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RAD-140 Testolone SARM Studies & Research

Dr. Watson with Umbrella talks about RAD-140, otherwise known as Testolone, which is one of the most widely researched Selective Androgen Receptor Modulators and certainly the one that has generated the most buzz.

What makes RAD-140 particularly interesting is that compared to other SARMs, there are few crucial differences in terms of what is actually being studied preclinically, because the potential indications are quite broad. Overall, the major research findings for RAD-140, thus far, involve one of 4 indications:

  • preventing and treating loss of muscle mass and muscle strength
  • promoting neuroprotection
  • treating breast cancer
  • positioning it to become a superior alternative to Testosterone Replacement Therapy

Given this broad set of applications, RAD-140 obviously has enormous clinical potential, and it aims to address two of the most important aspects of age-related deterioration: physical decline and neurological decline.

RAD-140 Origins & History

So let’s dive into just a few of the preclinical studies that led to such enthusiasm for RAD-140, and then we’ll talk about what comes next.

RAD-140 was first revealed to the world back in 2011 by a biopharmaceutical company called Radius Health, and it was the culmination of their goal of generating a superior tissue-selective modulator of the Androgen Receptor. So, what exactly does “tissue-selective” mean in this context?

In brief, it means they were searching for a single molecule can act as a positive regulator of the Androgen Receptor in some tissues, such as skeletal muscle and bone, yet also act as a negative regular of that same receptor in other tissues, such as the prostate.

RAD-140 SARM Study #1

In their first published study, research was conducted in vivo using both mice and primates, and they showed that RAD-140 was able to increase muscle mass without increasing the size of the prostate. This differentiates RAD-140 from testosterone, which increases both muscle mass and prostate size, which is undesirable.

Intriguingly. despite the dramatic increases in lean body mass over such a short time, there was no elevation of liver enzyme levels in any animal, at any dose, greater than 2 fold over baseline. Considering the well-established relationship between oral androgen use and liver stress, it was quite surprising that even at a dose 10-fold greaterthan the fully effective dose, the authors observed only minimal liver enzyme elevations.

RAD-140 SARM Study #2

The second study was quite intriguing because the researchers hypothesized that RAD-140 is neuroprotective, and they tested this using cultured neurons and adult male rats. This hypothesis may be surprising to you, since most people don’t realize that the brain is actually androgen-responsive, which is why androgens like testosterone can affect mood. In fact, low testosterone is an established risk factor for the development of Alzheimer’s disease (AD), while testosterone supplementation can protect against age-related decline in brain health.

In this study, the researchers wanted to know if RAD-140 could also protect the brain against neurodegeneration, using an animal model of neuron loss relevant to neurodegenerative disease. They tested this using toxins such as amyloid plaque protein and kay-in-ic acid, which is a toxin found in some types of seaweed, which is why you should definitely never eat bad sushi.

What the researchers did was to induce neurodegeneration, while simultaneously dosing testosterone or RAD-140, and then following up by measuring various markers of brain health. Fortunately, what they discovered is that RAD-140 is able to prevent loss of neurons following a variety of chemical insults, thus demonstrating that RAD-140 is indeed neuroprotective. As an added bonus, the male rats also increased muscle mass to the same degree as testosterone supplementation, but without increasing prostate growth.

Finally, a research group in Germany has recently published some exciting results in the Journal of Steroid Biochemistry and Molecular Biology, demonstrating for the first time the unique potency of RAD-140 for binding the Androgen Receptor (AR) using some very sophisticated computer modelling. They compared a variety of SARMs for their binding strength to the Androgen Receptor in human cells and they observed that RAD-140 showed the strongest binding.

The Future of RAD-140

Ok so what comes next for RAD-140?

Well, these are actually very exciting times for anyone interested in RAD-140, because the first set of clinical data is expected to drop before the end of 2020. This really is a pivotal moment, because despite all of the information out there, it is absolutely essential for the research community to have peer-reviewed clinical data on the safety and tolerability of RAD-140, so we are eagerly awaiting those developments.

Now, in terms of drug-delivery research and development, Umbrella Labs has recently developed sublingual-optimized protocols for SARMs, including RAD-140, to overcome the problem of first-pass metabolism in the liver. The rationale for doing so is because first-pass metabolism can dramatically reduce bioavailability and biodistribution, leading to lower potency and increased risk of hepatotoxicity.

This is actually something we’ll discuss in a future video, in much more detail, but suffice it to say that there are a variety of benefits to sublingual absorption under your tongue compared to swallowing, so we are hopeful that future clinical trials will leverage sublingual delivery of SARMs.

As always, please remember that SARMs are not FDA approved for any indication, nor are they dietary supplements, so they are currently for research use only. All clinical research must be done with oversight from the relevant Institutional Review Board, and all preclinical research must be done with oversight from your Institutional Animal Care and Use Committee, following the guidelines of the Animal Welfare Act.

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