RU-59063 explained

RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was never marketed.^[1] It was originally thought to be a potent antiandrogen, but subsequent research found that it actually possesses dose-dependent androgenic activity, albeit with lower efficacy than dihydrotestosterone (DHT).^[2] The drug is an N-substituted arylthiohydantoin and was derived from the first-generation nonsteroidal antiandrogen (NSAA) nilutamide.^[3] The second-generation NSAAs enzalutamide, RD-162, and apalutamide were derived from RU-59063.^[4]

RU-59063 has high affinity for the human androgen receptor (AR) (K_i = 2.2 nM; K_a = 5.4 nM) and 1,000-fold selectivity for the AR over other nuclear steroid hormone receptors, including the,,, and . It shows 3- and 8-fold higher affinity than testosterone for the rat and human AR, respectively, and up to 100-fold higher affinity for the rat AR than the first-generation NSAAs flutamide, nilutamide, and bicalutamide. It also has slightly higher affinity for the AR than DHT and nearly equal affinity to that of the very-high-affinity AR ligand metribolone (R-1881).^{[5] [6]} In addition, RU-59063, unlike testosterone and DHT, shows no specific binding to human plasma.

See also

• Cyanonilutamide
• RU-58642
• RU-58841

External links

• Sarms & Bodybuilding
• MK 677 Sarm For Research
• MK 677 25mg
• MK-677 Dosage, Results, Bodybuilding, Reviews, Cycle and Benefits

Notes and References

1. Teutsch G, Goubet F, Battmann T, Bonfils A, Bouchoux F, Cerede E, Gofflo D, Gaillard-Kelly M, Philibert D . Non-steroidal antiandrogens: synthesis and biological profile of high-affinity ligands for the androgen receptor . J. Steroid Biochem. Mol. Biol. . 48 . 1 . 111–9 . January 1994 . 8136296 . 10.1016/0960-0760(94)90257-7 . 31404295 .
2. Cadilla R, Turnbull P . Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential . Curr Top Med Chem . 6 . 3 . 245–70 . 2006 . 16515480 . 10.2174/156802606776173456.
3. Liu B, Su L, Geng J, Liu J, Zhao G . Developments in nonsteroidal antiandrogens targeting the androgen receptor . ChemMedChem . 5 . 10 . 1651–61 . 2010 . 20853390 . 10.1002/cmdc.201000259 . 23228778 .
4. Tran C, Ouk S, Clegg NJ, Chen Y, Watson PA, Arora V, Wongvipat J, Smith-Jones PM, Yoo D, Kwon A, Wasielewska T, Welsbie D, Chen CD, Higano CS, Beer TM, Hung DT, Scher HI, Jung ME, Sawyers CL . Development of a second-generation antiandrogen for treatment of advanced prostate cancer . Science . 324 . 5928 . 787–90 . 2009 . 19359544 . 2981508 . 10.1126/science.1168175 . 2009Sci...324..787T .
5. Ran F, Xing H, Liu Y, Zhang D, Li P, Zhao G . Recent Developments in Androgen Receptor Antagonists . Archiv der Pharmazie . 348. 11. 757–775. 2015 . 26462013 . 10.1002/ardp.201500187 . 11483849 .
6. Lim AC, Attard G . Improved therapeutic targeting of the androgen receptor: rational drug design improves survival in castration-resistant prostate cancer . Curr Drug Targets . 14 . 4 . 408–19 . 2013 . 23565754 . 10.2174/1389450111314040003.