RAD140 Testolone

RAD140 (Testolone) description

RAD140 (Testolone) is a potent, orally bioavailable, investigational nonsteroidal selective androgen receptor modulator (SARM) devoloped by Radius Health, Inc. as a future substitute of exogenous Testosterone replacement therapy (TRT). Current RAD140 research focuses on its potential benefits in increasing muscle mass, fighting muscle wasting, skeleton wasting (osteoporosis), breast cancer and protecting brain cells. RAD140 Testolone has chemical formula C₂₀H₁₆ClN₅O₂ and molecular mass 393.83 g·mol⁻¹.

RAD140 has excellent affinity for the androgen receptor

RAD140 demonstrated excellent affinity for the androgen receptor (Ki = 7 nM versus 29 nM for testosterone and 10 nM for dihydrotestosterone (DHT)) as well as good selectivity over other steroid hormone nuclear receptors, with the closest off target receptor being the progesterone receptor (IC50 = 750 nM vs 0.2 nM for progesterone). In vitro functional androgen agonist activity was confirmed in the C2C12 osteoblast differentiation assay, where an EC50 of 0.1 nM was shown (DHT = 0.05 nM).

RAD140 effectively stimulates the growth of muscle mass

A clinical study published in 2011 examined the anabolic androgenic effect of RAD140 in young primates, male cynomolgous monkeys. The results on animal body weight of 28-day dosing with RAD140 at 0.01 mg/kg, 0.1 mg/kg, and 1 mg/kg are shown in the following figure:

In this study, a mean weight gain of greater than 10% in just 28 days of dosing was achieved at a dose of just 0.1 mg/kg. A similar result was achieved also in the 1.0 mg / kg dose group.

Androgens induce numerous beneficial neural effects

The decline in testosterone levels in men during normal aging increases risks of dysfunction and disease in androgen-responsive tissues, including brain. In brain, low testosterone is an established factor for the development of Alzheimer’s disease (AD). Androgens induce numerous beneficial neural effects relevant to a protective role against AD, including reduction of the AD-related protein β-amyloid (Aβ) and promotion of synapse formation, neurogenesis, and specific aspects of cognition. An androgen action particularly important to neurodegenerative diseases is neuroprotection. Testosterone can increase neuron survival in several cell culture and animal models of injury.

Androgen-based hormone therapy may be an effective approach for the prevention of AD and related neurodegenerative disorders in aging men. However, the use of testosterone therapy has the potential to increase the risks for developing prostate cancer and or accelerating its progression. To overcome this limitation, novel compounds termed “selective androgen receptor modulators” (SARMs) have been developed that lack significant androgen action in prostate but exert agonist effects in select androgen-responsive tissues.

Neuroprotective effects of RAD140

In a scientific study published in 2014, the neuroprotective effects of RAD140 in cultured rat neurons and male rat brain were investigated. Neuroprotection is an important neural action of endogenous androgens that is relevant to neural health and resilience to neurodegenerative diseases.

In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults. Mechanistically, RAD140 neuroprotection was dependent upon MAPK signaling, as evidenced by elevation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126. Importantly, RAD140 was also neuroprotective in vivo using the rat kainate lesion model.

In experiments with gonadectomized, adult male rats, RAD140 was shown to exhibit peripheral tissue-specific androgen action that largely spared prostate, neural efficacy as demonstrated by activation of androgenic gene regulation effects, and neuroprotection of hippocampal neurons against cell death caused by systemic administration of the excitotoxin kainate. These novel findings demonstrate initial preclinical efficacy of a SARM in neuroprotective actions relevant to Alzheimer’s disease and related neurodegenerative diseases.

RAD140 has the potential to fight breast cancer

Breast cancer is the second leading cause of cancer-related death in women. Scientific study published in December 2017 in the journal of the American Association for Cancer Research demonstrated for the first time that RAD140 is an Androgen receptor (AR) agonist in breast cancer cells and suppresses the growth and proliferation of multiple AR/ER+ breast cancer cell line and xenograft models.

