RAD-140
Description
RAD140 is non-steroidal Selective Androgen Receptor Modulator (SARM). Drugs of this class mimic many of the beneficial actions of anabolic steroids, but are often quite removed from these drugs structurally. This often allows for
much higher anabolic-androgen separation, and differing side effect potential. The objective is typically to maximize stimulation of bone and muscle anabolic effects, and minimize other androgenic spillover, particularly in the
prostate. This drug is commonly used in the fitness community, as a muscle-building alternative to anabolic steroids.
In-vitro studies show that RAD140 has a much higher binding affinity (Ki= 7 nM) for the androgen receptor (AR) than
testosterone (Ki 29nM), and even
dihydrotestosterone (Ki= 10 nM). It appears to highly favor activity in muscle and bone as well, with only a weak potentially antagonistic effect in androgenic tissues. AR receptor specificity appears high also. RAD140 does not
interact with other steroid hormone receptors to any appreciable degree, barring extremely weak interaction with progesterone (IC50 = 750 nM). This is all suggestive of a drug with a refined anabolic profile. Such selective
anabolic activity is very much in line with the clinical objective of most SARMs.
RAD140 is in preclinical development. It has only been progressed as far as animal studies at this time. During these investigations, we’ve noted several interesting findings. First, in studies using rats, the drug had a stronger anabolic effect than testosterone propionate mg for mg. A
similar effect was noted with TP, but at a 40% higher dose.
On the other hand, RAD140 was far less androgenic. It required a 60 times higher dosage to produce the same prostate growth. In studies with monkeys, which considered more clinically, to clinically relevant to humans, the drug
was again shown to be a potent anabolic agent. Here, the total bodyweight of treated animals increased more than 10% over 28 days. The gain was almost exclusively in lean
body mass. RAD140 is also widely cited as being neuroprotective. Such effects were demonstrated during a series of in-vivo and
in-vitro animal experiments published in 2014.1 In particular, the drug was able to protect cultured neurons from the damaging effects of the beta-amyloid protein. It also protected against neuron loss in-vivo. It was suggested RAD140 could offer some therapeutic benefit
with Alzheimer’s disease and other neurodegenerative conditions. It is of note that androgens share this protective effect. It is unclear how unique and tangible this
benefit of RAD 140 is, at present. We would caution against drawing conclusions at this time. However, this investment on the part of manufacturer Radius does suggest more
research is pending.
Several other things of note occurred in animal
experiments, which help us to further characterize RAD140. For one, only minimal elevations in liver enzyme transaminase levels were reported, even in the highest
doses tested. This suggests it has a low level of liver toxicity. Liver toxicity is often high in oral androgens, which has been a significant drawback preventing their wider use in
therapeutics. RAD140 did exhibit classic “oral androgen” effects on serum lipids, however. Its abuse could increase the risk of cardiovascular disease. RAD140 appears to exhibit a number of favorable properties on paper. This could be an effective non-steroidal muscle builder, with reduced SARM-like androgenicity in certain tissues. However, its safety and efficacy in humans has not been established. Caution is
always recommended when considering the use of new investigatory drugs.
History
RAD 140 was first described in 2010 by Miller et al.2 it was developed by Radius Health, an American biotechnologies firm. The drug has since been subject to limited number of
in-vitro (cell incubation) and in-vivo studies in animals where it demonstrated strong anabolic/androgenic separation consistent with drugs of the SARM class. It is presently in the preclinical development stage at Radius
for the treatment of breast cancer. Phase I clinical trials were also reportedly planned for patients suffering from severe weight loss associated with cancer.
RAD140 is on the WADA banned substance list, and is detectable in doping controls.
Structural Characteristics
RAD 140 is an oxadiazole aniline derived SARM. It has the chemical name 2-chloro-4-((1R,25)-1-(5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl)-2-hydroxypropylamino)-3-methylbenzonitrile. It displays high oral bioavailability
(65-75% est), and has a half-life that is amenable to once daily dosing
How Supplied
RAD140 is not available as a pharmaceutical product. Standard dosage information is unavailable. Gray market preparations commonly contain 10 mg per capsule, or a 10 mg/mL concentration in oral solution.
Warnings
RAD140 is an unapproved new drug. A thorough
understanding of its safety and propensity for side effects in humans is lacking at this time.
Side Effects
Anecdotal reports suggest the drug is generally well tolerated, with few common reports of side effects. Similar to oral androgens, this drug is expected to negatively impact HDL (good) cholesterol levels and the HDL/LDL ratio. This may increase cardiovascular disease risk
Administration
RAD140 is given orally. This substance has not been approved for use in humans. Prescribing guidelines are unavailable.
When used for physique or performance-enhancing purposes, RAD140 is commonly taken at a dosage of 10-20 mg per day (men). Women usually opt for 5-10 mg
daily, as its propensity to produce virilizing side effects is unknown. The total daily dose is usually given in one application.
During studies with moneys, the anabolic effect of 0.1mg/kg was similar to that of 1 mg/kg. This suggests its optimal anabolic dose could be near 0.1 mg/kg. If this holds true for humans, it would make the optimal equivalent human dose .0324 mg/kg, or 2.75 mg per day for someone weighing roughly 185 lbs. or as ks.
Anecdotal evidence, however, does suggest a distinctly stronger anabolic effect at the commonly used doses. Cycles of RAD140 usually last 6 to 12 weeks. Anecdotal
reports do suggest this drug has a noticeable anabolic effect. Beyond that we are not in a position to categorize its effects, as the data is too limited.
Availability
RAD140 is not available as a prescription drug product it is sold exclusively as a research compound’ or gray market supplement. Note that the quality of gray market products can be difficult to assure.