Arimistane, also known by its chemical name Androsta-3,5-diene-7,17-dione, is a synthetic anabolic-androgenic steroid. It gained popularity in bodybuilding circles as an aromatase inhibitor (AI), a compound that blocks the enzyme responsible for converting male hormones (androgens) into female hormones (estrogens). Its rise in popularity was largely fueled by its online availability as a "dietary supplement," despite strong evidence of its illegality and potential health dangers. While many users sought to control estrogen-related side effects from anabolic steroid cycles or to increase testosterone, regulatory bodies like the FDA and WADA have taken firm action against it.
The Role of Aromatase and its Inhibition
Aromatase is a crucial enzyme in the steroid synthesis pathway. It converts androgens, specifically testosterone, into estrogens. The balance between androgens and estrogens is essential for proper physiological function in both males and females. In males, excess estrogen can lead to undesirable side effects, such as gynecomastia (enlarged male breast tissue), bloating, and low libido. Aromatase inhibitors are designed to disrupt this conversion process.
The Mechanism of Arimistane
Arimistane is classified as a "suicide inhibitor" of the aromatase enzyme. This means it irreversibly binds to the enzyme's active site, permanently deactivating it. This action effectively reduces the number of active aromatase enzymes available in the body, which, in turn, decreases the conversion of testosterone to estrogen. The irreversible nature of its binding distinguishes it from non-steroidal inhibitors that can release from the enzyme, potentially allowing estrogen levels to rebound. However, this potent action comes with significant and unpredictable risks.
The Banned Substance and Regulatory Status
Arimistane's reputation shifted dramatically due to its classification by major regulatory bodies. It is not an approved medical drug but a synthetic steroid often mislabeled as a dietary supplement.
World Anti-Doping Agency (WADA) Ban
Since 2017, arimistane has been on the World Anti-Doping Agency's (WADA) Prohibited List. It is categorized as a Hormone and Metabolic Modulator, meaning its use is forbidden in all competitive sports, both in-competition and out-of-competition. This ban is a direct response to its ability to artificially manipulate hormone levels, giving athletes an unfair performance-enhancing advantage.
FDA Action and Legal Status
The U.S. Food and Drug Administration (FDA) has explicitly stated that arimistane is not a legal dietary ingredient. The agency has sent warning letters to companies selling products containing Androsta-3,5-diene-7,17-dione, declaring that these products are adulterated and misbranded. The FDA considers arimistane an unapproved new drug and a misbranded prescription drug because it cannot be used safely without the supervision of a licensed practitioner.
Purported Uses and Misleading Marketing
Online retailers and supplement manufacturers have aggressively marketed arimistane for several unproven uses, primarily targeting the bodybuilding and fitness communities. These purported benefits include:
- Post-Cycle Therapy (PCT): Following a cycle of anabolic steroids, PCT is used to help restore the body's natural hormone production. Arimistane is sold for this purpose, claiming to help balance hormones and prevent estrogen rebound.
- Testosterone Boosting: By blocking the conversion of testosterone to estrogen, it is marketed as a way to increase the body's free and total testosterone levels.
- Body Composition and Aesthetics: Promoters claim it can create a 'harder,' more defined physique by reducing subcutaneous water retention and body fat.
Significant Health Risks and Side Effects
Given its status as a synthetic steroid and unapproved drug, arimistane's side effects are not well-studied in humans. However, based on its mechanism and the documented risks of other similar substances, several dangerous health effects have been identified.
Potential Adverse Effects
- Liver and Kidney Damage: Reported side effects include damage to both the liver and kidneys, potentially leading to long-term dysfunction.
- Decreased Bone Mineral Density: Aromatase inhibitors can lead to a reduction in bone mineral density, increasing the risk of osteoporosis and fractures, especially with prolonged use.
- Hormonal Imbalances: While intended to modulate hormones, the unregulated inhibition of estrogen can lead to significant and potentially harmful hormonal imbalances.
- Behavioral Changes: Behavioral changes have been reported, though the exact mechanisms are not fully understood.
- Hair Loss: Some users have reported experiencing hair loss as a side effect.
- Joint Pain and Stiffness: Like medically-approved aromatase inhibitors, unregulated versions can cause significant joint pain and stiffness (arthralgia).
Arimistane vs. Medically-Approved Aromatase Inhibitors
Feature | Arimistane (Androsta-3,5-diene-7,17-dione) | Medically-Approved AIs (e.g., Exemestane) |
---|---|---|
Regulatory Status | Not a legal dietary ingredient; classified as a banned synthetic steroid. | FDA-approved prescription drug. |
Availability | Primarily through online supplement vendors, often deceptively labeled. | Requires a doctor's prescription and dispensing by a licensed pharmacist. |
Uses | Marketed for bodybuilding, PCT, and increasing testosterone. Not scientifically supported and banned in sports. | Approved for treating hormone receptor-positive breast cancer in postmenopausal women. |
Scientific Evidence | Lack of good scientific evidence to support its purported uses. | Extensively studied in clinical trials for approved medical conditions. |
Oversight | No quality control or standardization. Often mislabeled. | Manufacturing, quality, and dosing are rigorously controlled and standardized. |
Safety Profile | Associated with serious health risks including liver/kidney damage. | Documented side effects, but managed under medical supervision. |
Conclusion: The Verdict on Arimistane
While marketed with promises of enhanced muscle growth and hormonal optimization for bodybuilders, arimistane is a dangerous and unregulated synthetic steroid. Its status as a banned substance by WADA and an illegal ingredient by the FDA should serve as a stark warning to anyone considering its use. The potential for severe and permanent health consequences, including liver and kidney damage, outweighs any speculative benefits. Medically-approved aromatase inhibitors exist for legitimate, supervised therapeutic uses, but arimistane is not among them. Consumers are strongly advised to avoid this substance and consult healthcare professionals for any concerns regarding hormonal health or athletic performance.
- For further information on the FDA's stance, see the official FDA Warning Letter on Arimistane.