Arimistane

What is Arimistane?

Arimistane or Androsta-3 5-diene-7 17-dione is an aromatase inhibitor. This compound is also an analog of DHEA, an androgenic hormone made by your adrenal glands. Arimistane also exists naturally in the body and was first discovered in human urine in 1971. [R]

Later on, in the early ’90s, Arimistane was synthesized and tested for its ability to inhibit aromatase in human placental microsomes.All the steroids used in the study, including Arimistane, inhibited the enzyme competitively, with Ki values ranging from 0.058 to 45 µM (micromolar).

Do Aromatase Inhibitors Potentially Increase Testosterone?

Research has shown that lowering estrogen levels, by administering an aromatase inhibitor, causes an increase in luteinizing hormone (LH), follicle-stimulating hormone (FSH), and testosterone. Aromatase inhibitors have therefore been suggested as a tool to increase testosterone levels. [R]

Another study was conducted to investigate the effects of aromatase inhibition in elderly men with low or borderline-low serum testosterone levels. The study found that aromatase inhibition increases testosterone levels to the youthful normal range, in older men with mild hypogonadism. [R]

Research on Aromatase Inhibitors for Gynecomastia

Multiple case reports indicate that Aromatase inhibitors may be used to treat or prevent gynecomastia or the enlargement of breast tissue in men. Gynecomastia is triggered due to a decrease in the amount of testosterone vis-`a-vis the aromatase enzyme. [R]

In one study, five boys with pubertal gynecomastia and breast tenderness were treated for 6 months with a specific aromatase inhibitor. Breast size decreased in 4 out of 5 patients, and in 1 of these 5 boys, glandular breast tissue disappeared completely. [R]

How Does Arimistane Work?

Arimistane may inhibit aromatase, which could lead to increased testosterone levels. It does this by reducing aromatase activity, thereby lowering estradiol, a form of the hormone estrogen. While it is identified with specific sex, both estradiol and testosterone are found in both women and men.

Arimistane vs Arimidex

Arimistane and Arimidex are both aromatase inhibitors.

Both work by suppressing aromatase, an enzyme that converts androgens into estradiol, a form of estrogen. Both also increase testosterone levels. The duo does that by decreasing the amount of estrogen the body produces.

However, while Arimistane isn’t FDA-approved, Arimidex was FDA-approved in 1995. It is used to treat breast hormone receptor-positive receptors in early breast cancer in postmenopausal women. Arimidex is typically given as an adjuvant treatment after surgery has been administered.

Arimistane Research

Only one human study has been conducted on Arimistane to date. In the study, urine samples of three healthy volunteers were analyzed after a controlled single administration of Arimistane. No relevant effects on the steroid profile could be detected. [R]

Arimistane FAQs

Is Arimistane a prohormone?

Prohormones are naturally occurring compounds that convert to anabolic hormones via enzymatic processes. Arimistane, however, is not a prohormone—it is sometimes described as a ‘suicidal aromatase inhibitor’ because it can bind irreversibly to the aromatase enzyme.

Can Arimistane increase testosterone?

While aromatase inhibitors as a drug class have been shown to increase testosterone in men, there is no direct clinical evidence that Arimistane itself increases testosterone levels in humans.

Is Arimistane legal?

Arimistane is included on the World Anti-Doping Agency’s list of prohibited substances. It is not FDA-approved for medical use, and its sale as a dietary supplement is illegal in the United States. It may still be sold for laboratory research purposes only.

Does Arimistane have any side effects?

Potential side effects of Arimistane in humans are unknown because no controlled safety studies have been conducted. However, aromatase inhibitors as a class can cause joint pain, hot flashes, fatigue, and changes in bone density.

Does Arimistane increase muscle mass in subjects?

Studies investigating the potential effect of this anti-estrogen compound on muscle mass are lacking.

The use of aromatase inhibitors is associated with the maintenance of total body fat, an increase in lean body mass, and free testosterone in AI subjects at 24 months. The mechanisms and implications of these changes require further exploration. [R].

Do aromatase inhibitors prevent estrogen rebound?

According to the American Cancer Society, aromatase inhibitors don’t stop the ovaries from making estrogen. They only limit estrogen levels in female subjects whose ovaries aren’t making estrogen (such as postmenopausal women). [R]

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