RAD-140 (Testolone)

What is RAD-140 (Testolone)?

RAD-140, also known by the development codes EP0062 and the black-market name Testolone, is a selective androgen receptor modulator (SARM). It is a nonsteroidal compound that acts as an agonist of the androgen receptor (AR), which is the biological target of androgens like testosterone and dihydrotestosterone (DHT).

RAD-140 was developed for the potential treatment of conditions such as hormone-sensitive breast cancer, sarcopenia (age-related muscle atrophy), osteoporosis, and weight loss due to cancer cachexia. However, development for these indications has been discontinued, and it is now primarily under development for the treatment of a specific type of breast cancer.

As a SARM, RAD-140 is designed to have a tissue-selective effect. In preclinical studies, it has shown anabolic effects in muscle tissue, while having partially agonistic or antagonistic effects in the prostate gland and seminal vesicles. This selectivity is what distinguishes it from traditional anabolic steroids, which often have a broader, less-selective effect on various tissues, including the prostate.

Side Effects and Benefits

Side Effects:

• Liver toxicity: There have been case reports of drug-induced liver injury associated with the use of RAD-140, and clinical trials have noted elevated liver enzymes.

• Hormonal changes: It can cause a decrease in sex hormone-binding globulin (SHBG) levels and an increase in prostate-specific antigen (PSA), which are markers of androgen receptor engagement.

• Gastrointestinal issues: Vomiting, dehydration, and decreased appetite have been reported.

• Other potential side effects: Hypophosphatemia (low phosphate levels) and weight loss.

Benefits:

• Muscle growth: Preclinical studies have shown that RAD-140 can produce anabolic effects in skeletal muscle.

• Potential for medical use: Its primary potential benefit lies in its tissue-selective action, which could make it a useful treatment for muscle wasting and bone diseases with fewer side effects than traditional steroids. However, as mentioned, these applications are no longer being pursued.

• Breast cancer treatment: It is currently under development for the treatment of androgen receptor-positive, estrogen receptor-negative, HER2-negative advanced breast cancer.

Pros and Cons

Pros:

• Tissue selectivity: It is designed to selectively target muscle and bone tissue while minimizing effects on the prostate, which is a significant advantage over traditional anabolic steroids.

• Oral bioavailability: It can be taken by mouth, unlike many traditional steroids that require injections.

• High affinity for the AR: It binds to the androgen receptor with high affinity, suggesting strong potential for its intended effects.

Cons:

• Not approved for human use: It is a research chemical with limited data on its long-term effects and safety in humans.

• Potential for liver damage: Case studies and clinical trial data have shown a risk of liver injury.

• Banned substance: It is on the World Anti-Doping Agency (WADA) list of prohibited substances and is banned by other athletic organizations.

• Black-market products: Many products sold online as RAD-140 may be mislabeled, contain different substances, or be of unknown purity and concentration, making their use even more dangerous.

Dosage and Frequency

There is no standardized or medically recommended dosage for RAD-140 because it is not approved for human use. The dosages used in limited clinical trials for breast cancer patients were 50 mg, 100 mg, and 150 mg once daily. However, these dosages were administered under medical supervision for a specific condition. Dosages used by individuals for performance enhancement vary widely and are not based on scientific evidence.

Half-Life and Detection Time

• Half-life: The elimination half-life of RAD-140 is approximately 45-60 hours, which supports once-daily dosing.

• Detection time: In athletic drug testing, the detection time for RAD-140 can vary widely depending on the dosage, frequency of use, and the specific testing method. A study in horses showed that it could be detected in plasma for up to 13 days and in urine for up to 6 days. However, more advanced testing methods can detect metabolites for much longer.

Sterogenic, Progestronic, and Prolactin Effects

• Sterogenic/Estrogenic: RAD-140 is a nonsteroidal compound. It does not aromatize into estrogen, which is a common side effect of many traditional anabolic steroids. This means it is not expected to cause estrogen-related side effects like gynecomastia (enlarged male breast tissue).

• Progestronic: RAD-140 shows some affinity for the progesterone receptor, with an IC50 value of 750 nM, which is significantly lower than for the androgen receptor. While it's not a strong progestin, this interaction could potentially have some effects, though they are not well-documented.

• Prolactin: There is no significant evidence to suggest that RAD-140 directly increases prolactin levels. Prolactin-related side effects, such as lactation or gynecomastia, are not typically associated with SARMs like RAD-140, unlike some progestogenic compounds.

Anabolic Androgenic Ratio

The anabolic androgenic ratio of a substance compares its anabolic (muscle-building) effects to its androgenic (masculinizing) effects. Testosterone is the benchmark with a ratio of 100:100 or simply 1:1.

While a specific number for the anabolic androgenic ratio of RAD-140 is often cited on online forums and websites, it is important to note that these numbers are based on preclinical data and are not officially recognized or standardized. The ratio is difficult to determine precisely and can vary depending on the animal model and the specific tissues being measured. Preclinical studies suggest that RAD-140 is highly tissue-selective, with a significant anabolic effect and a minimal androgenic effect on the prostate, which is the basis for its potential as a SARM.