cybrsage
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RAD140 is a SARM being created and tested by Radius Health for use in cancer patients and people with muscle wasting diseases. They are also investigating it for Alzheimer's Patients. What does it do? Well, it causes the body to build muscle if you do at least a little exercising. It makes the body WANT to build muscle and as such it goes into high gear doing it. A study on rats shows a "dramatic increase" in body weight from its use which was dose dependent, most of which was lean muscle. It also showed it had absolutely no harmful effects on the liver, though it did reduce both HDL and LDL cholesterol - one of which is good to go down, the other not so much.
So what about Alzheimer's and other brain ailments? An initial study showed it has great promise for its neuroprotective properties, which is wonderful news!
They are also testing it as a treatment for breast cancer!
However, due to other drugs appearing more promising for their needs, they have back-burnered RAD140 and have not started human trials.
Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140Clinical chemistry indicated the expected lowering of lipids (LDL, HDL, triglycerides).28 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.29,30 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.31Taken in sum, 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 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. 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. We are currently preparing RAD140 for phase I clinical studies in patients suffering from severe weight loss due to cancer cachexia.
So what about Alzheimer's and other brain ailments? An initial study showed it has great promise for its neuroprotective properties, which is wonderful news!
Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. - PubMed - NCBIImportantly, 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
They are also testing it as a treatment for breast cancer!
Radius Health Has Submitted a Marketing Authorization Application for the Investigational Drug Abaloparatide-SC for the Treatment of Postmenopausal Osteoporosis in Europe (NASDAQ:RDUS)The investigational drug RAD140, a nonsteroidal selective androgen receptor modulator, or SARM, is currently in preclinical development as a potential treatment for breast cancer. The androgen receptor (AR) is highly expressed in many estrogen receptor (ER)-positive breast cancers.
•Radius expects to commence a Phase 1 trial for the investigational drug RAD140 after making an Investigational New Drug (IND) submission in 2016.
However, due to other drugs appearing more promising for their needs, they have back-burnered RAD140 and have not started human trials.
https://www.sec.gov/Archives/edgar/data/1428522/000104746914005588/a2220482zex-99_1.htmRAD140
RAD140 is a nonsteroidal selective androgen receptor modulator, or SARM, that resulted from an internal drug discovery program that began in 2005. RAD140 has demonstrated potent anabolic activity on muscle and bone in preclinical studies and has completed 28-day preclinical toxicology studies in both rats and monkeys. Because of its high anabolic efficacy, receptor selectivity, potent oral activity and long duration half-life, we believe that RAD140 has clinical potential in a number of indications where the increase in lean muscle mass and/or bone density is beneficial, such as treating the weight loss due to cancer cachexia, muscle frailty and osteoporosis, and also in the treatment of breast cancer.
We may choose to advance the RAD140 program internally or to collaborate with third parties for its further development and commercialization. Therefore, the date of any FDA approval of RAD140, if ever, cannot be predicted at this time. As a result of the uncertainties around the development strategy for RAD140, we are unable to determine the duration and costs to complete current or future clinical stages of our RAD140 product candidate.