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What is Exemestane?

Exemestane is the active ingredient used in a few different medications primarily used to treat women suffering from breast cancer.  The most common of these medications is called Aromasin, thought there are a number of competitors.  

Exemestane is an aromatase inhibitor, which is a type of antiestrogen class, and readily available for your research and testing.  There are a few different types of breast cancer, but the most common types found in otherwise healthy humans are estrogen based; They require estrogen to grow.  Exemestane based medications like Aromasin are leveraged to decrease estrogen and stifle the cancer growth and spread.

Mechanism of Action

Typically ingested orally, exemestane is an irreversible steroidal aromatase inactivator.  In other words, exemestane is part of the same generalized class of drugs that contain medications used to treat breast cancer in women and gynecomastia in men.  These inhibitors work by blocking the enzyme aromatase. Aromatase is what turns androgen into estrogen in postmenopausal women and in men. It also is the leading stimulator for ovaries to create estrogen in premenopausal women.  By inhibiting aromatase’s efficacy, exemestane and the other aromatase inactivators are able to control and limit the production of estrogen.

Side Effects, Overdose Risk, and Other Unintentional Interactions

First and foremost, it’s worth mentioning that nobody has ever overdosed on exemestane.  It would seem that it is virtually impossible to do. Doubling, tripling, quadrupling, or increasing the recommended amount of use doesn’t seem to do anything other than stop estrogen production altogether.  The lack of overdose risk makes exemestane more attractive than the other aromatase inhibitor options.

As for side effects, exemestane is relatively harmless there too.  The leading side effects include those of which every woman experiences when they start to go through menopause.  Hot flashes, some light sweating, and potential insomnia all have been reported by users. Limiting or preventing estrogen production is essentially forcing your body into a menopausal state, so it’s not surprising you’d experience the same symptoms.

Since the liver is responsible for breaking down exemestane medications, most physicians will verify liver health before prescribing.  This is especially true in patients suffering from breast cancer. An already weakened liver shouldn’t receive more added stress through medication.  Subsequently, patients must not take other medications simultaneously that may increase or promote estrogen production. It will negate the purpose of both medications and simply cause unnecessary harm to the liver and kidneys.

Other Benefits/Use Cases

Exemestane has been found to counteract fat and water retention, which isn’t all that different from the treatment of gynecomastia.  Excessive aromatase production due to testosterone supplementation has been studied pretty thoroughly. Exemestane has been proven to help counteract those problems.

Exemestane has been found to increase the levels of the luteinizing hormone and the follicle stimulating hormones in humans.  Increasing these hormone levels will further escalate the total number of male sexual hormones over female sexual hormones, resulting in improved physical performance.  Physical performance can be characterized such as strength gains, quickness, and reaction time.

1 Higa, G M. “Exemestane: Treatment of Breast Cancer with Selective Inactivation of Aromatase.” Current Neurology and Neuroscience Reports., U.S. National Library of Medicine, 15 Nov. 2002, www.ncbi.nlm.nih.gov/pubmed/12455303.

2 D J Handelsman. “Indirect androgen doping by oestrogen blockade in sports.” British Journal of Pharmacology., U.S. National Library of Medicine, 21 Apr. 2008, www.ncbi.nlm.nih.gov/pubmed/12455303.

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