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 = 29 nM), 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 are considered more 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 betaamyloid 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 RAD140 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 nonsteroidal 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.
• Moderate Anabolic Effect
• Low Hepatotoxicity
• No Human Studies
• Efficacy/Safety Unknown
RAD14D0 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.
RA140 is on the WADA banned substance list, and is detectable in doping controls.3
RAD140 is an oxadiazole aniline derived SARM. It has the chemical name 2-chloro-4-((1R,2S)-1-(5-(4-cyanophenyl)1,3,4-oxadiazol-2yl)-2-hydroxypropylamino)-3methylbenzonitrile. It displays high oral bioavailability (65-75% est), and has a half-life that is amenable to once daily dosing
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.
RAD140 is an unapproved new drug. A thorough understanding of its safety and propensity for side effects in humans is lacking at this time.
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.
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 1020 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 0.1 mg/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 85 kg. 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.
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.
1 Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Jayaraman A, Christensen A, Moser VA, Vest RS, Miller CP, Hattersley G, Pike CJ. Endocrinology. 2014 Apr;155(4):1398-406
2 Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140. Miller CP, Shomali M, Lyttle CR, O’Dea LS, Herendeen H, Gallacher K, Paquin D, Compton DR, Sahoo B, Kerrigan SA, Burge MS, Nickels M, Green JL, Katzenellenbogen JA, Tchesnokov A, Hattersley G. ACS Med Chem Lett. 2010 Dec 2;2(2):124-9
3 Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105. Thevis M, Piper T, Beuck S, Geyer H, Schänzer W. Rapid Commun Mass Spectrom. 2013 Jun 15;27(11):117382