Methosarb (Calusterone)

Methosarb

Methosarb, known by its chemical name Calusterone, is an anabolic-androgenic steroid (AAS) that falls under the category of synthetic derivatives of testosterone. It has been explored for various medical applications, including as a potential treatment for breast cancer, but like many steroids, it has also found its way into the realm of performance enhancement and bodybuilding.

Calusterone is characterized by its unique structure that makes it resistant to metabolism by the enzyme 5-alpha reductase. This attribute means it does not convert to dihydrotestosterone (DHT) in the body, reducing the risk of androgenic side effects such as hair loss, acne, and prostate enlargement, which are commonly associated with other anabolic steroids. Its anabolic effects are considered to be moderate, making it less potent in terms of muscle mass gain compared to more powerful steroids.

One of the distinctive features of Calusterone is its oral bioavailability, thanks to a modification in its structure that allows it to withstand first-pass metabolism in the liver. This makes it convenient for users who prefer oral administration over the injectable forms of steroids.

Despite its potential, Calusterone is not widely used or well-known among bodybuilders and athletes, partly due to its moderate anabolic properties and the availability of more potent alternatives. Additionally, its use is limited by the lack of extensive research on its long-term effects and its status under the law and sports regulations, where it is likely classified as a prohibited substance.

Side effects of Calusterone can include those typical of anabolic steroids, such as alterations in cholesterol levels, liver toxicity, potential impacts on cardiovascular health, and suppression of natural testosterone production, necessitating a post-cycle therapy (PCT) to restore hormonal balance.

Overall, while Methosarb (Calusterone) presents some interesting characteristics, especially for those concerned about androgenic side effects, its role in bodybuilding and athletic performance enhancement remains minor compared to more commonly used anabolic steroids.

It is a 17-alpha-alkylated (17aa) anabolic steroid

Calusterone (Methosarb) is a 17-alpha-alkylated (17aa) anabolic steroid. The 17-alpha-alkylation modification is a chemical alteration that allows the steroid to be orally active and bioavailable by making it resistant to breakdown by the liver during the first pass. This alteration enables Calusterone to maintain its efficacy when taken orally, which is a desirable trait for those preferring pill form over injections.

The 17aa modification, while increasing the oral bioavailability of anabolic steroids, also raises concerns regarding liver toxicity. Steroids with this modification can be more stressful to the liver compared to their non-17aa counterparts. Therefore, individuals using 17aa steroids, including Calusterone, should be mindful of the potential for liver damage and may consider monitoring their liver health through regular blood tests, especially during longer cycles or when using higher dosages.

Side effects

Given Methosarb (Calusterone)’s unique properties and its relatively mild nature as an anabolic steroid, the side effects are expected to be less severe than those associated with more potent anabolic steroids. However, it’s important to recognize that even less potent steroids can cause side effects, especially when used at higher dosages or for extended periods. Potential side effects of Methosarb may include:

  1. Liver Toxicity: Despite being considered milder, any oral steroid, especially those that are 17-alpha-alkylated (17aa), can pose risks to liver health. Methosarb’s impact on liver enzymes and overall liver function would be a concern, particularly with long-term use.
  2. Suppression of Natural Testosterone Production: Like other anabolic steroids, Methosarb can suppress the body’s natural testosterone production, potentially leading to testicular atrophy, decreased sperm count, and infertility. This effect underscores the need for post-cycle therapy (PCT) to help restore natural hormone levels.
  3. Cardiovascular Risks: Steroid use can affect cholesterol levels, increasing the risk of cardiovascular disease. This includes potential increases in LDL (“bad”) cholesterol and decreases in HDL (“good”) cholesterol, as well as elevated blood pressure.
  4. Androgenic Side Effects: Although Methosarb is designed to minimize androgenic effects, there’s still a risk of experiencing typical androgenic side effects such as acne, hair loss (for those genetically predisposed to male pattern baldness), and increased body hair growth.
  5. Estrogenic Side Effects: Depending on the compound’s ability to aromatize (convert to estrogen), there may be a risk of estrogenic side effects such as gynecomastia (development of breast tissue in men) and water retention. However, the extent of these effects with Methosarb specifically may be limited due to its structure and potency.
  6. Psychological Effects: Steroid use can sometimes lead to psychological effects, including mood swings, aggression, and depression.

It’s essential to approach the use of Methosarb or any steroid with caution, acknowledging the potential health risks and considering the legal and ethical implications, especially within competitive sports. Consulting with a healthcare provider before starting any steroid regimen is advisable to mitigate risks and ensure safe usage.

Summary

This drug is so significantly modified at the carbon 7-beta position that it barely qualifies as an anabolic steroid or androgen. Its effectiveness for building muscle or enhancing athletic performance is almost negligible, making it unsuitable for use in these contexts, even alongside potent anabolic steroids like Dianabol, Deca-Durabolin, Trenbolone, or testosterone.

Though it was never approved by the FDA for male use, the dosages that might be considered therapeutic could reach up to 200 mg/day, but its use is not advisable for women.

Additional context suggests that high doses needed to potentially impact testosterone or muscle growth would also likely suppress natural testosterone production. Yet, the mild nature of Methosarb means achieving such an effect is improbable. Essentially, even at high doses, the body may only absorb a small amount, with the rest being excreted as waste, limiting its potential for both positive effects and side effects.

Raw Data

  • Manufacturer: Not Manufactured
  • Molecular Weight: 316.478
  • Formula: C21H32O2
  • Melting Point (base): 128 oC
  • Effective Dose (Men): Approx. 200 mg/day (Not FDA approved For Men)
  • Effective Dose (Women): Approx. 200 mg/day
  • Half-Life: Unknown
  • Detection Time: Unknown
  • Anabolic/Androgenic Ratio: Unknown but virtually none
  • 17-beta-hydroxy-7-beta, 17-dimethylandrost-4-ene-3-one
  • 17 beta-OH-7 beta, 17 alpha-dimethyl-androst-4-ene-3-one
  • 7 beta, 17 alpha-dimethyltestosterone