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What is Andarine?

Feb 19，2020

Andarine ((2R)-3-(4-Cyanophenoxy)-N-[4-cyano-3-(trifluoromethyl)phenyl]-2-hydroxy- 2-methyl propanamide; MK-2866; Propanamide, 3-[4-(acetylamino)phenoxy]-2-hydroxy-2-methyl -N-[4-nitro-3-(trifluoromethyl)phenyl]-, (2S)-; sarM s4; 3-(4-acetaMidophenoxy)-2-hydroxy -2-Methyl-N-[4-nitro-3-(trifluoroMethyl)phenyl]propanaMide; Andarine(GTX-007); GTx007; C19H14F3N3O3), as the arylpropionamide derivate[1], has been developed in pharmaceutical industry as a new class of therapeutics called Selective Androgen Receptor Modulator (SARM, either agonists or antagonists at particular androgen receptors) with specific selectivity for particular tissues and organs, that could substitute the synthetic anabolic drugs used in medical treatments [2].

The pharmacological activity of andarine, as an effective anabolic agonist without side-effects, has been studied in vitro and in vivo that often associated with anabolic-androgenic steroids [3]. In vitro, androgen receptor binding of the andarine was analyzed a radioligand competitive binding assay, and the results showed that andarine bound to the androgen receptor with high affinity. Thus andarine identified as potential AR agonists. In addition, in an in vitro cotransfection system, the ability of andarine (10 nM) to stimulate androgen receptor mediated transcription was determined to be 93%, suggesting that andarine has high stimulation for androgen receptor. The pharmacological activity of andarine in vivo has also been examined in a castrated rat model after 14 days of drug. The experiment results showed that andarine could casue dose-dependent stimulation for growth of prostate, seminal vesicles, and levator ani muscle, and their weights in castrated animals have been maximally promoted than intact controls, revealing the androgenic and anabolic activities of andarine in animals. As a dose rate of andarine as low as 0.3 mg/day, it was able to fully maintain the levator ani muscle weight in castrated animals at the same level as intact controls, further informing the potent and efficacious anabolic activity of andarine. The acute toxicity in animals from andarine was also performed, and drug- or dose-related changes of the hematology diagnostic indices have not been found, suggesting that andarine has not acute toxicity for animals.

The pharmacological activity of andarine suggest the great potential of andarine in the development of the clinically available SARMs, which offers unique therapeutic advantages over their steroidal counterparts and an exciting opportunity to differentially regulate the androgen effects in various target tissues, thus minimizing the interference to normal [4]. Thus, andarine has promising in advanced clinical trials that aim to treat age-related maladies and to counteract symptoms of severe diseases such as sarcopenia and cancer cachexia. However, andarine may be misused in sports where athletes and/or their handlers may seek to gain unfair advantage. Therefore, andarine as agonist is prohibited for use by the International Federation of Horseracing Authorities and the World Anti-Doping Agency [5].

References

[1] https://www.chemicalbook.com/ProductChemicalPropertiesCB82473534.htm.

[2] Cawley, A. T., Smart, C., Greer, C., Liu Lau, M., & Keledjian, J. (2016). Detection of the selective androgen receptor modulator andarine (S-4) in a routine equine blood doping control sample. Drug Test Anal, 8(2), 257-261.

[3] Yin, D., Gao, W., Kearbey, J. D., Xu, H., Chung, K., He, Y., ... & Dalton, J. T. (2003). Pharmacodynamics of selective androgen receptor modulators. Journal of Pharmacology and Experimental Therapeutics, 304(3), 1334-1340.

[4] A. Negro-Vilar. Selective androgen receptor modulators (SARMs): A novel approach to androgen therapy for the new millennium. J. Clin. Endocrinol. Metab. 1999, 84, 3459.

[5] International Federation of Horseracing Authorities. Article 6 of the International Agreement on Breeding, Racing and Wagering. Availableat: http://www.ifhaonline.org/agreementDisplay.asp#a6 [25 May 2015].