasin - Exemestane

Exemestane is a steroidal suicide aromatase inhibitor/irreversible aromatase inactivator, lowering production of estrogen in the body by blocking the aromatase enzyme. Similar in structure to formestane, exemestane’s medical use like most aromatase inhibitors is for treatment of estrogen-dependent breast cancer. It is usually only prescribed in those cases where therapies using less aggressive compounds have not produced the results hoped for, such as selective estrogen receptor modulators.

For use by strength athletes and bodybuilders, exemestane has several properties that would be beneficial. First, exemestane reportedly can lower estrogen 85% on average (1). In doing so of course this will aid in the prevention of estrogen related side effects caused by aromatizing steroids. The drug also raises testosterone levels in users which can be advantageous if used during post-cycle therapy (2). Add to this the fact that there is some evidence that exemestane may elevate levels of insulin growth factor [IGF] (3).

Like other aromatase inhibitors, there is also conflicting information and studies regarding the effect that exemestane has on users blood lipids/cholesterol, with some studies indicating that the compound has little to no effect while others say that it is quite harsh (4,5).


Use/Dosing

Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose (1). The active life of the drug is between 24 and 30 hours. This is significant since it is quite shorter than for the non-steroidal inhibitors (1). A single oral dose of 25 milligrams of exemestane causes a relatively long-lasting reduction in plasma and urinary estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persists for about 4 to 5 days (1, 4).

It has been shown that 25 milligrams of exemestane is basically just as effective as 50 milligrams at suppressing estrogen, raising testosterone levels, and levels of IGF (2). It is therefore unnecessary to go higher in doses than 25 milligrams per day. Due to the active life of the compound exemestane should be administered roughly once every twenty-four hours.

It appears that the only negative aspect of the compound in terms of the dosing schedule is that it takes approximately seven days for it to reach steady blood plasma levels. However, this is not a major hindrance to its use. It just simply requires that a user begin using exemestane a week prior to when they want the effect of the compound to be full realized.


Risks/Side Effects


Exemestane has no significant drug toxicity at doses up to 600 milligrams per day. It is well tolerated by most users with the maximum tolerated dose toxicity not yet being identified (1). Negative side effects related to the use of this compound are usually quite mild and can include things such as transient gastrointestinal effects, hot flashes, nausea, and/or fatigue (1, 2). As previously mentioned, the effect of exemestane on the blood lipids/cholesterol are unknown due to the conflicting research and therefore should be monitored when using the compound. Sexual dysfunction is also a possibility due to the lowering of estrogen levels as well. However reports of this are relatively rare.

Due to the mild negative side effects associated with the compound, as well as the potency of the drug in alleviating estrogen-related side effects when administering aromatizing anabolic steroids, exemestane is seemingly a relatively safe choice when looking for an aromatase inhibitor.


References

1. Brueggemeier RW. Overview of the pharmacology of the aromatase inactivator exemestane. Breast Cancer Res Treat 2002;74:177-185.

2. 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. 2003 Dec;88(12):5951-6.

3. Martinetti A, Zilembo N, Ferrari L, Massimini G, Polli A, La Torre I, Giovanazzi R, Pozzi P, Bidoli P, De Candis D, Seregni E, Bombardieri E, Bajetta E. Bone turnover markers and insulin-like growth factor components in metastatic breast cancer: results from a randomised trial of exemestane vs megestrol acetate. Anticancer Res. 2003 Jul-Aug;23(4):3485-91.

4. Buzdar AU. An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane. Cancer. 2002 Nov 1;95(9):2006-16.

5. Atalay G, Dirix L, Biganzoli L, Beex L, Nooij M, Cameron D, Lohrisch C, Cufer T, Lobelle JP, Mattiaci MR, Piccart M, Paridaens R. The effect of exemestane on serum lipid profile in postmenopausal women with metastatic breast cancer: a companion study to EORTC Trial 10951, 'Randomized phase II study in first line hormonal treatment for metastatic breast cancer with exemestane or tamoxifen in postmenopausal patients'. Ann Oncol. 2004 Feb;15(2):211-7.
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Old 05-08-2013, 03:08 AM
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Good read!
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Old 05-08-2013, 06:29 AM
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I was very happy with the Maximpep exemastane....see the review!!!!
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