Rad-140 The Safest Anabolic Ever

July 12, 2017

Get your Research on.

 

Rad-140 a highly anabolic tissue selective SARM

 

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About RAD140


RAD140 is a non-steroidal selective androgen receptor modulator (SARM).

 

The androgen receptor (AR) is frequently expressed in many estrogen receptor (ER)-positive, ER-negative, and triple-negative breast cancers.

 

Because of its receptor and tissue selectivity, potent activity, oral bioavailability, and long half-life, RAD140 could have clinical potential in the treatment of breast cancer.

 

RAD140 resulted from an internal drug discovery program focused on the androgen receptor pathway, and exhibits a differentiated mechanism of action compared to ER-targeted therapy.

 

Rad-140 Current knowledge

 

RAD140 has all the hallmarks of a SARM.

 

It is potency selective, since it stimulates muscle weight increases at a lower dose than that required by testosterone and increases body weight over a very short time, without elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value.

 

Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations.

 

Taken in sum, RAD140 has all the hallmarks of a SARM. It stimulates lean tissue gains and increases at a lower dose than that required to stimulate prostate enlargement. 

 

Moreover, Being highly selective with full anabolic effect on muscle and demonstrating less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone.

 

RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well. We believe the overall preclinical profile of RAD140 is very good, and the compound has completed preclinical toxicology in both rats and monkeys. 
 

Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats.


Jayaraman A, et al. Endocrinology. 2014.

Abstract


The decline in testosterone levels in men during normal aging increases risks of dysfunction and disease in androgen-responsive tissues, including brain.

 

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.

 

The efficacy of SARMs in brain is largely unknown. In this study, we investigate the SARM RAD140 in cultured rat neurons and male rat brain for its ability to provide neuroprotection, 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.

 

I paraphrased this study.

Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140

The stability of RAD140 was high (t1/2 > 2 h) in incubations with rat, monkey, and human microsomes, and it also had good bioavailability in rats (F = 27−63%) and monkeys (65−75%). 

(This shows high oral bioavailability in primates.)

RAD140 demonstrated excellent affinity for the androgen receptor (Ki = 7 nM vs 29 nM for testosterone and 10 nM for DHT) as well as good selectivity over other steroidhormone nuclear receptors, with the closest off target receptor being the progesterone receptor 

RAD140 increased the weight of the levator ani muscle above that of the intact control starting with the lowest tested dose (0.1mg/kg). (RAD140 builds muscle at dosing of 10mg in a 220Lb "animal")

Interestingly, RAD140 demonstrated no stimulation of the prostate above the intact animal control level until the highest dose tested, 30 mg/kg.

 

At 0.3 mg/kg, RAD140 demonstrated muscle efficacy similar to Testosterone Propionate at 0.5 mg/kg. (I interpret this to mean 30mg RAD140 per day builds muscle as effectively as 50mg Testosterone Propionate per day in a 220Lb "animal")

MONKEY DOSING INFO

The results on animal body weight of 28-day dosing with RAD140 at 0.01 mg/kg.

 

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 ( These monkeys gained 10% muscle in 28 days with the equivalent dose of 10mg per day in a 220Lbs "monkey".

 

That means if you weigh 220Lbs, you would gain 22Lbs of lean muscle in 28 days at 10mg/day, if you respond like a monkey!) 
Muscle showed a qualitative trend that increases with dose.

 

Although  it appears that the majority of mass increase was due to lean mass increase.

 

Despite the rather dramatic increases in body weight over such a short time, there was no elevation of liver enzyme transaminase levels in any animal at any dose >2 fold over its baseline value.

 

Given the well-established relationship between oral androgen use and liver stress indicators, we were quite pleased that at a dose 10-fold greater than the fully effective dose we saw minimal liver enzyme elevations.

RAD140 is potency selective, since it stimulates muscle weight increases at a lower dose than that required to stimulate prostate weight increases. Moreover, it is also efficacy selective, because it is fully anabolic on muscle but demonstrates less than complete efficacy on the prostate and seminal vesicles and, in fact, can partially antagonize the stimulation of the seminal vesicles induced by testosterone.

 

(Taking RAD140 simultaneously with testosterone can lower some negative side effects from testosterone)

 

RAD140 has excellent pharmacokinetics and is a potent anabolic in nonhuman primates as well.

 

 

 

 

 

 

 

 

 

 

     

     

     

     

     

     

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