GLPG0492

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

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1. Nique, F., Hebbe, S., Triballeau, N., et al. Identification of a 4-(hydroxymethyl)diarylhydantoin as a selective androgen receptor modulator. J. 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 dystrophy. Pharmacol. Res. 72, 9-24 (2013).

3. Blanqué, R., Lepescheux, L., Auberval, M., et al. Characterization of GLPG0492, a selective androgen receptor modulator, in a mouse model of hindlimb immobilization. BMC Musculoskelet. Disord. 15:291, (2014).