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RagingWhoreMoan
01-20-2014, 11:51 PM
Formestane
Chemical Name(s):
4-Hydroxyandrost-4-ene-3, 17-dione
4-hydroxy-4-androstene-3,17-dione
4-Hydroxyandrostenedione

Chemical Formula:
C19H26O3

Molecular Weight:
302

CAS:
NA

Q Qatio:
NA

Anabolic #:
NA

Androgenic #:
NA

Oral Bioavailability:
Estimated at 4%

AR Binding Affinity:
NA

SHBG Binding Affinity:
NA

Half Life:
2-3 hours oral, Transdermal: Varies by matrix

Legal Status (US):
Not listed as a controlled substance

Average Dose:
Aromatase inhibition
100-200mg/day (transdermal)
150-250mg/day (oral)
Anabolic effects
800-1000mg/day (oral)

Average Cycle Length:
4-8 weeks

Ratings (On Scale of -5 to +5):

Muscle Gain: +1
Strength Gain: 0
Fat Gain (Negative Indicates Fat loss): -1
Water Retention: +1
Aggression: 0
Libido: -1
Acne: 1
Hair Loss: 0
Prostate Enlargement: 0
Liver Toxicity: 0
Lethargy 0

Characteristics

Formestane is a steroidal aromatase inhibitor, known as a suicidal inhibitor because it permanently binds to the aromatase enzyme.

Formestane was originally used as an injectable for breast cancer patients, but due to its possible androgenic effects it has largely been replaced by non-steroidial AIs in the medical community. Most of its use is now is limited to the bodybuilding community since it is available as a legal dietary supplement for reducing estrogen and increasing testosterone production.

Although formestane can effectively reduce estrogen through oral consumption, its low oral bioavailability has lead to the development of several transdermal based products (which appear to offer higher efficacy at a lower dose).

Relative to 6-oxo and ATD, Formestane is a more potent aromatase inhibitor, which appears to effectively reduce natural estrogen levels by as much as 50% within several days (while higher doses may further suppress estrogen). Because of formestanes potent ability at reducing estrogen it will tend to reduce HDL levels, while increasing LDL levels, thus harming the cholesterol profile. For this reason, it is recommended to limit cycles of formestane to 8 weeks max.

Because formestane also has a strong affinity for the 5a-reductase enzyme it will reduce DHT levels in the body by effectively competing with testosterone for the 5a-reductase.

Formestane converts to the active androgen 4-hydroxytestosterone which has about half the anabolic potency, and about 25% of the androgenic potency as testosterone. This would suggest that fairly high doses of formestane (800-1000mg/day) could lead to some level of anabolic enhancement (although the amount required for this would surely lead to undesirably low estrogen levels).

Formestane is successfully used as a standalone during re-composition cycles to help reduce “bloat” and fat storage. It can also be used as an anti-estrogen to counter aromatization of aromatizing steroids.

Common Clones:

Formestane by Primordial Performance
Formex by Innovative Body Enhancement (IBE)
Formestane by Competitive Edge Labs (CEL)
Formadex by BCS LABS

References

Anabolic Pharmacology
Seth Roberts (2009)

Presser
02-04-2024, 07:45 AM
Formestane, a steroidal aromatase inhibitor, has found its niche within the bodybuilding community for its dual capabilities in estrogen reduction and anabolic support. Originally developed and used in the treatment of estrogen-receptor-positive breast cancer in post-menopausal women, formestane's role in bodybuilding is distinct and multifaceted, reflecting the complex interplay between hormones in achieving muscle growth and definition.


### Chemical Background and Mechanism


Formestane, known chemically as 4-Hydroxyandrost-4-ene-3, 17-dione, operates as a "suicidal inhibitor" of the aromatase enzyme. This means it permanently binds to the aromatase enzyme, effectively blocking the conversion of androgens into estrogens. This reduction in estrogen levels is crucial for bodybuilders, especially those using anabolic-androgenic steroids (AAS), to minimize estrogenic side effects such as gynecomastia and excessive water retention. Its chemical attributes and potency make it a valuable asset for those looking to enhance their physique through hormonal manipulation【6†source】【7†source】.


### Formestane in Bodybuilding


In the realm of bodybuilding, formestane is primarily utilized for its estrogen-lowering effects and its ability to increase free testosterone levels. By inhibiting the aromatase enzyme, formestane reduces the conversion of testosterone into estrogen, thereby increasing the availability of testosterone for muscle growth and recovery. This action not only supports anabolic processes but also helps in reducing fat storage and bloating, creating a leaner and more defined physique【6†source】【7†source】.


Moreover, formestane's capacity to lower sex hormone-binding globulin (SHBG) levels further elevates free testosterone, enhancing anabolic effects and improving muscle strength and size. These benefits are particularly sought after by bodybuilders during cutting phases or when attempting to maintain lean mass while reducing body fat【7†source】.


### Administration and Dosage


Formestane can be administered orally or transdermally, with the latter being preferred due to its higher efficacy at lower doses and its ability to bypass the liver, reducing potential hepatotoxicity. Typical dosages for aromatase inhibition range from 100 to 200mg per day when applied transdermally, and for anabolic effects, doses can go up to 800-1000mg per day. However, due to its potent estrogen-lowering effects, it is advised to limit formestane cycles to a maximum of 8 weeks to avoid adverse effects on cholesterol levels and overall health【6†source】.


### Legal Status and Availability


It's important to note that formestane's legal status has shifted over the years. Once available as a legal dietary supplement, changes in legislation, particularly in the United States with the Designer Steroid Anabolic Control Act of 2014, have moved formestane to the realm of controlled substances, limiting its availability to the black market for bodybuilding purposes【7†source】.


### Conclusion


Formestane's role in bodybuilding underscores the intricate balance of hormones necessary for optimal muscle growth and fat loss. Its powerful effects as an aromatase inhibitor and anabolic agent make it a valuable, albeit controversial, tool in the bodybuilder's arsenal. As with any substance that alters hormone levels, careful consideration, and responsible use are paramount to maximizing benefits while minimizing risks. The evolving legal landscape also necessitates a cautious approach to its acquisition and use within the bodybuilding community.