Sobetirome (GC1; QRX431)

Description: Sobetirome (GC-1; QRX-431) is a novel, potent and selective thyroid hormone receptor-beta (TRbeta) agonist which bind selectively to TRbeta-1 with an EC50 of 0.16 uM. Sobetirome inhibits proliferation but induces differentiation and TR beta mRNA expression in mouse and rat osteoblast-like cells. Sobetirome selectively binds to and activates TRbeta over TRalpha and this receptor selectivity led to the hypothesis that sobetirome would lower cholesterol through activation of liver TRbeta without stimulating cardiac function through TRalpha activation in the heart. The tissue selective thyromimetic properties of sobetirome have been demonstrated in numerous animal models, which led to its clinical development as a novel cholesterol-lowering agent.

References: 2 Beber EH, Capelo LP, Fonseca TL, Costa CC, Lotfi CF, Scanlan TS, Gouveia CH. The thyroid hormone receptor (TR) beta-selective agonist GC-1 inhibits proliferation but induces differentiation and TR beta mRNA expression in mouse and rat osteoblast-like cells. Calcif Tissue Int. 2009 Apr; 84(4):324-33. doi: 10.1007/s00223-009-9230-1. Epub 2009 Mar 11. PubMed PMID: 19280098.