Steroidal androgens suppress Androgen receptor (AR) and Estrogen receptor (ER) positive (AR/ER+) breast cancer cells and were used to treat breast cancer, eliciting favorable response. The performed study evaluated the activity and efficacy of the oral Selective androgen receptor modulator RAD140 in in vivo and in vitro models of AR/ER+ breast cancer. A series of in vitro assays were used to determine the affinity of RAD140 to 4 nuclear receptors and evaluate its tissue-selective AR activity. The efficacy and pharmacodynamics of RAD140 as monotherapy or in combination with palbociclib were evaluated in AR/ER+ breast cancer xenograft models.

RAD140 bound AR with high affinity and specificity and activated AR in breast cancer but not prostate cancer cells. Oral administration of RAD140 substantially inhibited the growth of AR/ER+ breast cancer patient-derived xenografts. Patient derived xenografts (PDX) are models of cancer where the tissue or cells from a patient’s tumor are implanted into an immunodeficient or humanized mouse. PDX models are used to create an environment that allows for the natural growth of cancer, its monitoring, and corresponding treatment evaluations for the original patient.

The AR pathway was found to be activated in RAD140-treated breast cancer cells and xenografts, while genes within the ER pathway, including ESR1, were suppressed. In addition, RAD140 treatment was found to decrease the expression of DNA replication–related genes in breast cancer cells, consistent with previous report that these genes were suppressed in androgen-treated prostate cancer cells. Combined administration of RAD140 with the CDK4/6 inhibitor palbociclib was more efficacious compared with either of the agents used alone.

These findings suggest a distinct mechanism of action of RAD140, which includes the AR-mediated suppression of ESR1 in inhibiting AR/ER+ breast cancer growth. The potent antitumor activity and tissue-selective AR activity, along with overall tolerability in animal models and oral availability together lend support to further clinical investigation of RAD140 in AR/ER+ breast cancer patients..

RAD140 (Testolone) and bodybuilding

Similar to anabolic steroids, RAD140 effectively stimulates the growth of muscle mass. However, its safety profile is significantly better compared to steroids. RAD140 has significantly fewer dangerous and undesirable side effects, and the potential health risks are many times lower than those that can be caused by anabolic steroid use. Therefore, RAD140 is also used (abused) by bodybuilders, athletes and people who are trying to achieve a muscular figure, want to achieve similar results as when using steroids, but also want eliminate / minimize possible unwanted side effects. We emphasize that RAD140 is not an approved nutritional supplement or stimulant for athletes: RAD140 is an experimental substance that is still under investigation, its long-term effects are not yet fully known and further research is needed. Keep in mind that RAD140, like all our other products, is sold solely for scientific and research clinical use.

RAD140 and doping

Although RAD140 is not illegal, in professional sports it is prohibited. WADA (World Anti-Doping Agency) banned all Selective androgen receptor modulators (including RAD140) as early as 2008. 

Scientifically investigated possible benefits of RAD140

• • Significant and selective anabolic effect on muscles and bones, without strong androgenic adverse effects on other organs
  • Has strong neuroprotective effects, may be effective in preventing Alzheimer’s disease and related neurodegenerative disorders
  • Has the potential to fight breast cancer
  • Can help treat serious diseases associated with muscle loss
  • Can help protect brain cells and their proper functions
  • May help in the treatment of osteoporosis
  • Helps build and maintain muscle mass
  • May help reduce excess fat

Advantages of RAD140 over Anabolic Steroids

• • RAD140 (Testolone) is selective and primarily aimed at acting in muscles and bones. Due to this selectivity, unlike anabolic steroids, it does not cause strong androgenic negative effects on other organs
  • Similar to anabolic steroids, RAD140 can help achieve significant muscle gains, but has significantly fewer dangerous and undesirable side effects, and the potential health risks are many times lower than those that can be caused by steroid use:
    • • RAD140 does not convert on Estrogens or DHT
      • RAD140 does not cause significant retention of water and salts
      • RAD140 does not cause increased Cortisol levels
      • RAD140 does not cause prostate enlargement
      • RAD140 does not cause kidney disease
      • RAD140 does not cause acne and oily skin
      • RAD140 does not cause swollen face
      • RAD140 does not cause aggression, explosiveness
      • RAD140 is highly effective when administered orally (no injections needed)

RAD140 possible side-effects and risks

• • Suppressed levels of natural Testosterone 
  • Anxiety, depression
  • Nausea and vomiting
  • Possible liver toxicity
  • Abnormal body hair growth in women
  • Excessive hair loss in men (which stops after the end of RAD140 treatment)
  • The long-term effects of RAD140 are unknown

RAD140 (Testolone) FAQ

What is RAD140 Testolone?

