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STENDEC

Topical SARM

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How long before this stuff hits the UGL market?

 

J Med Chem. 2015 Dec 18. [Epub ahead of print]

2-Chloro-4-[[(1R,2R)-2-hydroxy-2-methyl-cyclopentyl]amino]-3-methyl-benzonitrile: A Transdermal Selective Androgen Receptor Modulator (SARM) for Muscle Atrophy.

Saeed A, Vaught GM, Gavardinas K, Matthews D, Green JE, Garcia PL, Bullock HA, Calvert NA, Patel NJ, Sweetana SA, Krishnan V, Henck JW, Luz JG, Wang Y, Jadhav P.

 

Abstract

A transdermal SARM has a potential to have therapeutic benefit through anabolic activity in muscle, while sparing undesired effects of benign prostate hyperplasia (BPH) and liver-mediated decrease in HDL-C. 2-Chloro-4-[(2-hydroxy-2-methyl-cyclopentyl)amino]-3-methyl-benzonitrile 6 showed the desired muscle and prostate effects in a preclinical ORX rat model. Compound 6 had minimal effect on HDL-C levels in cynomolgus monkeys and showed human cadaver skin permeability, thus making it an effective tool for proof of concept studies in a clinical setting.

 

PMID: 26683992

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FWIW I have been running with an oral SARM called Ostarine MK-2866 for a few weeks which appears to be delivering as promised, ie no signs of prostate issues and no other noticeable sides. Have gained several pounds of what must be lean muscle as I am visibly leaner (though heavier)  as well. 

 

I realize that you referenced a transdermal not an oral, however I thought I'd post this (anecdotal evidence) in case it might be of use.

 

If anyone is interested Ostarine appears to be currently available for sale in the USA (I'm not in the US)

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@ Stendec

 

I'm on 25mg of Ostarine per day. (I can only assume it is indeed Ostarine, getting it from a "reputable" source in my part of the world.) I'm not suggesting it's devoid of side effects, however at my age (52) I'm primarily concerned with specific issues such as BPH-like symptoms and not all that much with partial shutdown as I'm on transdermal TRT anyway. Regularly do screening and haven't seen any negative impact on the critical numbers either. This stuff is definitely not rocket fuel but I'm satisfied with the overall results when considered in context.

 

I happen to be aware of a source in the USA if anyone is interested, please note that I am not recommending or endorsing, I just stumbled across it and superficially at least, appears to be legit.

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Andrology. 2018 Mar 12. doi: 10.1111/andr.12479. [Epub ahead of print]
Development of a selective androgen receptor modulator for transdermal use in hypogonadal patients.
Krishnan V1, Patel NJ1, Mackrell JG1, Sweetana SA1, Bullock H1, Ma YL1, Waterhouse TH1, Yaden BC1, Henck J1, Zeng QQ1, Gavardinas K1, Jadhav P1, Saeed A1, Garcia-Losada P1, Robins DA1, Benson CT1.

We have identified a non-steroidal selective androgen receptor modulator (SARM), termed LY305, that is bioavailable through a transdermal route of administration while highly cleared via hepatic metabolism to limit parent compound exposure in the liver. Selection of this compound and its transdermal formulation was based on the optimization of skin absorption properties using both in vitro and in vivo skin models that supported PBPK modeling for human PK predictions. This molecule is an agonist in perineal muscle while being a weak partial agonist in the androgenic tissues such as prostate. When LY305 was tested in animal models of skeletal atrophy it restored the skeletal muscle mass through accelerated repair. In a bone fracture model, LY305 remained osteoprotective in the regenerating tissue and void of deleterious effects. Finally, in a small cohort of healthy volunteers, we assessed the safety and tolerability of LY305 when administered transdermally. LY305 showed a dose-dependent increase in serum exposure and was well tolerated with minimal adverse effects. Notably, there were no statistically significant changes to hematocrit or HDL after 4-week treatment period. Collectively, LY305 represents a first of its kind de novo development of a non-steroidal transdermal SARM with unique properties which could find clinical utility in hypogonadal men.

 

KEYWORDS:
HDL ; clinical; selective androgen receptor modulator; skeletal muscle

 

PMID: 29527831

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I'm pretty sure I recall a company that had transdermal PH's and SARM's on the UK supplement website powermyself.com 

Transformed was the name of the company, I think....too lazy to verify.

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Okay, it's Transformation Labs. And it looks like Ostarine is the only TD SARM. 

 

They also have TD; Trendione, 11Keto-testosterone, epistane, and trest.

 

Have never used their products, just thought it was (somewhat) relevant.

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