GLPG0492 is a selective androgen receptor modulator (SARM).1 It activates the androgen receptor in a transactivation assay (EC50 = 12 nM in HeLa cells expressing the human receptor). GLPG0492 (10 mg/kg per day) increases levator ani muscle weight, a marker of anabolic activity, but has no effect on ventral prostate weight, a marker of androgenic activity, in castrated rats. It increases twitch tension in isolated diaphragm strips, as well as increases the total distance run in a treadmill test and decreases gastrocnemius muscle fibrosis in the exercised-mdx mouse model of muscular dystrophy when administered at a dose of 30 mg/kg.2 GLPG0492 also reverses immobilization-induced muscle atrophy in a mouse model of hindlimb immobilization.3
1.Nique, F., Hebbe, S., Triballeau, N., et al.Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulatorJ. Med. Chem.55(19)8236-8247(2012) 2.Cozzoli, A., Capogrosso, R.F., Sblendorio, V.T., et al.GLPG0492, a novel selective androgen receptor modulator, improves muscle performance in the exercised-mdx mouse model of muscular dystrophyPharmacol. Res.729-24(2013) 3.Blanqué, R., Lepescheux, L., Auberval, M., et al.Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilizationBMC Musculoskelet. Disord.15:291(2014)