RAD140 (Testolone) is a potent, orally bioavailable, investigational nonsteroidal selective androgen receptor modulator (SARM) devoloped by Radius Health, Inc. as a future substitute of exogenous Testosterone replacement therapy.

What is RAD140 used for?

RAD140 is an experimental substance that is still under investigation. Current RAD140 research focuses on its potential benefits in increasing muscle mass, fighting muscle wasting, skeleton wasting (osteoporosis), breast cancer and protecting brain cells.

Does RAD140 build muscle?

The results of clinical trials in young primates conducted confirmed that RAD140 effectively helps increase muscle mass, it has strong anabolic properties, and moreover, it act selectively only in tissues where it is required, in the muscles and bones.

Is RAD140 dangerous for the prostate?

RAD140 is selective for action mainly in muscle and bone, does not convert to dihydrotestosterone, therefore, unlike anabolic steroids, it does not pose a risk to the prostate.

Does RAD140 cause increased cortisol production?

RAD140 does not affect cortisol levels and does not increase its production in the body.

Is RAD140 banned in sports?

Yes, RAD140 falls into the S1 Anabolic Agent category of banned substances in the WADA “Prohibited List”.

Does RAD140 lower testosterone?

RAD140 suppresses the production of natural Testosterone, but considerably less than some anabolic steroids. The effect on the reduction of testosterone production is also influenced by the size of the dose and the length of its use.

Does RAD140 increase DHT?

RAD140 does not convert to estrogens and DHT. Because it has not a steroid structure, reductase and aromatase enzymes (which are responsible for the conversion of androgens to DHT and estrogens), are unable to join.

Is RAD 140 stronger than testosterone?

Bodybuilders claim that both LGD-4033 and RAD140 SARMs allow them to achieve massive muscle gains that are fully comparable to those that can be achieved with the most effective bulking steroids, and consider these SARMs to be a much more effective for building muscle mass than testosterone.

What is the half life of RAD140?

As no results of RAD140 clinical studies in humans are known, the half-life of RAD140 in humans is not known. However, it is estimated that the half-life of RAD140 is about 24 hours in human.

Is RAD 140 Safe?

According to a study conducted by researchers at the University of Southern California, Los Angeles, RAD 140 appears to be safer than testosterone replacement therapy (TRT) in rats. Further research is required to determine if RAD 140 is also safer than TRT in human subjects.

Can RAD140 give you gyno?

Compared to anabolic steroids, the risk with RAD-140 is much lower. However, suppression of testosterone production is sufficient to cause a hormonal imbalance, and such an imbalance may be sufficient to trigger the development of gynecomastia.

Is RAD140 a steroid?

RAD140 is not a steroid. It is investigational Nonsteroidal selective androgen receptor modulator (SARM).

RAD140 dosage

As no results of RAD140 clinical trials in humans are yet known, it is not yet possible to speak of frequently used or safe clinical doses of RAD140 in humans. However, a clinical study performed in young primates showed that even a low dose of 0.1 mg RAD140 per kg body weight has already led to strong anabolic effects and a significant increase in muscle mass. This suggests that RAD140 is a very potent SARM, which begins to show its strong anabolic effects already from relatively low doses.

In various bodybuilding forums and discussions on the internet, bodybuilders and users who have used (abused) RAD140 to build muscle mention 10 mg of RAD140 daily as a basic and sufficient dose to achieve significant results; and a cycle duration of 6-8 weeks. In the case of more experienced (hardcore) bodybuilders, there is talk of an optimal dose of 20 mg RAD140 per day and a cycle duration of 8 to 10 weeks. However, none of these doses are based on any scientific research.

We emphasize that RAD140 is not an approved nutritional supplement or stimulant for athletes. It is an experimental substance that is still under investigation and not all of its side effects may be known. Keep in mind that RAD140, like all our other products, is sold solely for scientific and research clinical use.