RAD140, commonly known as Testolone, is a research compound being studied for the treatment of cancer and muscle wasting disorders.
Although it is not yet approved for human use, RAD140 has gained popularity amongst bodybuilders and athletes looking to increase muscle mass. Read on to learn more about RAD140 and its effects on the body.
Note: By writing this post, we are not recommending this drug. Some of our readers who were already taking the drug requested that we commission a post on it, and we are simply providing information that is available in the scientific literature. Please discuss your medications with your doctor.
What is Testolone (RAD140)?
RAD140, also known as Testolone, is a new compound that is gaining popularity. It belongs to a class of molecules called selective androgen receptor modulators, or SARMs. SARMs bind to the androgen receptor, which is the main site of action of the hormone testosterone. RAD140 is currently being investigated for the treatment of muscle deterioration and breast cancer [R].
Androgens and Androgen Deficiency
Androgens are steroid hormones (like testosterone, dihydrotestosterone, and androstenedione) that are present in both men and women.
Aside from their main role in sexual development and function, androgens also influence bones, muscles, the liver, and the brain [R].
Both men and women need androgens to remain healthy, but as we age, these hormones begin to decline. This decline is associated with a loss of muscle mass and physical strength, often causing broken bones and physical disability. Additionally, it is associated with cancers, the progression of AIDS, and growth failure [R, R].
Testosterone replacement therapy is a common approach to treating androgen deficiency-related diseases. Although this form of therapy is effective, it results in a number of unwanted side effects, some as serious as prostate cancer in men and infertility in women [R, R].
SARMs provide a new approach to treating hormone-related disorders.
SARMs selectively activate the androgen receptors in specific tissues like bone and muscle without activating them in other tissues. This selectivity makes SARMs favorable to current hormone replacement therapies because it limits side effects [R].
RAD140 has recently gained popularity amongst bodybuilders. The selective activity in bone and muscle increases growth and build. It is therefore considered an anabolic compound, meaning that it increases protein use and the formation of new molecules [R].
Unlike other hormones therapies, RAD140 can be taken orally [R].
The FDA has not yet approved RAD140 for use in humans. However, it can be purchased online as a supplement.
Mechanism of Action
RAD140 is a nonsteroidal selective androgen receptor modulator (SARM). It stimulates androgen receptors in the bone and the muscle with greater affinity than in the reproductive organs [R].
RAD140 is selective because of the way different proteins interact with the androgen receptor once RAD140 binds. Different cells will respond to RAD140 binding by releasing different proteins. The proteins can then either initiate or inhibit the effects of RAD140 at the androgen receptor. This results in only some androgen receptors being activated throughout the body, but not all [R, R].
The structure of RAD140 is also unique and does not mimic the steroidal structure of other hormones like testosterone. This is beneficial because it prevents the conversion of RAD140 into other hormones that may be active in undesirable ways [R].
RAD140 stimulates bones and muscles while inhibiting the prostate and the seminal vesicles, which are responsible for sperm production. Additionally, RAD140 does not increase liver enzymes and is considered to have low toxicity in rats [R].
RAD140 also activated androgen receptors in injured brain regions, such as the hippocampus, in rats. It activates specific biochemical pathways (MAPK pathway) that improve cellular health and viability [R].
Potential Uses of RAD140
1) Increasing Muscle Mass
Many severe diseases like cancer, AIDS, and multiple sclerosis cause cachexia, or unhealthy levels of weight loss of both fat and muscle tissue. This results in muscle wasting (loss of muscle tissue), fatigue, and weakness that make recovery even harder [R].
RAD140, like other SARMs, mimics the positive effects of testosterone for bodybuilders while limiting the side effects. Although the benefits of RAD140 itself have not been proven, drugs of this class (SARMs) can help bodybuilding by increasing strength and power [R].
2) Breast Cancer
RAD140 is showing promising results in treating breast cancer that tests positive for androgen and estrogen receptors (AR/ER+ breast cancer). In cells taken from patients with AR/ER+ breast cancer, RAD140 treatment suppressed cancer cell growth by blocking the effects of estrogen on tissues [R, R].
Specifically, RAD140 prevents the production of a protein called ESR1, which is implicated in the development of cancer [R].
3) Neurodegenerative Diseases
Androgens are generally able to decrease amyloid beta accumulation, increase brain cell growth and synaptic plasticity (this is important for learning and memory). Some of these effects are attributed to the conversion of these androgens into other steroidal hormones like estrogen [R].
However, because RAD140 does not have the same structure as typical androgens, it is not converted to other hormones. Therefore, some of these neuroprotective effects may be lost [R].
