MK-4541 was first described in the scientific literature by 2014.[5][6] It was identified by screening of 3,000 compounds that were manually designed and predicted to have SARM activity.[9][5] The drug was developed by Merck.[3] It might be being developed for potential medical use, but its developmental status has not been publicly disclosed.[3] In any case, MK-4541 is not known to have advanced past preclinical studies as of 2020.[1]
^ abcFonseca GW, Dworatzek E, Ebner N, Von Haehling S (August 2020). "Selective androgen receptor modulators (SARMs) as pharmacological treatment for muscle wasting in ongoing clinical trials". Expert Opinion on Investigational Drugs. 29 (8): 881–891. doi:10.1080/13543784.2020.1777275. PMID32476495.
^ abcdeSchmidt A, Meissner RS, Gentile MA, Chisamore MJ, Opas EE, Scafonas A, et al. (September 2014). "Identification of an anabolic selective androgen receptor modulator that actively induces death of androgen-independent prostate cancer cells". The Journal of Steroid Biochemistry and Molecular Biology. 143: 29–39. doi:10.1016/j.jsbmb.2014.02.005. PMID24565564.
^ abcdChisamore MJ, Gentile MA, Dillon GM, Baran M, Gambone C, Riley S, et al. (October 2016). "A novel selective androgen receptor modulator (SARM) MK-4541 exerts anti-androgenic activity in the prostate cancer xenograft R-3327G and anabolic activity on skeletal muscle mass & function in castrated mice". The Journal of Steroid Biochemistry and Molecular Biology. 163: 88–97. doi:10.1016/j.jsbmb.2016.04.007. PMID27106747.
^ abBirudukota N, Mudgal MM, Shanbhag V (December 2019). "Discovery and development of azasteroids as anticancer agents". Steroids. 152: 108505. doi:10.1016/j.steroids.2019.108505. PMID31568765.
^ abSolomon ZJ, Mirabal JR, Mazur DJ, Kohn TP, Lipshultz LI, Pastuszak AW (January 2019). "Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications". Sexual Medicine Reviews. 7 (1): 84–94. doi:10.1016/j.sxmr.2018.09.006. PMC6326857. PMID30503797. Likewise, work by Schmidt et al. focused on MK-4541, which induces Caspase-3 activity and apoptosis in androgen independent AR positive prostate cancer cell lines while sparing AR- and AR + non-prostate cancer cells.[25] Chisamore et al. also demonstrated that administration of MK-4541 resulted in a decrease in plasma testosterone levels, likely through AR-mediated negative feedback signaling through the hypothalamic-pituitary-gonadal axis.[13]
^Li D, Zhou W, Pang J, Tang Q, Zhong B, Shen C, et al. (September 2019). "A magic drug target: Androgen receptor". Medicinal Research Reviews. 39 (5): 1485–1514. doi:10.1002/med.21558. PMID30569509. In literatures, a group of nonsteroidal SARMs (eg, RAD140 [36],153 MK‐4541 [37],154 and BA321 [38] 155) have been reported. [...] MK‐4541 was screened out from 3000 manually designed SARMs by biological experiments established to distinguish AR antagonists in PCa therapy, and then further verified by its anabolic activity.152,156