4) Weight Loss
People supplementing with RAD140 report fat loss over time, but clinical studies have not proven this. RAD140 can indirectly decrease fat tissue by increasing muscle, making it favorable for patients looking to lose weight without impacting lean muscle mass.
There is no set dose for RAD140, as it has yet to be clinically investigated in humans. However, it is typically advised to be used in dose ranges of 20 to 30 mg/day.
Post Cycle Therapy
Bodybuilders using muscle building androgens like traditional steroid hormones or SARMs need to use these substances in cycles. Typically, users will supplement with the substance consistently for 8 to 12 weeks. After a cycle is completed, users need to stop supplementing to allow hormones to return to their natural levels.
This is called post cycle therapy, or PCT, and it is a necessary process to ensure the safety of supplementing with hormones [R].
The length of a PCT may vary but often correlates with the length of the dosing period. For example, if a person supplements for 8 weeks consecutively, they should in turn stop treatment for the same amount of time. However, some people may require longer periods of time to recover from supplementing [R].
Limitations and Caveats
RAD140 is a promising candidate for the treatment of a number of chronic illnesses, but these benefits have yet to be explored in human studies.
RAD140 has only been tested in rats and nonhuman primates. Although it is purchased and used as a supplement by athletes, the long-term benefits and risks of human use are unknown.
It is important to note that the results seen in animal studies are not always representative of the benefits to humans.
Risks and Side Effects
RAD140 is a very new investigational substance and therefore there are no clinically reported side effects. The low side effect profile is attributed to the selectivity of action in the body [R].
This does not mean that RAD140 has no side effects or that it is risk-free. The risks have yet to be determined.
- Breast tenderness/growth in men
- Abnormal body hair growth in women
- Changes in sex drive
- Male pattern baldness/hair loss
- Mood swings and anxiety/depression
- Nausea and vomiting
The most commonly user-reported side effect is hair loss and shedding. This is said to stop after the drug is stopped.
RAD140 vs. Ostarine
Currently, the most researched and commonly used SARM is Ostarine, also known as Enobosarm. Ostarine resembles RAD140 in a number of ways. They are both nonsteroidal, meaning they are structurally different from natural steroid hormones. This also means that they cannot be converted to other hormones in the body. Both have minimal effects on reproductive organs and other tissues [R, R].
Ostarine is currently being tested in humans for its ability to treat osteoporosis and improve unhealthy weight loss (cachexia) seen in severe illnesses [R].
Ostarine is very popular with bodybuilders for its ability to decrease fat tissue and increase muscle mass. However, opposite to RAD140, Ostarine is considered to be more useful for fat loss than it is for muscle mass increase [R].
World Anti-Doping Association (WADA), an organization that monitors the use of drugs in sports, banned Ostarine. Detection of SARMs in the blood of athletes can lead to these athletes being banned from participating in sports [R].
Because RAD140 is such a new substance, the WADA has yet to ban its use in particular. However, it has no approved use in humans to date and its use should be approached with this in mind [R].
Genes That May Influence RAD140 Results
Patients with hormonal imbalances or androgen deficiencies should approach the use of RAD140 with caution [R].
Mutations in the gene coding for the androgen receptor, AR, may change the body’s response to RAD140. Depending on the nature of the mutation, RAD140 can have increased or decreased activity in the body. Patients with variations in this gene may also be susceptible to more side effects with RAD140 [R, R].
As a bodybuilding supplement, people have found that RAD140 successfully aids in lean muscle mass development and in the loss of fat tissue. It has also been reported to improve speed, stamina, and endurance during exercise, which accelerates the rate of fat tissue loss and muscle growth.
RAD140 reportedly exhibit its benefits in a short amount of time relative to other SARM’s. Most dosing cycles consist of 8 to 12 weeks, but RAD140 can benefit some people within as little as 4 weeks. The amount of time taken to see results depend on the individual and their natural metabolism/fitness levels.
Because RAD140 is selective for certain tissues, it has a very small effect on testosterone release. This makes it useful for women who wish to increase muscle mass and build without becoming more masculine.
Even though the release of testosterone is low, you should still follow a PCT period to promote natural hormone production.
Alternatively, some people prefer to use RAD140 during their PCT only and continue to use androgenic steroids as their main substance for bulking up. This may be beneficial by maintaining the muscle mass gained during bulking, bridging the gap between cycles.
There are vendors who sell RAD140 online, we at SelfHacked advise against using this drug given that its safety has not been confirmed in humans.